Ciclosporin 1mg/ml eye drops preservative free
Prescription only
Requires a prescription from a doctor or prescriber
Cyclosporine is a calcineurin inhibitor known for its immunomodulatory properties that prevent organ transplant rejection and treat various inflammatory and autoimmune conditions.
Active ingredients:
Ciclosporin
Formulation:No preservatives — preferred for sensitive patients
Preservative-free
No active safety alerts
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Updated 3 months ago(16 Jan 2026)Safety monitoring data
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British National Formulary
Ciclosporin
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(14)
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Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
129 found
Half-life
19 hours
Mechanism
Cyclosporine is a calcineurin inhibitor that inhibits T cell activation.
Food interactions
4 warnings
Human targets
5 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
30%
The absorption of cyclosporine occurs mainly in the intestine.
[A174049][A189405]…
[A174049][A189405]…
Half-life
19 hours
The half-life of cyclosporine is biphasic and very variable on different conditions but it is reported in general to last 19 hours.
[A174088]…
[A174088]…
Protein binding
50%
About 50% of the administered dose is taken up by erythrocytes while about 34% is bound to lipoproteins.
[A174088]…
[A174088]…
Volume of distribution
33%
The distribution of cyclosporine in the blood consists of 33%-47% in plasma, 4%-9% in the lymphocytes, 5%-12% in the granulocytes, and 41%-58% in the erythrocytes.
[L3002]…
[L3002]…
Metabolism
10-20%
Cyclosporine is metabolized in the intestine and the liver by CYP450 enzymes, predominantly CYP3A4 with contributions from CYP3A5.
[A174049][A189402]…
[A174049][A189402]…
Elimination
3-6%
After sulfate conjugation, cyclosporine remains in the bile where it is broken down to the original compound and then re-absorbed into the circulation.…
Clearance
250 mg
Cyclosporin shows a linear clearance profile that ranges from 0.38…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Vet approved
Small molecule
About this compound
Cyclosporine is a calcineurin inhibitor known for its immunomodulatory properties that prevent organ transplant rejection and treat various inflammatory and autoimmune conditions. It is isolated from the fungus Beauveria nivea.[A174049] Initially manufactured by Sandoz and approved for use by the FDA in 1983, cyclosporine is now available in various products by Novartis (previously known as Sandoz).[L11097][L3734][L11118]
Properties:
View FDA drug labelsolid
Avg. mass: 1202.63 Da
DrugBank indication
Cyclosporine is approved for a variety of conditions. Firstly, it is approved for the prophylaxis of organ rejection in allogeneic kidney, liver, and heart transplants. It is also used to prevent bone marrow transplant rejection.
For the above indications, cyclosporine can be used in conjunction with azathioprine and corticosteroids. Finally, cyclosporine can be used in patients who have chronic transplant rejection and have received previous immunosuppressive therapy[L3002] and to prevent or treat graft-versus-host disease (GVHD).
[L11097]
Secondly, cyclosporine is used for the treatment of patients with severe active rheumatoid arthritis (RA) when they no longer respond to methotrexate alone.
[L3734]
It can be used for the treatment of adult non-immunocompromised patients with severe, recalcitrant, plaque psoriasis that have failed to respond to at least one systemic therapy or when systemic therapies are not tolerated or contraindicated.
[L3734]
The ophthalmic solution of cyclosporine is indicated to increase tear production in patients suffering from keratoconjunctivitis sicca.
[L11097]
In addition, cyclosporine is approved for the treatment of steroid dependent and steroid-resistant nephrotic syndrome due to glomerular diseases which may include minimal change nephropathy, focal and segmental glomerulosclerosis or membranous glomerulonephritis.
[L11097]
A cyclosporine ophthalmic emulsion is indicated in the treatment of vernal keratoconjunctivitis in adults and children.
[L34694]
Off-label, cyclosporine is commonly used for the treatment of various autoimmune and inflammatory conditions such as atopic dermatitis, blistering disorders, ulcerative colitis, juvenile rheumatoid arthritis, uveitis, connective tissue diseases, as well as idiopathic thrombocytopenic purpura.
[A139][A174085][A189393][A189396][A189399]
For the above indications, cyclosporine can be used in conjunction with azathioprine and corticosteroids. Finally, cyclosporine can be used in patients who have chronic transplant rejection and have received previous immunosuppressive therapy[L3002] and to prevent or treat graft-versus-host disease (GVHD).
[L11097]
Secondly, cyclosporine is used for the treatment of patients with severe active rheumatoid arthritis (RA) when they no longer respond to methotrexate alone.
[L3734]
It can be used for the treatment of adult non-immunocompromised patients with severe, recalcitrant, plaque psoriasis that have failed to respond to at least one systemic therapy or when systemic therapies are not tolerated or contraindicated.
[L3734]
The ophthalmic solution of cyclosporine is indicated to increase tear production in patients suffering from keratoconjunctivitis sicca.
[L11097]
In addition, cyclosporine is approved for the treatment of steroid dependent and steroid-resistant nephrotic syndrome due to glomerular diseases which may include minimal change nephropathy, focal and segmental glomerulosclerosis or membranous glomerulonephritis.
[L11097]
A cyclosporine ophthalmic emulsion is indicated in the treatment of vernal keratoconjunctivitis in adults and children.
[L34694]
Off-label, cyclosporine is commonly used for the treatment of various autoimmune and inflammatory conditions such as atopic dermatitis, blistering disorders, ulcerative colitis, juvenile rheumatoid arthritis, uveitis, connective tissue diseases, as well as idiopathic thrombocytopenic purpura.
[A139][A174085][A189393][A189396][A189399]
Also known as(162)
Ciclosporin
Ciclosporina
Ciclosporine
Ciclosporinum
CsA
CyA
Cyclosporin
Cyclosporin A
Dosage forms(87)
Solution (Oral) — 10 g
Solution (Ophthalmic) — 0.09 % w/v
Solution / drops (Ophthalmic; Topical) — 0.0009 mg/1mL
Solution / drops (Ophthalmic; Topical) — 0.0009 g/1mL
Solution / drops (Ophthalmic) — 0.9 mg/ml
Solution / drops (Ophthalmic) — 0.05 %
Solution (Oral) — 100 MG/ML
Solution (Oral) — 100 mg
Molecular properties(17)
Drug interactions(2401)
Known interactions with other medications. Always consult a healthcare professional.
Pimecrolimus
Unknown severity
The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cyclosporine.
