Sparsentan 400mg tablets
Prescription only
Requires a prescription from a doctor or prescriber
Tablet
400mg
Oral
Active ingredients:
Sparsentan
No active safety alerts
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Filspari 400mg tablets
Therapeutically similar medicines
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Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
Clinical guidelines and formulary information
British National Formulary
Sparsentan
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(2)
Sparsentan for treating primary IgA nephropathy (TA1074)
TA1074
Technology appraisal
Updated Oct 2025Targeted-release budesonide for treating primary IgA nephropathy (TA1128)
TA1128
Technology appraisal
Updated Feb 2026Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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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. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
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Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
32 found
Half-life
9.6 hours
Mechanism
Sparsentan is a molecule that acts as a dual antagonist of the endothelin type A…
Food interactions
1 warning
Human targets
3 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
200-1600 mg
Following administration of single doses of 200-1600 mg, the Cmax and AUC of sparsentan increase in a less than dose-proportional manner.…
Half-life
9.6 hours
Sparsentan has an estimated half-life of 9.6 hours at steady state.
[L45300]
[L45300]
Protein binding
99%
Sparsentan is more than 99% bound to human plasma proteins.
[L45300]
[L45300]
Volume of distribution
61.4 L
At the approved recommended dosage, sparsentan has an apparent volume of distribution at steady state of 61.4 L.
[L45300]
[L45300]
Metabolism
Sparsentan is mainly metabolized by cytochrome P450 3A.
[L45300]
[L45300]
Elimination
400 mg
Sparsentan is mainly excreted through feces and urine. In healthy subjects given a single dose (400 mg) of radiolabeled sparsentan, approximately…
Clearance
400 mg
Sparsentan has a time-dependent clearance, possibly due to it inducing its own metabolism over time.…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Small molecule
About this compound
Sparsentan is a dual antagonist of the endothelin type A receptor (ETAR) and the angiotensin II (Ang II) type 1 receptor (AT1R) with a similar affinity for both (9.3 nM for ETAR and 0.8 nM for AT1R).[A257330][L45300] Sparsentan is first in its class and orally active, and was created by merging the structural elements of [irbesartan], an AT1R antagonist, and biphenylsulfonamide, an ETAR antagonist.[A257330]
In February 2023, the use of sparsentan to reduce proteinuria in adults with primary immunoglobulin A nephropathy (IgAN) at risk of rapid disease progression was approved by the FDA under accelerated approval based on reduction of proteinuria.[L45300][L45315] In September 2024, it was granted full approval for an expanded indication.[L51419] Sparsentan was initially developed for the treatment of hypertension;[A257340] however, it has shown to be efficient in the reduction of proteinuria in patients with IgAN and focal segmental glomerulosclerosis (FSGS).[A257325][A257335][L45310] Compared to [irbesartan], sparsentan reduces proteinuria to a greater extent. Furthermore, it is the first non-immunosuppressive therapy for the reduction of proteinuria in IgAN.[L45315] The use of sparsentan may cause hepatotoxicity and embryo-fetal toxicity.[L45300]
On April 24, 2024, sparsentan was granted conditional marketing authorization by the European Commission for the treatment of adults with primary IgAN.[L51559]
In February 2023, the use of sparsentan to reduce proteinuria in adults with primary immunoglobulin A nephropathy (IgAN) at risk of rapid disease progression was approved by the FDA under accelerated approval based on reduction of proteinuria.[L45300][L45315] In September 2024, it was granted full approval for an expanded indication.[L51419] Sparsentan was initially developed for the treatment of hypertension;[A257340] however, it has shown to be efficient in the reduction of proteinuria in patients with IgAN and focal segmental glomerulosclerosis (FSGS).[A257325][A257335][L45310] Compared to [irbesartan], sparsentan reduces proteinuria to a greater extent. Furthermore, it is the first non-immunosuppressive therapy for the reduction of proteinuria in IgAN.[L45315] The use of sparsentan may cause hepatotoxicity and embryo-fetal toxicity.[L45300]
On April 24, 2024, sparsentan was granted conditional marketing authorization by the European Commission for the treatment of adults with primary IgAN.[L51559]
Properties:
solid
Avg. mass: 592.76 Da
DrugBank indication
Sparsentan is indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy (IgAN) at risk of disease progression.
