Deuruxolitinib 8mg tablets
Prescription only
Requires a prescription from a doctor or prescriber
Tablet
8mg
Oral
Deuruxolitinib is a deuterated form of [ruxolitinib] that selectively inhibits Janus kinases (JAK) JAK1 and JAK2.
Active ingredients:
Deuruxolitinib
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1 products
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View all licensed products for Deuruxolitinib on the MHRA register
Possibly available on the UK market
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Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
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Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
Not available
Mechanism
The Janus kinase‒signal transducer and activator of transcription (JAK-STAT) pat…
Food interactions
1 warning
Human targets
3 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
8 mg
Following oral administration of deuruxolitinib, Cmax and AUCs increased dose-proportionally over a dose range from 8 mg to 48 mg (6 times the approved recommended dosage) in healthy subjects.…
Half-life
The mean elimination half-life is approximately four hours.
[L51068]
[L51068]
Protein binding
91.5%
Deuruxolitinib plasma protein binding is 91.5% and blood to plasma concentration ratio is approximately 1.3.
[L51068]
[L51068]
Volume of distribution
50 L
The steady-state volume of distribution is approximately 50 L.
[L51068]
[L51068]
Metabolism
76%
Deuruxolitinib is primarily metabolized by CYP2C9 (76%) and CYP3A4 (21%) and to a lesser extent by CYP1A2 (3%).…
Elimination
After a single dose of radiolabeled deuruxolitinib, there was no unchanged dose recovered in either urine or feces.
[L51068]
[L51068]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Deuruxolitinib is a deuterated form of [ruxolitinib] that selectively inhibits Janus kinases (JAK) JAK1 and JAK2. Deuteration allows the drug to circumvent extensive oxidative metabolism around the cyclopentyl ring, which increases the duration of the pharmacological activity of deuruxolitinib.[A264113]
On July 26, 2024, deuruxolitinib was approved by the FDA for the treatment of severe alopecia areata.[L51083] Alopecia areata is an autoimmune condition that attacks the hair follicles and leads to unpredictable hair loss in the scalp and other areas of the body.[A264108] The Janus kinase (JAK) signal transducer and activator of transcription (STAT) pathway has been implicated in the pathophysiology of alopecia areata, as it regulates the expression of inflammatory mediators.[A264108][A264113][A264123] Deuruxolitinib works to block the inflammatory responses caused by JAKs.[L51068]
On July 26, 2024, deuruxolitinib was approved by the FDA for the treatment of severe alopecia areata.[L51083] Alopecia areata is an autoimmune condition that attacks the hair follicles and leads to unpredictable hair loss in the scalp and other areas of the body.[A264108] The Janus kinase (JAK) signal transducer and activator of transcription (STAT) pathway has been implicated in the pathophysiology of alopecia areata, as it regulates the expression of inflammatory mediators.[A264108][A264113][A264123] Deuruxolitinib works to block the inflammatory responses caused by JAKs.[L51068]
Properties:
solid
Avg. mass: 314.42 Da
DrugBank indication
Deuruxolitinib is indicated for the treatment of adult patients with severe alopecia areata. It is not recommended for use in combination with other Janus kinase (JAK) inhibitors, biologic immunomodulators, cyclosporine, or other potent immunosuppressants.
[L51068]
[L51068]
Also known as(76)
(3r)-3-(2,2,3,3,4,4,5,5-d8)cyclopentyl-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)propanenitrile
1h-pyrazole-1-propanenitrile, .beta.-(cyclopentyl-2,2,3,3,4,4,5,5-d8)-4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-, (.beta.r)-
D8-ruxolitinib
Deuruxolitinib
2.7.10.2
JAK-2
Janus kinase 2
2.7.10.2
Molecular properties(4)
Drug interactions(398)
Known interactions with other medicines. Always consult a healthcare professional.
The metabolism of Deuruxolitinib can be increased when combined with Phenytoin.
Pentobarbital
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Pentobarbital.
Carbamazepine
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Carbamazepine.
The metabolism of Deuruxolitinib can be increased when combined with Mitotane.