Roflumilast
Unknown severity
The serum concentration of Roflumilast can be increased when it is combined with Cyclosporine.
Sipuleucel-T
Moderate
The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Cyclosporine.
Acetazolamide
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Acetazolamide.
Adalimumab
Unknown severity
The serum concentration of Cyclosporine can be decreased when it is combined with Adalimumab.
The serum concentration of Afatinib can be increased when it is combined with Cyclosporine.
The serum concentration of Aliskiren can be increased when it is combined with Cyclosporine.
Ambrisentan
Unknown severity
The serum concentration of Ambrisentan can be increased when it is combined with Cyclosporine.
Amiodarone
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Amiodarone.
Amphotericin B
Moderate
Amphotericin B may increase the nephrotoxic activities of Cyclosporine.
Ketoconazole
Moderate
Ketoconazole may increase the nephrotoxic activities of Cyclosporine.
Atorvastatin
Unknown severity
The excretion of Atorvastatin can be decreased when combined with Cyclosporine.
Boceprevir
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Boceprevir.
The serum concentration of Bosentan can be increased when it is combined with Cyclosporine.
Bromocriptine
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Bromocriptine.
Carbamazepine
Unknown severity
The serum concentration of Cyclosporine can be decreased when it is combined with Carbamazepine.
Carvedilol
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Carvedilol.
Caspofungin
Unknown severity
The risk or severity of adverse effects can be increased when Cyclosporine is combined with Caspofungin.
Chloramphenicol
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Chloramphenicol.
Cyclosporine may decrease the excretion rate of Glycochenodeoxycholic Acid which could result in a higher serum level.
Prasterone sulfate
Moderate
Cyclosporine may decrease the excretion rate of Prasterone sulfate which could result in a higher serum level.
Glimepiride
Moderate
Cyclosporine may decrease the excretion rate of Glimepiride which could result in a higher serum level.
Cyclosporine may decrease the excretion rate of Atropine which could result in a higher serum level.
Fluorescein
Moderate
Cyclosporine may decrease the excretion rate of Fluorescein which could result in a higher serum level.
Nitrofurantoin
Moderate
Cyclosporine may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.
Cyclosporine may decrease the excretion rate of Cefaclor which could result in a higher serum level.
Cyclosporine may decrease the excretion rate of Indocyanine green acid form which could result in a higher serum level.
Benzbromarone
Moderate
Cyclosporine may decrease the excretion rate of Benzbromarone which could result in a higher serum level.
Pilsicainide
Moderate
Cyclosporine may decrease the excretion rate of Pilsicainide which could result in a higher serum level.
Glycyrrhizic acid
Moderate
Cyclosporine may decrease the excretion rate of Glycyrrhizic acid which could result in a higher serum level.
Cyclosporine may decrease the excretion rate of Glipizide which could result in a higher serum level.
Rosiglitazone
Moderate
Cyclosporine may decrease the excretion rate of Rosiglitazone which could result in a higher serum level.
Tinidazole
Moderate
Cyclosporine may decrease the excretion rate of Tinidazole which could result in a higher serum level.
Cholic Acid
Moderate
Cyclosporine may decrease the excretion rate of Cholic Acid which could result in a higher serum level.
Taurocholic acid
Moderate
Cyclosporine may decrease the excretion rate of Taurocholic acid which could result in a higher serum level.
Loratadine
Moderate
Cyclosporine may decrease the excretion rate of Loratadine which could result in a higher serum level.
Dipyridamole
Moderate
Cyclosporine may decrease the excretion rate of Dipyridamole which could result in a higher serum level.
Belantamab mafodotin
Moderate
Cyclosporine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Colchicine
Unknown severity
The serum concentration of Colchicine can be increased when it is combined with Cyclosporine.
Colesevelam
Unknown severity
The serum concentration of Cyclosporine can be decreased when it is combined with Colesevelam.
Crizotinib
Unknown severity
The serum concentration of Cyclosporine can be increased when it is combined with Crizotinib.
Cyclophosphamide
Unknown severity
The serum concentration of Cyclosporine can be decreased when it is combined with Cyclophosphamide.
The serum concentration of Digoxin can be increased when it is combined with Cyclosporine.
Metildigoxin
Unknown severity
The serum concentration of Metildigoxin can be increased when it is combined with Cyclosporine.
Acetyldigoxin
Unknown severity
The serum concentration of Acetyldigoxin can be increased when it is combined with Cyclosporine.
Dronedarone
Unknown severity
The serum concentration of Dronedarone can be increased when it is combined with Cyclosporine.
The serum concentration of Edoxaban can be increased when it is combined with Cyclosporine.
The serum concentration of Cyclosporine can be decreased when it is combined with Efavirenz.
Enzalutamide
Unknown severity
The serum concentration of Cyclosporine can be decreased when it is combined with Enzalutamide.
The serum concentration of Etoposide can be increased when it is combined with Cyclosporine.
Showing 50 of 2401 interactions
Food & lifestyle interactions
Avoid Grapefruit
Avoid grapefruit products.
Advice
Avoid potassium-containing products. Taking products that increase serum potassium may increase the risk of hyperkalemia.
Advice
Avoid St. John's Wort.
Advice
Take at the same time every day. Take consistently with regard to food.
Toxicity & overdose
The oral LD50 in rats is 1480 mg/kg and the TDLO in humans is 12 mg/kg.
[L11085]
Overdose information
In cases of overdose with oral cyclosporine, forced emesis and gastric lavage are recommended 2 hours after ingestion. There are little data available in the literature regarding overdoses with cyclosporine, but hepatotoxicity and nephrotoxicity may occur.
[L3734]
One case report of an cyclosporine overdose due to medical error was made involving a 26 year old female and noted the occurrence of nausea, flushing, tremor, vertigo and vomiting, which resolved within about 1 day. Anorexia and a feeling of increased body girth were also experienced by this patient and resolved within about 2 weeks.
[A189453]
When overdose with cyclosporine is observed, it is important to consider that dialysis and charcoal, hemoperfusion are not effective techniques to remove cyclosporine from the body.
[L3734]
[L11085]
Overdose information
In cases of overdose with oral cyclosporine, forced emesis and gastric lavage are recommended 2 hours after ingestion. There are little data available in the literature regarding overdoses with cyclosporine, but hepatotoxicity and nephrotoxicity may occur.
[L3734]
One case report of an cyclosporine overdose due to medical error was made involving a 26 year old female and noted the occurrence of nausea, flushing, tremor, vertigo and vomiting, which resolved within about 1 day. Anorexia and a feeling of increased body girth were also experienced by this patient and resolved within about 2 weeks.