[L51414]
[L51414]
Also known as(89)
Sparsentan
Endothelin receptor type A
ET-A
ETA
ETA-R
ETRA
hET-AR
AGTR1A
Dosage forms(2)
Tablet, film coated (Oral) — 200 mg/1
Tablet, film coated (Oral) — 400 mg/1
Molecular properties(19)
Drug interactions(779)
Known interactions with other medications. Always consult a healthcare professional.
The risk or severity of adverse effects can be increased when Aliskiren is combined with Sparsentan.
Canagliflozin
Major
The risk or severity of hypotension, hyperkalemia, and reduced intravascular volume can be increased when Canagliflozin is combined with Sparsentan.
Drospirenone
Unknown severity
The risk or severity of hyperkalemia can be increased when Sparsentan is combined with Drospirenone.
Eplerenone
Unknown severity
The risk or severity of hyperkalemia can be increased when Eplerenone is combined with Sparsentan.
The risk or severity of hyperkalemia can be increased when Ardeparin is combined with Sparsentan.
The risk or severity of hyperkalemia can be increased when Heparin is combined with Sparsentan.
Enoxaparin
Unknown severity
The risk or severity of hyperkalemia can be increased when Enoxaparin is combined with Sparsentan.
Sulodexide
Unknown severity
The risk or severity of hyperkalemia can be increased when Sulodexide is combined with Sparsentan.
Semuloparin
Unknown severity
The risk or severity of hyperkalemia can be increased when Semuloparin is combined with Sparsentan.
Danaparoid
Unknown severity
The risk or severity of hyperkalemia can be increased when Danaparoid is combined with Sparsentan.
Dalteparin
Unknown severity
The risk or severity of hyperkalemia can be increased when Dalteparin is combined with Sparsentan.
Tinzaparin
Unknown severity
The risk or severity of hyperkalemia can be increased when Tinzaparin is combined with Sparsentan.
Nadroparin
Unknown severity
The risk or severity of hyperkalemia can be increased when Nadroparin is combined with Sparsentan.
The risk or severity of hyperkalemia can be increased when Bemiparin is combined with Sparsentan.
The risk or severity of hyperkalemia can be increased when Reviparin is combined with Sparsentan.
Parnaparin
Unknown severity
The risk or severity of hyperkalemia can be increased when Parnaparin is combined with Sparsentan.
Methyclothiazide
Moderate
Methyclothiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Bendroflumethiazide
Moderate
Bendroflumethiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Benzthiazide
Moderate
Benzthiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Cyclothiazide
Moderate
Cyclothiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Hydroflumethiazide
Moderate
Hydroflumethiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Chlorothiazide
Moderate
Chlorothiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Hydrochlorothiazide
Moderate
Hydrochlorothiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Trichlormethiazide
Moderate
Trichlormethiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Polythiazide
Moderate
Polythiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Mebutizide
Moderate
Mebutizide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Cyclopenthiazide
Moderate
Cyclopenthiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Buthiazide
Moderate
Buthiazide may increase the hypotensive and Electrolyte Disturbance activities of Sparsentan.
Lithium hydroxide
Unknown severity
The serum concentration of Lithium hydroxide can be increased when it is combined with Sparsentan.
Lithium citrate
Unknown severity
The serum concentration of Lithium citrate can be increased when it is combined with Sparsentan.
Lithium carbonate
Unknown severity
The serum concentration of Lithium carbonate can be increased when it is combined with Sparsentan.
The risk or severity of hyperkalemia can be increased when Tolvaptan is combined with Sparsentan.
Trimethoprim
Unknown severity
The risk or severity of hyperkalemia can be increased when Trimethoprim is combined with Sparsentan.
Ciprofloxacin
Unknown severity
The risk or severity of hyperkalemia can be increased when Sparsentan is combined with Ciprofloxacin.