The metabolism of Deuruxolitinib can be increased when combined with Primidone.
The metabolism of Deuruxolitinib can be increased when combined with Rifampin.
Phenobarbital
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Phenobarbital.
Rifapentine
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Rifapentine.
Dexamethasone
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Dexamethasone.
Fosphenytoin
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Fosphenytoin.
St. John's Wort
Moderate
The metabolism of Deuruxolitinib can be increased when combined with St. John's Wort.
Midostaurin
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Midostaurin.
Enzalutamide
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Enzalutamide.
Lumacaftor
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Lumacaftor.
Apalutamide
Moderate
The metabolism of Deuruxolitinib can be increased when combined with Apalutamide.
Cyclosporine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Cyclosporine.
Fluvoxamine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Fluvoxamine.
Fluconazole
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Fluconazole.
Erythromycin
Moderate
The serum concentration of Deuruxolitinib can be increased when it is combined with Erythromycin.
Ziprasidone
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Ziprasidone.
Isradipine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Isradipine.
The metabolism of Deuruxolitinib can be decreased when combined with Diltiazem.
The metabolism of Deuruxolitinib can be decreased when combined with Clozapine.
Haloperidol
Moderate
The serum concentration of Haloperidol can be increased when it is combined with Deuruxolitinib.
Ciprofloxacin
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Ciprofloxacin.
Voriconazole
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Voriconazole.
Nicardipine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Nicardipine.
The metabolism of Deuruxolitinib can be decreased when combined with Verapamil.
Aprepitant
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Aprepitant.
The metabolism of Deuruxolitinib can be decreased when combined with Isoniazid.
Primaquine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Primaquine.
Miconazole
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Miconazole.
The metabolism of Deuruxolitinib can be decreased when combined with Danazol.
Fusidic acid
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Fusidic acid.
Zimelidine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Zimelidine.
Dronedarone
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Dronedarone.
Milnacipran
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Milnacipran.
Simeprevir
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Simeprevir.
Isavuconazonium
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Isavuconazonium.
Desvenlafaxine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Desvenlafaxine.
Nilvadipine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Nilvadipine.
Seproxetine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Seproxetine.
Linagliptin
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Linagliptin.
The metabolism of Deuruxolitinib can be decreased when combined with Indalpine.
Netupitant
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Netupitant.
Barnidipine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Barnidipine.
Benidipine
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Benidipine.
Venetoclax
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Venetoclax.
Isavuconazole
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Isavuconazole.
Fosnetupitant
Moderate
The metabolism of Deuruxolitinib can be decreased when combined with Fosnetupitant.
Showing 50 of 398 interactions
Food & lifestyle interactions
Advice
Take with or without food. Food had negligible effects on deuruxolitinib phramacokinetics.
Toxicity & overdose
There is no experience regarding human overdose with deuruxolitinib. There is no specific antidote for overdose with deuruxolitinib. Treatment should be symptomatic and supportive and monitor patients for signs and symptoms of adverse reactions.
[L51068]
There is no information regarding the acute toxicity (LD50) of deuruxolitinib.
[L51068]
There is no information regarding the acute toxicity (LD50) of deuruxolitinib.