[A189453]
When overdose with cyclosporine is observed, it is important to consider that dialysis and charcoal, hemoperfusion are not effective techniques to remove cyclosporine from the body.
[L3734]
How it works
Mechanism of action
Cyclosporine is a calcineurin inhibitor that inhibits T cell activation.[A174049][A174088][A189411] Its binding to the receptor cyclophilin-1 inside cells produces a complex known as cyclosporine-cyclophilin. This complex subsequently inhibits calcineurin, which in turn stops the dephosphorylation as well as the activation of the nuclear factor of activated T cells (NF-AT) that normally cause inflammatory reactions. NF-AT is a transcription factor that promotes the production of cytokines such as IL-2, IL-4, interferon-gamma and TNF-alpha, all of which are involved in the inflammatory process. Specifically, the inhibition of IL-2, which is necessary for T cell activation or proliferation, is believed to be responsible for cyclosporine's immunosuppressive actions.[A174049][A189408] In addition to the above, the inhibition of NF-AT leads to lower levels of other factors associated with T helper cell function and thymocyte development.[A174049]
Pharmacodynamics
Cyclosporine exerts potent immunosuppressive actions on T cells, thereby prolonging survival following organ and bone marrow transplants.[L3734] This drug prevents and controls serious immune-mediated reactions including allograft rejection, graft versus host disease, and inflammatory autoimmune disease.[L3734]
Some notable effects of cyclosporine are hypertrichosis, gingival hyperplasia, and hyperlipidemia. There is also some debate about this drug causing nephrotoxicity.[A189402]
Some notable effects of cyclosporine are hypertrichosis, gingival hyperplasia, and hyperlipidemia. There is also some debate about this drug causing nephrotoxicity.[A189402]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
The absorption of cyclosporine occurs mainly in the intestine.
[A174049][A189405]
Absorption of cyclosporine is highly variable with a peak bioavailability of 30% sometimes occurring 1-8 hours after administration with a second peak observed in certain patients.
[A174088][L11097]
The absorption of cyclosporine from the GI tract has been found to be incomplete, likely due to first pass effects.
[A189402]
Cmax in both the blood and plasma occurs at approximately 3.5 hours post-dose.
[L3002]
The Cmax of a 0.1% cyclosporine ophthalmic emulsion is 0.67 ng/mL after instilling one drop four times daily.
[L34694]
A note on erratic absorption
During chronic administration, the absorption of Sandimmune Soft Gelatin Capsules and Oral Solution have been observed to be erratic, according to Novartis prescribing information. Those being administered the soft gelatin capsules or oral solution over the long term should be regularly monitored by testing cyclosporine blood concentrations and adjusting the dose accordingly.
[L3002]
When compared with the other oral forms of Sandimmune, Neoral capsules and solution have a higher rate of absorption that results in a higher Tmax and a 59% higher Cmax with a 29 % higher bioavailability.
[L3002]
[A174049][A189405]
Absorption of cyclosporine is highly variable with a peak bioavailability of 30% sometimes occurring 1-8 hours after administration with a second peak observed in certain patients.
[A174088][L11097]
The absorption of cyclosporine from the GI tract has been found to be incomplete, likely due to first pass effects.
[A189402]
Cmax in both the blood and plasma occurs at approximately 3.5 hours post-dose.
[L3002]
The Cmax of a 0.1% cyclosporine ophthalmic emulsion is 0.67 ng/mL after instilling one drop four times daily.
[L34694]
A note on erratic absorption
During chronic administration, the absorption of Sandimmune Soft Gelatin Capsules and Oral Solution have been observed to be erratic, according to Novartis prescribing information. Those being administered the soft gelatin capsules or oral solution over the long term should be regularly monitored by testing cyclosporine blood concentrations and adjusting the dose accordingly.
[L3002]
When compared with the other oral forms of Sandimmune, Neoral capsules and solution have a higher rate of absorption that results in a higher Tmax and a 59% higher Cmax with a 29 % higher bioavailability.
[L3002]
Half-life
The half-life of cyclosporine is biphasic and very variable on different conditions but it is reported in general to last 19 hours.
[A174088]
Prescribing information also states a terminal half-life of approximately 19 hours, but with a range between 10 to 27 hours.
[L3002]
[A174088]
Prescribing information also states a terminal half-life of approximately 19 hours, but with a range between 10 to 27 hours.
[L3002]
Protein binding
About 50% of the administered dose is taken up by erythrocytes while about 34% is bound to lipoproteins.
[A174088]
Prescribing information for Sandimmune states that 90% is mainly bound to lipoproteins.
[L3002]
[A174088]
Prescribing information for Sandimmune states that 90% is mainly bound to lipoproteins.
[L3002]
Volume of distribution
The distribution of cyclosporine in the blood consists of 33%-47% in plasma, 4%-9% in the lymphocytes, 5%-12% in the granulocytes, and 41%-58% in the erythrocytes.
[L3002]
The reported volume of distribution of cyclosporine ranges from 4-8 L/kg. It concentrates mainly in leucocyte-rich tissues as well as tissues that contain high amounts of fat because it is highly lipophilic.
[A189402]
Cyclosporine, in the eye drop formulation, crosses the blood-retinal barrier.
[A174088][A189450]
[L3002]
The reported volume of distribution of cyclosporine ranges from 4-8 L/kg. It concentrates mainly in leucocyte-rich tissues as well as tissues that contain high amounts of fat because it is highly lipophilic.
[A189402]
Cyclosporine, in the eye drop formulation, crosses the blood-retinal barrier.
[A174088][A189450]
Metabolism
Cyclosporine is metabolized in the intestine and the liver by CYP450 enzymes, predominantly CYP3A4 with contributions from CYP3A5.
[A174049][A189402]
The involvement of CYP3A7 is not clearly established.
[A189402]
Cyclosporine undergoes several metabolic pathways and about 25 different metabolites have been identified. One of its main active metabolites, AM1, demonstrates only 10-20% activity when compared to the parent drug, according to some studies.
[A174088][A189402]
The 3 primary metabolites are M1, M9, and M4N, which are produced from oxidation at the 1-beta, 9-gamma, and 4-N-demethylated positions, respectively.
[A189402]
[A174049][A189402]
The involvement of CYP3A7 is not clearly established.
[A189402]
Cyclosporine undergoes several metabolic pathways and about 25 different metabolites have been identified. One of its main active metabolites, AM1, demonstrates only 10-20% activity when compared to the parent drug, according to some studies.