Cyclosporine
Unknown severity
The risk or severity of hyperkalemia can be increased when Sparsentan is combined with Cyclosporine.
Nicorandil
Unknown severity
The risk or severity of hyperkalemia can be increased when Nicorandil is combined with Sparsentan.
The risk or severity of adverse effects can be increased when Icosapent is combined with Sparsentan.
Indomethacin
Unknown severity
The risk or severity of adverse effects can be increased when Indomethacin is combined with Sparsentan.
Nabumetone
Unknown severity
The risk or severity of adverse effects can be increased when Nabumetone is combined with Sparsentan.
The therapeutic efficacy of Sparsentan can be decreased when used in combination with Ketorolac.
The risk or severity of adverse effects can be increased when Tenoxicam is combined with Sparsentan.
The risk or severity of adverse effects can be increased when Celecoxib is combined with Sparsentan.
The risk or severity of adverse effects can be increased when Tolmetin is combined with Sparsentan.
The risk or severity of adverse effects can be increased when Rofecoxib is combined with Sparsentan.
The risk or severity of adverse effects can be increased when Piroxicam is combined with Sparsentan.
Fenoprofen
Unknown severity
The risk or severity of adverse effects can be increased when Fenoprofen is combined with Sparsentan.
Valdecoxib
Unknown severity
The risk or severity of adverse effects can be increased when Valdecoxib is combined with Sparsentan.
Diclofenac
Unknown severity
The risk or severity of adverse effects can be increased when Diclofenac is combined with Sparsentan.
The risk or severity of adverse effects can be increased when Sulindac is combined with Sparsentan.
Flurbiprofen
Unknown severity
The risk or severity of adverse effects can be increased when Flurbiprofen is combined with Sparsentan.
Showing 50 of 779 interactions
Food & lifestyle interactions
Take in Morning
Take before a meal. Sparsentan AUC and Cmax increase following the administration of a high fat, high calorie meal. Advise patients to take the full daily dose with water prior to the morning or evening meal. Maintain the same dosing pattern in relationship to meals.
Toxicity & overdose
No overdose experience has been reported with sparsentan. Doses up to 1600 mg/day and 400 mg/day have been given to healthy volunteers and patients, respectively. Overdose of sparsentan may result in decreased blood pressure.
Provide standard supportive measures, as required, in case of an overdose. Since sparsentan is highly protein-bound, dyalisis may not be effective.
[L45300]
A 2-year rat carcinogenicity study where male and female mice received 0.7 and 26 times the AUC at the maximum recommended human dose (MRHD), respectively, found no evidence of increased incidence of neoplasia. A 26-week transgenic mouse study reported similar results. In vitro bacteria reverse mutation and chromosomal aberration assays and an in vivo rat micronucleus study did not find evidence of mutagenicity or clastogenicity for sparsentan.
Sparsentan did not lead to an impairment of fertility in male or female rats and monkeys.
[L45300]
Provide standard supportive measures, as required, in case of an overdose. Since sparsentan is highly protein-bound, dyalisis may not be effective.
[L45300]
A 2-year rat carcinogenicity study where male and female mice received 0.7 and 26 times the AUC at the maximum recommended human dose (MRHD), respectively, found no evidence of increased incidence of neoplasia. A 26-week transgenic mouse study reported similar results. In vitro bacteria reverse mutation and chromosomal aberration assays and an in vivo rat micronucleus study did not find evidence of mutagenicity or clastogenicity for sparsentan.
Sparsentan did not lead to an impairment of fertility in male or female rats and monkeys.