How it works
Mechanism of action
The Janus kinase‒signal transducer and activator of transcription (JAK-STAT) pathway, which involves four JAK kinases - JAK1, JAK2, JAK3, and tyrosine kinase 2 (Tyk2) - is activated by various cytokine receptors and regulate the expression of mediators responsible for hematopoiesis and immune function, such as type I and type II cytokines and growth factors.[A264113][A264118][A264123][L51068] JAK signalling involves the recruitment of STATs (signal transducers and activators of transcription) to cytokine receptors, activation and subsequent localization of STATs to the nucleus, leading to modulation of gene expression.[L51068] Dysregulated JAK activity, leading to aberrant immune responses, has been characterized in various inflammatory conditions, including alopecia areata.[A264113] For example, high levels of IFN-γ and CD8+NKG2D+T cells, which are activated by JAK signalling, are believed to cause autoantigen expression and an autoimmune attack on hair follicles.[A264113][A264118][A264123] Deuruxolitinib is a Janus kinase (JAK) inhibitor that aims to attenuate the inflammatory response around hair follicles.[L51068] It selectively targets JAK1 and JAK2.[A264123]
Pharmacodynamics
In an in vitro kinase activity assay, deuruxolitinib had greater inhibitory potency for JAK1, JAK2 and TYK2 relative to JAK3. The relevance of inhibition of JAK enzymes to therapeutic effectiveness is not currently known.[L51068]
Deuruxolitinib inhibited whole blood IL-6 stimulated pSTAT3 in healthy subjects 2 hours postdose. The relevance of this finding in patients is unknown.[L51068]
Deuruxolitinib inhibited whole blood IL-6 stimulated pSTAT3 in healthy subjects 2 hours postdose. The relevance of this finding in patients is unknown.[L51068]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Following oral administration of deuruxolitinib, Cmax and AUCs increased dose-proportionally over a dose range from 8 mg to 48 mg (6 times the approved recommended dosage) in healthy subjects. Steady-state plasma concentrations were achieved within one to two days, with minimal accumulation, after twice daily administration.
[L51068]
Deuruxolitinib bioavailability is 90%, with peak plasma concentrations reached within 1.5 hours.
[L51068]
No clinically significant differences in the pharmacokinetics of deuruxolitinib were observed following the administration of a high-fat, high-calorie meal (approximately 50% fat and 800-1000 calories).
[L51068]
[L51068]
Deuruxolitinib bioavailability is 90%, with peak plasma concentrations reached within 1.5 hours.
[L51068]
No clinically significant differences in the pharmacokinetics of deuruxolitinib were observed following the administration of a high-fat, high-calorie meal (approximately 50% fat and 800-1000 calories).
[L51068]
Half-life
The mean elimination half-life is approximately four hours.
[L51068]
[L51068]
Protein binding
Deuruxolitinib plasma protein binding is 91.5% and blood to plasma concentration ratio is approximately 1.3.
[L51068]
[L51068]
Volume of distribution
The steady-state volume of distribution is approximately 50 L.
[L51068]
[L51068]
Metabolism
Deuruxolitinib is primarily metabolized by CYP2C9 (76%) and CYP3A4 (21%) and to a lesser extent by CYP1A2 (3%). The two most abundant human metabolites C-21714 and C-21717, each of which accounted for approximately 5% of total drug-related AUC and both are approximately 10-fold less pharmacologically active than deuruxolitinib.
[L51068]
The exact metabolic pathways of deuruxolitinib and the structures of its metabolites have not been fully characterized.
[L51068]
The exact metabolic pathways of deuruxolitinib and the structures of its metabolites have not been fully characterized.
Route of elimination
After a single dose of radiolabeled deuruxolitinib, there was no unchanged dose recovered in either urine or feces.
[L51068]
[L51068]
Drug targets(3)
Proteins and enzymes this drug interacts with in the body
Tyrosine-protein kinase JAK2
JAK2
inhibitor
Specific functionacetylcholine receptor binding
Cellular location
Endomembrane system
General function & pharmacology
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR), thrombopoietin receptor (MPL/TPOR); or type II receptors including IFN-alpha, IFN-beta, IFN-gamma and multiple interleukins .
PMID:15690087 PMID:7615558 PMID:9657743 PMID:15899890
Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins .
PMID:15690087 PMID:9618263
Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor.
Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain .
PMID:9657743
Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis.
Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B) .
PMID:21368206
In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation .
PMID:20098430
Plays a role in cell cycle by phosphorylating CDKN1B .
PMID:21423214
Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin .
PMID:19783980
Up-regulates the potassium voltage-gated channel activity of KCNA3 PMID:25644777
PMID:15690087 PMID:7615558 PMID:9657743 PMID:15899890
Following ligand-binding to cell surface receptors, phosphorylates specific tyrosine residues on the cytoplasmic tails of the receptor, creating docking sites for STATs proteins .
PMID:15690087 PMID:9618263
Subsequently, phosphorylates the STATs proteins once they are recruited to the receptor.