[A174088][A189402]
The 3 primary metabolites are M1, M9, and M4N, which are produced from oxidation at the 1-beta, 9-gamma, and 4-N-demethylated positions, respectively.
[A189402]
Route of elimination
After sulfate conjugation, cyclosporine remains in the bile where it is broken down to the original compound and then re-absorbed into the circulation. Cyclosporine excretion is primarily biliary with only 3-6%[A189402][L3002] of the dose (including the parent drug and metabolites) excreted in the urine while 90% of the administered dose is eliminated in the bile. From the excreted proportion, under 1% of the dose is excreted as unchanged cyclosporine.
[A174088][L3002]
[A174088][L3002]
Clearance
Cyclosporin shows a linear clearance profile that ranges from 0.38 to 3 Lxh/kg[A174088], however, there is substantial inter- patient variability.
[A189402]
A 250 mg dose of cyclosporine in the oral soft gelatin capsule of a lipid micro-emulsion formulation shows an approximate clearance of 22.5 L/h.
[A189453]
[A189402]
A 250 mg dose of cyclosporine in the oral soft gelatin capsule of a lipid micro-emulsion formulation shows an approximate clearance of 22.5 L/h.
[A189453]
Drug targets(5)
Proteins and enzymes this drug interacts with in the body
Guided entry of tail-anchored proteins factor CAMLG
CAMLG
binder
Specific functionubiquitin protein ligase binding
Cellular location
Endoplasmic reticulum membrane
General function & pharmacology
Required for the post-translational delivery of tail-anchored (TA) proteins to the endoplasmic reticulum .
PMID:23041287 PMID:24392163 PMID:27226539
Together with GET1/WRB, acts as a membrane receptor for soluble GET3/TRC40, which recognizes and selectively binds the transmembrane domain of TA proteins in the cytosol .
PMID:23041287 PMID:24392163 PMID:27226539
Required for the stability of GET1 .
PMID:32187542
Stimulates calcium signaling in T cells through its involvement in elevation of intracellular calcium .
PMID:7522304
Essential for the survival of peripheral follicular B cells (By similarity)
PMID:23041287 PMID:24392163 PMID:27226539
Together with GET1/WRB, acts as a membrane receptor for soluble GET3/TRC40, which recognizes and selectively binds the transmembrane domain of TA proteins in the cytosol .
PMID:23041287 PMID:24392163 PMID:27226539
Required for the stability of GET1 .
PMID:32187542
Stimulates calcium signaling in T cells through its involvement in elevation of intracellular calcium .
PMID:7522304
Essential for the survival of peripheral follicular B cells (By similarity)
Calcineurin subunit B type 2
PPP3R2
inhibitor
Specific functioncalcium ion binding
Cellular location
Mitochondrion
General function & pharmacology
Regulatory subunit of calcineurin, a calcium-dependent, calmodulin stimulated protein phosphatase. Confers calcium sensitivity
Peptidyl-prolyl cis-trans isomerase A
PPIA
inhibitor
binder
Specific functioncyclosporin A binding
Cellular location
Cytoplasm
General function & pharmacology
Catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides .
PMID:2001362 PMID:20676357 PMID:21245143 PMID:21593166 PMID:25678563
Exerts a strong chemotactic effect on leukocytes partly through activation of one of its membrane receptors BSG/CD147, initiating a signaling cascade that culminates in MAPK/ERK activation .
PMID:11943775 PMID:21245143
Activates endothelial cells (ECs) in a pro-inflammatory manner by stimulating activation of NF-kappa-B and ERK, JNK and p38 MAP-kinases and by inducing expression of adhesion molecules including SELE and VCAM1 .
PMID:15130913
Induces apoptosis in ECs by promoting the FOXO1-dependent expression of CCL2 and BCL2L11 which are involved in EC chemotaxis and apoptosis .
PMID:31063815
In response to oxidative stress, initiates proapoptotic and antiapoptotic signaling in ECs via activation of NF-kappa-B and AKT1 and up-regulation of antiapoptotic protein BCL2 .
PMID:23180369
Negatively regulates MAP3K5/ASK1 kinase activity, autophosphorylation and oxidative stress-induced apoptosis mediated by MAP3K5/ASK1 .
PMID:26095851
Necessary for the assembly of TARDBP in heterogeneous nuclear ribonucleoprotein (hnRNP) complexes and regulates TARDBP binding to RNA UG repeats and TARDBP-dependent expression of HDAC6, ATG7 and VCP which are involved in clearance of protein aggregates .
PMID:25678563
Plays an important role in platelet activation and aggregation (By similarity). Regulates calcium mobilization and integrin ITGA2B:ITGB3 bidirectional signaling via increased ROS production as well as by facilitating the interaction between integrin and the cell cytoskeleton (By similarity). Binds heparan sulfate glycosaminoglycans .
PMID:11943775
Inhibits replication of influenza A virus (IAV) .
PMID:19207730
Inhibits ITCH/AIP4-mediated ubiquitination of matrix protein 1 (M1) of IAV by impairing the interaction of ITCH/AIP4 with M1, followed by the suppression of the nuclear export of M1, and finally reduction of the replication of IAV PMID:22347431 PMID:30328013
PMID:2001362 PMID:20676357 PMID:21245143 PMID:21593166 PMID:25678563
Exerts a strong chemotactic effect on leukocytes partly through activation of one of its membrane receptors BSG/CD147, initiating a signaling cascade that culminates in MAPK/ERK activation .
PMID:11943775 PMID:21245143
Activates endothelial cells (ECs) in a pro-inflammatory manner by stimulating activation of NF-kappa-B and ERK, JNK and p38 MAP-kinases and by inducing expression of adhesion molecules including SELE and VCAM1 .
PMID:15130913
Induces apoptosis in ECs by promoting the FOXO1-dependent expression of CCL2 and BCL2L11 which are involved in EC chemotaxis and apoptosis .
PMID:31063815
In response to oxidative stress, initiates proapoptotic and antiapoptotic signaling in ECs via activation of NF-kappa-B and AKT1 and up-regulation of antiapoptotic protein BCL2 .
PMID:23180369
Negatively regulates MAP3K5/ASK1 kinase activity, autophosphorylation and oxidative stress-induced apoptosis mediated by MAP3K5/ASK1 .
PMID:26095851
Necessary for the assembly of TARDBP in heterogeneous nuclear ribonucleoprotein (hnRNP) complexes and regulates TARDBP binding to RNA UG repeats and TARDBP-dependent expression of HDAC6, ATG7 and VCP which are involved in clearance of protein aggregates .