Phosphorylated STATs then form homodimer or heterodimers and translocate to the nucleus to activate gene transcription. For example, cell stimulation with erythropoietin (EPO) during erythropoiesis leads to JAK2 autophosphorylation, activation, and its association with erythropoietin receptor (EPOR) that becomes phosphorylated in its cytoplasmic domain .
PMID:9657743
Then, STAT5 (STAT5A or STAT5B) is recruited, phosphorylated and activated by JAK2. Once activated, dimerized STAT5 translocates into the nucleus and promotes the transcription of several essential genes involved in the modulation of erythropoiesis.
Part of a signaling cascade that is activated by increased cellular retinol and that leads to the activation of STAT5 (STAT5A or STAT5B) .
PMID:21368206
In addition, JAK2 mediates angiotensin-2-induced ARHGEF1 phosphorylation .
PMID:20098430
Plays a role in cell cycle by phosphorylating CDKN1B .
PMID:21423214
Cooperates with TEC through reciprocal phosphorylation to mediate cytokine-driven activation of FOS transcription. In the nucleus, plays a key role in chromatin by specifically mediating phosphorylation of 'Tyr-41' of histone H3 (H3Y41ph), a specific tag that promotes exclusion of CBX5 (HP1 alpha) from chromatin .
PMID:19783980
Up-regulates the potassium voltage-gated channel activity of KCNA3 PMID:25644777
Tyrosine-protein kinase JAK1
JAK1
inhibitor
Specific functionATP binding
Cellular location
Endomembrane system
General function & pharmacology
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway .
PMID:16239216 PMID:28111307 PMID:32750333 PMID:7615558 PMID:8232552
Kinase partner for the interleukin (IL)-2 receptor PMID:11909529 as well as interleukin (IL)-10 receptor .
PMID:12133952
Kinase partner for the type I interferon receptor IFNAR2 .
PMID:16239216 PMID:28111307 PMID:32750333 PMID:7615558 PMID:8232552
In response to interferon-binding to IFNAR1-IFNAR2 heterodimer, phosphorylates and activates its binding partner IFNAR2, creating docking sites for STAT proteins .
PMID:7759950
Directly phosphorylates STAT proteins but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors PMID:16239216 PMID:32750333 PMID:8232552
PMID:16239216 PMID:28111307 PMID:32750333 PMID:7615558 PMID:8232552
Kinase partner for the interleukin (IL)-2 receptor PMID:11909529 as well as interleukin (IL)-10 receptor .
PMID:12133952
Kinase partner for the type I interferon receptor IFNAR2 .
PMID:16239216 PMID:28111307 PMID:32750333 PMID:7615558 PMID:8232552
In response to interferon-binding to IFNAR1-IFNAR2 heterodimer, phosphorylates and activates its binding partner IFNAR2, creating docking sites for STAT proteins .
PMID:7759950
Directly phosphorylates STAT proteins but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors PMID:16239216 PMID:32750333 PMID:8232552
Non-receptor tyrosine-protein kinase TYK2
TYK2
inhibitor
Specific functionATP binding
General function & pharmacology
Tyrosine kinase of the non-receptor type involved in numerous cytokines and interferons signaling, which regulates cell growth, development, cell migration, innate and adaptive immunity .
PMID:10542297 PMID:10995743 PMID:7657660 PMID:7813427 PMID:8232552
Plays both structural and catalytic roles in numerous interleukins and interferons (IFN-alpha/beta) signaling .
PMID:10542297
Associates with heterodimeric cytokine receptor complexes and activates STAT family members including STAT1, STAT3, STAT4 or STAT6 .
PMID:10542297 PMID:7638186
The heterodimeric cytokine receptor complexes are composed of (1) a TYK2-associated receptor chain (IFNAR1, IL12RB1, IL10RB or IL13RA1), and (2) a second receptor chain associated either with JAK1 or JAK2 .
PMID:10542297 PMID:25762719 PMID:7526154 PMID:7813427
In response to cytokine-binding to receptors, phosphorylates and activates receptors (IFNAR1, IL12RB1, IL10RB or IL13RA1), creating docking sites for STAT members .