PMID:25678563
Plays an important role in platelet activation and aggregation (By similarity). Regulates calcium mobilization and integrin ITGA2B:ITGB3 bidirectional signaling via increased ROS production as well as by facilitating the interaction between integrin and the cell cytoskeleton (By similarity). Binds heparan sulfate glycosaminoglycans .
PMID:11943775
Inhibits replication of influenza A virus (IAV) .
PMID:19207730
Inhibits ITCH/AIP4-mediated ubiquitination of matrix protein 1 (M1) of IAV by impairing the interaction of ITCH/AIP4 with M1, followed by the suppression of the nuclear export of M1, and finally reduction of the replication of IAV PMID:22347431 PMID:30328013
Peptidyl-prolyl cis-trans isomerase F, mitochondrial
PPIF
binder
Specific functioncyclosporin A binding
Cellular location
Mitochondrion matrix
General function & pharmacology
PPIase that catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides and may therefore assist protein folding .
PMID:20676357
Involved in regulation of the mitochondrial permeability transition pore (mPTP) .
PMID:26387735
It is proposed that its association with the mPTP is masking a binding site for inhibiting inorganic phosphate (Pi) and promotes the open probability of the mPTP leading to apoptosis or necrosis; the requirement of the PPIase activity for this function is debated .
PMID:26387735
In cooperation with mitochondrial p53/TP53 is involved in activating oxidative stress-induced necrosis .
PMID:22726440
Involved in modulation of mitochondrial membrane F(1)F(0) ATP synthase activity and regulation of mitochondrial matrix adenine nucleotide levels (By similarity). Has anti-apoptotic activity independently of mPTP and in cooperation with BCL2 inhibits cytochrome c-dependent apoptosis PMID:19228691
PMID:20676357
Involved in regulation of the mitochondrial permeability transition pore (mPTP) .
PMID:26387735
It is proposed that its association with the mPTP is masking a binding site for inhibiting inorganic phosphate (Pi) and promotes the open probability of the mPTP leading to apoptosis or necrosis; the requirement of the PPIase activity for this function is debated .
PMID:26387735
In cooperation with mitochondrial p53/TP53 is involved in activating oxidative stress-induced necrosis .
PMID:22726440
Involved in modulation of mitochondrial membrane F(1)F(0) ATP synthase activity and regulation of mitochondrial matrix adenine nucleotide levels (By similarity). Has anti-apoptotic activity independently of mPTP and in cooperation with BCL2 inhibits cytochrome c-dependent apoptosis PMID:19228691
Protein phosphatase 3 catalytic subunit alpha
PPP3CA
inhibitor
Specific functionATPase binding
Cellular location
Cytoplasm
General function & pharmacology
Calcium-dependent, calmodulin-stimulated protein phosphatase which plays an essential role in the transduction of intracellular Ca(2+)-mediated signals .
PMID:15671020 PMID:18838687 PMID:19154138 PMID:23468591 PMID:30254215
Many of the substrates contain a PxIxIT motif and/or a LxVP motif .
PMID:17498738 PMID:17502104 PMID:22343722 PMID:23468591 PMID:27974827
In response to increased Ca(2+) levels, dephosphorylates and activates phosphatase SSH1 which results in cofilin dephosphorylation .
PMID:15671020
In response to increased Ca(2+) levels following mitochondrial depolarization, dephosphorylates DNM1L inducing DNM1L translocation to the mitochondrion .
PMID:18838687
Positively regulates the CACNA1B/CAV2.2-mediated Ca(2+) release probability at hippocampal neuronal soma and synaptic terminals (By similarity). Dephosphorylates heat shock protein HSPB1 (By similarity). Dephosphorylates and activates transcription factor NFATC1 .
PMID:19154138
In response to increased Ca(2+) levels, regulates NFAT-mediated transcription probably by dephosphorylating NFAT and promoting its nuclear translocation .
PMID:26248042
Dephosphorylates and inactivates transcription factor ELK1 .
PMID:19154138
Dephosphorylates DARPP32 .
PMID:19154138
May dephosphorylate CRTC2 at 'Ser-171' resulting in CRTC2 dissociation from 14-3-3 proteins .
PMID:30611118
Dephosphorylates transcription factor TFEB at 'Ser-211' following Coxsackievirus B3 infection, promoting nuclear translocation .
PMID:33691586
Required for postnatal development of the nephrogenic zone and superficial glomeruli in the kidneys, cell cycle homeostasis in the nephrogenic zone, and ultimately normal kidney function (By similarity).
Plays a role in intracellular AQP2 processing and localization to the apical membrane in the kidney, may thereby be required for efficient kidney filtration (By similarity). Required for secretion of salivary enzymes amylase, peroxidase, lysozyme and sialic acid via formation of secretory vesicles in the submandibular glands (By similarity). Required for calcineurin activity and homosynaptic depotentiation in the hippocampus (By similarity).
Required for normal differentiation and survival of keratinocytes and therefore required for epidermis superstructure formation (By similarity). Positively regulates osteoblastic bone formation, via promotion of osteoblast differentiation (By similarity). Positively regulates osteoclast differentiation, potentially via NFATC1 signaling (By similarity).
May play a role in skeletal muscle fiber type specification, potentially via NFATC1 signaling (By similarity). Negatively regulates MAP3K14/NIK signaling via inhibition of nuclear translocation of the transcription factors RELA and RELB (By similarity). Required for antigen-specific T-cell proliferation response (By similarity).
Dephosphorylates KLHL3, promoting the interaction between KLHL3 and WNK4 and subsequent degradation of WNK4 .
PMID:30718414
Negatively regulates SLC9A1 activity PMID:31375679
PMID:15671020 PMID:18838687 PMID:19154138 PMID:23468591 PMID:30254215
Many of the substrates contain a PxIxIT motif and/or a LxVP motif .
PMID:17498738 PMID:17502104 PMID:22343722 PMID:23468591 PMID:27974827
In response to increased Ca(2+) levels, dephosphorylates and activates phosphatase SSH1 which results in cofilin dephosphorylation .
PMID:15671020
In response to increased Ca(2+) levels following mitochondrial depolarization, dephosphorylates DNM1L inducing DNM1L translocation to the mitochondrion .
PMID:18838687
Positively regulates the CACNA1B/CAV2.2-mediated Ca(2+) release probability at hippocampal neuronal soma and synaptic terminals (By similarity). Dephosphorylates heat shock protein HSPB1 (By similarity). Dephosphorylates and activates transcription factor NFATC1 .