PMID:7526154 PMID:7657660
In turn, recruited STATs are phosphorylated by TYK2 (or JAK1/JAK2 on the second receptor chain), form homo- and heterodimers, translocate to the nucleus, and regulate cytokine/growth factor responsive genes .
PMID:10542297 PMID:25762719 PMID:7657660
Negatively regulates STAT3 activity by promototing phosphorylation at a specific tyrosine that differs from the site used for signaling PMID:29162862
PMID:10542297 PMID:10995743 PMID:7657660 PMID:7813427 PMID:8232552
Plays both structural and catalytic roles in numerous interleukins and interferons (IFN-alpha/beta) signaling .
PMID:10542297
Associates with heterodimeric cytokine receptor complexes and activates STAT family members including STAT1, STAT3, STAT4 or STAT6 .
PMID:10542297 PMID:7638186
The heterodimeric cytokine receptor complexes are composed of (1) a TYK2-associated receptor chain (IFNAR1, IL12RB1, IL10RB or IL13RA1), and (2) a second receptor chain associated either with JAK1 or JAK2 .
PMID:10542297 PMID:25762719 PMID:7526154 PMID:7813427
In response to cytokine-binding to receptors, phosphorylates and activates receptors (IFNAR1, IL12RB1, IL10RB or IL13RA1), creating docking sites for STAT members .
PMID:7526154 PMID:7657660
In turn, recruited STATs are phosphorylated by TYK2 (or JAK1/JAK2 on the second receptor chain), form homo- and heterodimers, translocate to the nucleus, and regulate cytokine/growth factor responsive genes .
PMID:10542297 PMID:25762719 PMID:7657660
Negatively regulates STAT3 activity by promototing phosphorylation at a specific tyrosine that differs from the site used for signaling PMID:29162862
Metabolizing enzymes(3)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP2C9Cytochrome P450 2C9
substrate
CYP3A4Cytochrome P450 3A4
substrate
CYP1A2Cytochrome P450 1A2
substrate
Transporters(5)
Proteins that transport this drug across cell membranes
Broad substrate specificity ATP-binding cassette transporter ABCG2
ABCG2
substrate
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
ATP-dependent translocase ABCB1
ABCB1
substrate
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
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
Organic anion transporter 3
SLC22A8
inhibitor
Specific functionorganic anion transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient .
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
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
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
PMID:14586168 PMID:15644426 PMID:15846473 PMID:16455804 PMID:31553721
Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) .
PMID:14586168 PMID:15846473 PMID:15864504 PMID:22108572 PMID:23832370
Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain .
PMID:11306713 PMID:14586168 PMID:15846473
E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange .
PMID:26377792
Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule .
PMID:11907186
Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate .
PMID:22108572 PMID:23832370
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
May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside .
PMID:15644426
May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate .
PMID:11669456 PMID:15846473 PMID:16455804
Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) .
PMID:14675047
May contribute to the release of cortisol in the adrenals .
PMID:15864504
Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB).
In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
Multidrug and toxin extrusion protein 2
SLC47A2
inhibitor
Specific functionantiporter activity
Cellular location
Cell membrane
General function & pharmacology
Multidrug efflux pump that functions as a H(+)/organic cation antiporter. Mediates the efflux of cationic compounds, such as the model cations, tetraethylammonium (TEA) and 1-methyl-4-phenylpyridinium (MPP+), the platinum-based drug oxaliplatin or weak bases that are positively charged at physiological pH, cimetidine, the platinum-based drugs cisplatin and oxaliplatin or the antidiabetic drug metformin. Mediates the efflux of endogenous compounds such as, creatinine, thiamine and estrone-3-sulfate.
Plays a physiological role in the excretion of drugs, toxins and endogenous metabolites through the kidney
Plays a physiological role in the excretion of drugs, toxins and endogenous metabolites through the kidney
Scientific references(4)
King B., Mesinkovska N., Mirmirani P., Bruce S., Kempers S., Guttman-Yassky E., Roberts J.L., McMichael A., Colavincenzo M., Hamilton C., Braman V., Cassella J.V.
Phase 2 randomized, dose-ranging trial of CTP-543, a selective Janus Kinase inhibitor, in moderate-to-severe alopecia areata.
Journal American Academy Dermatology
2022 Aug87(2):306-313. doi: 10.1016/j.jaad.2022.03.045. Epub 2022 Mar 29
Yan T., Wang T., Tang M., Liu N.
Comparative efficacy and safety of JAK inhibitors in the treatment of moderate-to-severe alopecia areata: a systematic review and network meta-analysis.
Front Pharmacology
2024 Apr 1015:1372810. doi: 10.3389/fphar.2024.1372810. eCollection 2024
Barati Sedeh F., Michaelsdottir T.E., Henning M.A.S., Jemec G.B.E., Ibler K.S.
Comparative Efficacy and Safety of Janus Kinase Inhibitors Used in Alopecia Areata: A Systematic Review and Meta-analysis.
Acta Derm Venereol
2023 Jan 25103:adv00855. doi: 10.2340/actadv.v103.4536
Sardana K., Bathula S., Khurana A.
Which is the Ideal JAK Inhibitor for Alopecia Areata - Baricitinib, Tofacitinib, Ritlecitinib or Ifidancitinib - Revisiting the Immunomechanisms of the JAK Pathway.
Indian Dermatology Online Journal
2023 Jun 2814(4):465-474. doi: 10.4103/idoj.idoj_452_22. eCollection 2023 Jul-Aug
Affected organisms(1)
Humans and other mammals
Salt forms(1)
Deuruxolitinib phosphate(DBSALT003523)
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)
Deuruxolitinib
Additional database identifiers
ChemSpider
115010950
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6192
GenAtlas
JAK2
GeneCards
JAK2
GenBank Gene Database
AF058925
Guide to Pharmacology
2048
UniProt Accession
JAK2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6190
GeneCards
JAK1
Guide to Pharmacology
2047
UniProt Accession
JAK1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:12440
GeneCards
TYK2
GenBank Gene Database
X54637
GenBank Protein Database
37504
Guide to Pharmacology
2269
UniProt Accession
TYK2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_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:2596
GenAtlas
CYP1A2
GeneCards
CYP1A2
GenBank Gene Database
Z00036
Guide to Pharmacology
1319
UniProt Accession
CP1A2_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: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:10972
GeneCards
SLC22A8
GenBank Gene Database
AF097491
GenBank Protein Database
4378059
Guide to Pharmacology
1027
UniProt Accession
S22A8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:26439
GeneCards
SLC47A2
Guide to Pharmacology
1217
UniProt Accession
S47A2_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite:
- DrugBank 6.02024Recommended citationKnox C., Wilson M., Klinger C.M., et alDrugBank 6.0: the DrugBank Knowledgebase for 2024Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
- DrugBank 5.02018Wishart D.S., Feunang Y.D., Guo A.C., et alDrugBank 5.0: a major update to the DrugBank database for 2018Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
- DrugBank 4.02014Law V., Knox C., Djoumbou Y., et alDrugBank 4.0: shedding new light on drug metabolismNucleic Acids Res. 2014 Jan 142(1):D1091-7
- DrugBank 3.02011Knox C., Law V., Jewison T., et alDrugBank 3.0: a comprehensive resource for 'omics' research on drugsNucleic Acids Res. 2011 Jan39(Database issue):D1035-41
- DrugBank 2.02008Wishart D.S., Knox C., Guo A.C., et alDrugBank: a knowledgebase for drugs, drug actions and drug targets.Nucleic Acids Research2008 Jan36(Database issue):D901-6
- DrugBank 1.02006Wishart D.S., Knox C., Guo A.C., et alDrugBank: a comprehensive resource for in silico drug discovery and exploration.Nucleic Acids Research2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 4 Mar 2026Structured knowledge from the free knowledge base
drugbank match (98%)
Linked open data from Wikidata (Q123485858), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication.
Source: Q123485858CC0 1.0
Updated 31 Oct 2026