PMID:19154138
In response to increased Ca(2+) levels, regulates NFAT-mediated transcription probably by dephosphorylating NFAT and promoting its nuclear translocation .
PMID:26248042
Dephosphorylates and inactivates transcription factor ELK1 .
PMID:19154138
Dephosphorylates DARPP32 .
PMID:19154138
May dephosphorylate CRTC2 at 'Ser-171' resulting in CRTC2 dissociation from 14-3-3 proteins .
PMID:30611118
Dephosphorylates transcription factor TFEB at 'Ser-211' following Coxsackievirus B3 infection, promoting nuclear translocation .
PMID:33691586
Required for postnatal development of the nephrogenic zone and superficial glomeruli in the kidneys, cell cycle homeostasis in the nephrogenic zone, and ultimately normal kidney function (By similarity).
Plays a role in intracellular AQP2 processing and localization to the apical membrane in the kidney, may thereby be required for efficient kidney filtration (By similarity). Required for secretion of salivary enzymes amylase, peroxidase, lysozyme and sialic acid via formation of secretory vesicles in the submandibular glands (By similarity). Required for calcineurin activity and homosynaptic depotentiation in the hippocampus (By similarity).
Required for normal differentiation and survival of keratinocytes and therefore required for epidermis superstructure formation (By similarity). Positively regulates osteoblastic bone formation, via promotion of osteoblast differentiation (By similarity). Positively regulates osteoclast differentiation, potentially via NFATC1 signaling (By similarity).
May play a role in skeletal muscle fiber type specification, potentially via NFATC1 signaling (By similarity). Negatively regulates MAP3K14/NIK signaling via inhibition of nuclear translocation of the transcription factors RELA and RELB (By similarity). Required for antigen-specific T-cell proliferation response (By similarity).
Dephosphorylates KLHL3, promoting the interaction between KLHL3 and WNK4 and subsequent degradation of WNK4 .
PMID:30718414
Negatively regulates SLC9A1 activity PMID:31375679
Metabolizing enzymes(4)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP2C19Cytochrome P450 2C19
inhibitor
CYP2D6Cytochrome P450 2D6
inhibitor
CYP3A5Cytochrome P450 3A5
substrate
CYP3A4Cytochrome P450 3A4
substrate
inhibitor
Transporters(10)
Proteins that transport this drug across cell membranes
ATP-dependent translocase ABCB1
ABCB1
substrate
inhibitor
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Bile salt export pump
ABCB11
substrate
inhibitor
Specific functionABC-type bile acid transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner .
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
PMID:15791618 PMID:16332456 PMID:18985798 PMID:19228692 PMID:20010382 PMID:20398791 PMID:22262466 PMID:24711118 PMID:29507376 PMID:32203132
Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts .
PMID:16332456
Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion PMID:15901796 PMID:18245269
Ileal sodium/bile acid cotransporter
SLC10A2
inhibitor
Specific functionbile acid
Cellular location
Membrane
General function & pharmacology
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine .
PMID:7592981 PMID:9458785 PMID:9856990
Transports various bile acids, unconjugated or conjugated, such as cholate and taurocholate .
PMID:7592981 PMID:9458785 PMID:9856990
Also responsible for bile acid transport in the renal proximal tubules, a salvage mechanism that helps conserve bile acids (Probable). Works collaboratively with the Na(+)-taurocholate cotransporting polypeptide (NTCP), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
PMID:7592981 PMID:9458785 PMID:9856990
Transports various bile acids, unconjugated or conjugated, such as cholate and taurocholate .
PMID:7592981 PMID:9458785 PMID:9856990
Also responsible for bile acid transport in the renal proximal tubules, a salvage mechanism that helps conserve bile acids (Probable). Works collaboratively with the Na(+)-taurocholate cotransporting polypeptide (NTCP), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
Hepatic sodium/bile acid cotransporter
SLC10A1
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
As a major transporter of conjugated bile salts from plasma into the hepatocyte, it plays a key role in the enterohepatic circulation of bile salts necessary for the solubilization and absorption of dietary fat and fat-soluble vitamins .
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It is strictly dependent on the extracellular presence of sodium .
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It exhibits broad substrate specificity and transports various bile acids, such as taurocholate, cholate, as well as non-bile acid organic compounds, such as estrone sulfate .
PMID:14660639 PMID:34060352
Works collaboratively with the ileal transporter (NTCP2), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It is strictly dependent on the extracellular presence of sodium .
PMID:14660639 PMID:24867799 PMID:34060352 PMID:8132774
It exhibits broad substrate specificity and transports various bile acids, such as taurocholate, cholate, as well as non-bile acid organic compounds, such as estrone sulfate .
PMID:14660639 PMID:34060352
Works collaboratively with the ileal transporter (NTCP2), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation PMID:33222321
Solute carrier family 22 member 6
SLC22A6
substrate
inhibitor
Specific functionalpha-ketoglutarate transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate .
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
PMID:11669456 PMID:11907186 PMID:14675047 PMID:22108572 PMID:23832370 PMID:28534121 PMID:9950961
Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine .
PMID:9887087
Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins .
PMID:28534121
Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion .
PMID:11907186
Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP .
PMID:26377792
Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain .
PMID:22108572 PMID:23832370
May transport glutamate .
PMID:26377792
Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body .
PMID:11669456 PMID:14675047
Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate .
PMID:14675047 PMID:26377792
Xenobiotics include the mycotoxin ochratoxin (OTA) .
PMID:11669456
May also contribute to the transport of organic compounds in testes across the blood-testis-barrier PMID:35307651
ATP-binding cassette sub-family C member 10
ABCC10
substrate
inhibitor
Specific functionABC-type glutathione S-conjugate transporter activity
Cellular location
Cell membrane
General function & pharmacology
ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes physiological compounds, and xenobiotics from cells. Lipophilic anion transporter that mediates ATP-dependent transport of glucuronide conjugates such as estradiol-17-beta-o-glucuronide and GSH conjugates such as leukotriene C4 (LTC4) .
PMID:12527806 PMID:15256465
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Mediates multidrug resistance (MDR) in cancer cells by preventing the intracellular accumulation of certain antitumor drugs, such as, docetaxel and paclitaxel .
PMID:15256465 PMID:23087055
Does not transport glycocholic acid, taurocholic acid, MTX, folic acid, cAMP, or cGMP PMID:12527806
PMID:12527806 PMID:15256465
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Mediates multidrug resistance (MDR) in cancer cells by preventing the intracellular accumulation of certain antitumor drugs, such as, docetaxel and paclitaxel .
PMID:15256465 PMID:23087055
Does not transport glycocholic acid, taurocholic acid, MTX, folic acid, cAMP, or cGMP PMID:12527806
ATP-binding cassette sub-family C member 2
ABCC2
inhibitor
Specific functionABC-type glutathione S-conjugate transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
ATP-dependent transporter of the ATP-binding cassette (ABC) family that binds and hydrolyzes ATP to enable active transport of various substrates including many drugs, toxicants and endogenous compound across cell membranes. Transports a wide variety of conjugated organic anions such as sulfate-, glucuronide- and glutathione (GSH)-conjugates of endo- and xenobiotics substrates .
PMID:10220572 PMID:10421658 PMID:11500505 PMID:16332456
Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification .
PMID:10421658
Also mediates hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 .
PMID:11500505
Transports sulfated bile salt such as taurolithocholate sulfate .
PMID:16332456
Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors .
PMID:10220572 PMID:11500505 PMID:12441801
Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine PMID:10220572 PMID:11500505
PMID:10220572 PMID:10421658 PMID:11500505 PMID:16332456
Mediates hepatobiliary excretion of mono- and bis-glucuronidated bilirubin molecules and therefore play an important role in bilirubin detoxification .
PMID:10421658
Also mediates hepatobiliary excretion of others glucuronide conjugates such as 17beta-estradiol 17-glucosiduronic acid and leukotriene C4 .
PMID:11500505
Transports sulfated bile salt such as taurolithocholate sulfate .
PMID:16332456
Transports various anticancer drugs, such as anthracycline, vinca alkaloid and methotrexate and HIV-drugs such as protease inhibitors .
PMID:10220572 PMID:11500505 PMID:12441801
Confers resistance to several anti-cancer drugs including cisplatin, doxorubicin, epirubicin, methotrexate, etoposide and vincristine PMID:10220572 PMID:11500505
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
inhibitor
Specific functionABC-type xenobiotic transporter activity
Cellular location
Cell membrane
General function & pharmacology
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562
Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388
In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239
Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).
Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042
In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response
Solute carrier organic anion transporter family member 1B1
SLCO1B1
substrate
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the Na(+)-independent uptake of organic anions .
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
PMID:10358072 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463
Solute carrier organic anion transporter family member 1B3
SLCO1B3
inhibitor
Specific functionbile acid transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Mediates the Na(+)-independent uptake of organic anions .
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
PMID:10779507 PMID:15159445 PMID:17412826
Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4) .
PMID:10779507 PMID:11159893 PMID:12568656 PMID:15159445 PMID:17412826 PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions .
PMID:19129463
Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Involved in the clearance of bile acids and organic anions from the liver .
PMID:22232210
Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:15159445
May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver PMID:16624871 PMID:16627748
Scientific references(19)
Lichtiger S., Present D.H., Kornbluth A., Gelernt I., Bauer J., Galler G., Michelassi F., Hanauer S.
Cyclosporine in Severe Ulcerative Colitis Refractory to Steroid Therapy.
New England Journal of Medicine
1994330(26):1841-1845. doi: 10.1056/nejm199406303302601
Forsythe P., Paterson S.
Ciclosporin 10 years on: indications and efficacy.
Vet Rec
2014 Mar174 Suppl 2:13-21. doi: 10.1136/vr.102484
Cockerill G.W., Bert A.G., Ryan G.R., Gamble J.R., Vadas M.A., Cockerill P.N.
Regulation of granulocyte-macrophage colony-stimulating factor and E- selectin expression in endothelial cells by cyclosporin A and the T- cell transcription factor NFAT.
Blood
199586(7):2689-2698. doi: 10.1182/blood.v86.7.2689.2689
Lallemand F., Schmitt M., Bourges J.L., Gurny R., Benita S., Garrigue J.S.
Cyclosporine A delivery to the eye: A comprehensive review of academic and industrial efforts.
European Journal Pharmacy Biopharm
2017 Aug117:14-28. doi: 10.1016/j.ejpb.2017.03.006. Epub 2017 Mar 14
Faulds D., Goa K.L., Benfield P.
Cyclosporin.
A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in immunoregulatory disorders
Drugs. 1993 Jun45(6):953-1040. doi: 10.2165/00003495-199345060-00007
Kappers-Klunne M.C., van't Veer M.B.
Cyclosporin A for the treatment of patients with chronic idiopathic thrombocytopenic purpura refractory to corticosteroids or splenectomy.
British Journal Haematol
2001 Jul114(1):121-5. doi: 10.1046/j.1365-2141.2001.02893.x
Lee S.H., Chung H., Yu H.G.
Clinical outcomes of cyclosporine treatment for noninfectious uveitis.
Korean Journal Ophthalmology
2012 Feb26(1):21-5. doi: 10.3341/kjo.2012.26.1.21. Epub 2012 Jan 14
Yang T.H., Wu T.H., Chang Y.L., Liao H.T., Hsu C.C., Tsai C.Y., Chou Y.C.
Cyclosporine for the treatment of lupus nephritis in patients with systemic lupus erythematosus.
Clinical Nephrol
2018 Apr89(4):277-285. doi: 10.5414/CN109325
Barbarino J.M., Staatz C.E., Venkataramanan R., Klein T.E., Altman R.B.
PharmGKB summary: cyclosporine and tacrolimus pathways.
Pharmacogenet Genomics
2013 Oct23(10):563-85. doi: 10.1097/FPC.0b013e328364db84
Freeman D.J.
Pharmacology and pharmacokinetics of cyclosporine.
Clinical Biochemistry
1991 Feb24(1):9-14. doi: 10.1016/0009-9120(91)90084-r
Russell G., Graveley R., Seid J., al-Humidan A.K., Skjodt H.
Mechanisms of action of cyclosporine and effects on connective tissues.
Semin Arthritis Rheum
1992 Jun21(6 Suppl 3):16-22. doi: 10.1016/0049-0172(92)90009-3
Kapturczak M.H., Meier-Kriesche H.U., Kaplan B.
Pharmacology of calcineurin antagonists.
Transplant Proc
2004 Mar36(2 Suppl):25S-32S. doi: 10.1016/j.transproceed.2004.01.018
Occhiutto M.L., Freitas F.R., Maranhao R.C., Costa V.P.
Breakdown of the blood-ocular barrier as a strategy for the systemic use of nanosystems.
Pharmaceutics
2012 May 144(2):252-75. doi: 10.3390/pharmaceutics4020252
Tafazoli A.
Accidental Overdose of Oral Cyclosporine in Haematopoietic Stem Cell Transplantation: A Case Report and Literature Review.
Drug Saf Case Reports
2015 Dec2(1):20. doi: 10.1007/s40800-015-0023-3
Flechner S.M., Katz A.R., Rogers A.J., Van Buren C., Kahan B.D.
The presence of cyclosporine in body tissues and fluids during pregnancy.
American Journal Kidney Diseases
1985 Jan5(1):60-3. doi: 10.1016/s0272-6386(85)80138-4
Nyberg G., Haljamae U., Frisenette-Fich C., Wennergren M., Kjellmer I.
Breast-feeding during treatment with cyclosporine.
Transplantation
1998 Jan 2765(2):253-5. doi: 10.1097/00007890-199801270-00019
Dehesa L., Abuchar A., Nuno-Gonzalez A., Vitiello M., Kerdel F.A.
Psoriasis treated with ustekinumab in a patient with hepatitis C.
International Journal of Dermatology
201352(3):381-382. doi: 10.1111/j.1365-4632.2011.04876.x
Wang Z., Zhang L.
Treatment effect of cyclosporine A in patients with painful bladder syndrome/interstitial cystitis: A systematic review.
Experimental Therapeutics Medicine
2016 Jul12(1):445-450. doi: 10.3892/etm.2016.3301. Epub 2016 Apr 27
Tappeiner C., Roesel M., Heinz C., Michels H., Ganser G., Heiligenhaus A.
Limited value of cyclosporine A for the treatment of patients with uveitis associated with juvenile idiopathic arthritis.
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2009 May23(5):1192-8. doi: 10.1038/eye.2008.174. Epub 2008 Jun 13
ATC classification(2 codes)
ATC L04AD01
ATC S01XA18
Affected organisms(1)
Humans and other mammals
International brands(2)
Experimental properties(6)
Commercial products(120)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Additional database identifiers
Drugs Product Database (DPD)
11396
Drugs Product Database (DPD)
1915
Drugs Product Database (DPD)
13144
ChemSpider
4447449
BindingDB
50022815
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1471
GenAtlas
CAMLG
GeneCards
CAMLG
GenBank Gene Database
U18242
GenBank Protein Database
619670
UniProt Accession
CAMLG_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9318
GenAtlas
PPP3R2
GeneCards
PPP3R2
GenBank Gene Database
AF145026
GenBank Protein Database
33150800
UniProt Accession
CANB2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9253
GenAtlas
PPIA
GeneCards
PPIA
GenBank Gene Database
Y00052
GenBank Protein Database
30309
Guide to Pharmacology
2751
UniProt Accession
PPIA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9259
GenAtlas
PPIF
GeneCards
PPIF
GenBank Gene Database
M80254
GenBank Protein Database
181274
UniProt Accession
PPIF_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9314
GeneCards
PPP3CA
GenBank Gene Database
L14778
GenBank Protein Database
306477
UniProt Accession
PP2BA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2621
GeneCards
CYP2C19
GenBank Gene Database
M61854
GenBank Protein Database
181344
Guide to Pharmacology
1328
UniProt Accession
CP2CJ_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2625
GenAtlas
CYP2D6
GeneCards
CYP2D6
GenBank Gene Database
M20403
GenBank Protein Database
181350
Guide to Pharmacology
1329
UniProt Accession
CP2D6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2638
GenAtlas
CYP3A5
GeneCards
CYP3A5
GenBank Gene Database
J04813
GenBank Protein Database
181346
Guide to Pharmacology
1338
UniProt Accession
CP3A5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:42
GenAtlas
ABCB11
GeneCards
ABCB11
GenBank Gene Database
AF091582
GenBank Protein Database
3873243
Guide to Pharmacology
778
UniProt Accession
ABCBB_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10906
GeneCards
SLC10A2
GenBank Gene Database
U10417
GenBank Protein Database
595399
Guide to Pharmacology
960
UniProt Accession
NTCP2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10905
GeneCards
SLC10A1
GenBank Gene Database
L21893
GenBank Protein Database
410214
Guide to Pharmacology
959
UniProt Accession
NTCP_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10970
GenAtlas
hROAT1
GeneCards
SLC22A6
GenBank Gene Database
AF057039
GenBank Protein Database
3831566
Guide to Pharmacology
1025
UniProt Accession
S22A6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:52
GeneCards
ABCC10
GenBank Gene Database
AY032599
GenBank Protein Database
21103955
UniProt Accession
MRP7_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:53
GenAtlas
ABCC2
GeneCards
ABCC2
GenBank Gene Database
U63970
GenBank Protein Database
1764162
Guide to Pharmacology
780
UniProt Accession
MRP2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:74
GenAtlas
ABCG2
GeneCards
ABCG2
GenBank Gene Database
AF103796
GenBank Protein Database
4185796
Guide to Pharmacology
792
UniProt Accession
ABCG2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10959
GenAtlas
SLCO1B1
GeneCards
SLCO1B1
GenBank Gene Database
AF060500
GenBank Protein Database
5051630
Guide to Pharmacology
1220
UniProt Accession
SO1B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10961
GeneCards
SLCO1B3
GenBank Gene Database
AJ251506
GenBank Protein Database
9187497
Guide to Pharmacology
1221
UniProt Accession
SO1B3_HUMAN
International reference pricing
31 formulations
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
From $1.32/capsule
To $499.62/bottle
Gengraf 25 mg capsule
$1.32/capsule
Cyclosporine 25 mg softgel
$1.38/softgel capsule
Neoral 25 mg gelatin capsule
$1.53/capsule
Cyclosporine 25 mg capsule
$1.56/capsule
Sandimmune 25 mg capsule
$2.48/capsule
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
16 active patents, 15 expired
12059449
United States
Approved 13 Aug 2024 · Expires 1 Apr 2042
16 years
11413323
United States
Approved 16 Aug 2022 · Expires 11 Oct 2039
13y 6m
11154513
United States
Approved 26 Oct 2021 · Expires 20 Nov 2038
12y 7m
10813976
United States
Approved 27 Oct 2020 · Expires 22 Sept 2037
11y 5m
10918694
United States
Approved 16 Feb 2021 · Expires 28 Feb 2037
10y 11m
The earliest active patent expires November 2027. Generic versions may become available after this date.
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)