[L45300]
How it works
Mechanism of action
Sparsentan is a molecule that acts as a dual antagonist of the endothelin type A receptor (ETAR) and the angiotensin II (Ang II) type 1 receptor (AT1R).[L45300] It possesses two clinically validated mechanisms of action and selectively blocks the action of two potent vasoconstrictor and mitogenic agents, Ang II and endothelin 1 (ET-1), at their respective receptors.[A257330] ET-1 and Ang II contribute to the pathogenesis of immunoglobulin A nephropathy (IgAN), a condition characterized by the increased production of galactose-deficient IgA1 (Gd-IgA1) antibodies. Gd-IgA1 antibodies lead to mesangial cell activation and proliferation, which stimulates and is stimulated by ET-1 and Ang II production. The pathological cycle of IgAN results in a compromised glomerular filtration barrier and subsequent proteinuria and haematuria.[L45310] By acting as both an angiotensin receptor blocker (ARB) and an endothelin receptor antagonist (ERA), sparsentan reduces proteinuria in patients with IgAN.[A257325][A257335][L45310] Sparsentan has a high affinity for both ETAR (Ki= 12.8 nM) and AT1R (Ki=0.36 nM), and greater than 500-fold selectivity for these receptors over the endothelin type B and angiotensin II subtype 2 receptors.[L45300]
Pharmacodynamics
Sparsentan is a dual endothelin and angiotensin II receptor antagonist. At week 36, the exposure-response (E-R) relationship between sparsentan exposure and the percentage reduction from baseline in urine protein-to-creatinine ratio (UPCR) was not statistically significant over the observed sparsentan exposure range. E-R relationships were not statistically significant for any grade of hypotension or the worst grade of peripheral edema.[L45300]
In healthy subjects, sparsentan caused QTcF prolongation with a maximal mean effect of 8.8 msec at 800 mg and 8.1 msec at 1600 mg. The mechanism behind the observed QTc prolongation is unknown but is unlikely to be mediated via direct inhibition of hERG channels. At the recommended dose, no clinically relevant QTc prolongation is expected. The use of sparsentan may cause hepatotoxicity, embryo-fetal toxicity, hypotension, acute kidney injury, hyperkalemia, and fluid retention.[L45300]
In healthy subjects, sparsentan caused QTcF prolongation with a maximal mean effect of 8.8 msec at 800 mg and 8.1 msec at 1600 mg. The mechanism behind the observed QTc prolongation is unknown but is unlikely to be mediated via direct inhibition of hERG channels. At the recommended dose, no clinically relevant QTc prolongation is expected. The use of sparsentan may cause hepatotoxicity, embryo-fetal toxicity, hypotension, acute kidney injury, hyperkalemia, and fluid retention.[L45300]
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Following administration of single doses of 200-1600 mg, the Cmax and AUC of sparsentan increase in a less than dose-proportional manner. Sparsentan has time-dependent pharmacokinetics, possibly due to it inducing its own metabolism over time, and at the approved recommended dosage, it reaches steady-state plasma levels within 7 days. Following a single oral dose of 400 mg, the Cmax, AUC and median time to peak plasma concentration of sparsentan are 6.97 μg/mL, 83 μg×h/mL, and 3 hours, respectively.
Following daily doses of 400 mg sparsentan, the steady-state Cmax is 6.47 μg/mL, and the AUC is 63.6 μg×h/mL. The administration of a single oral dose (800 mg) of sparsentan with a high-fat, high-calorie meal (1000 kcal, 50% fat) increased the AUC and Cmax by 22% and 108%, respectively. With a single 200 mg dose, a high-fat, high-calorie meal did not have a clinically significant effect on sparsentan pharmacokinetics.
[L45300]
Following daily doses of 400 mg sparsentan, the steady-state Cmax is 6.47 μg/mL, and the AUC is 63.6 μg×h/mL. The administration of a single oral dose (800 mg) of sparsentan with a high-fat, high-calorie meal (1000 kcal, 50% fat) increased the AUC and Cmax by 22% and 108%, respectively. With a single 200 mg dose, a high-fat, high-calorie meal did not have a clinically significant effect on sparsentan pharmacokinetics.
[L45300]
Half-life
Sparsentan has an estimated half-life of 9.6 hours at steady state.
[L45300]
[L45300]
Protein binding
Sparsentan is more than 99% bound to human plasma proteins.
[L45300]
[L45300]
Volume of distribution
At the approved recommended dosage, sparsentan has an apparent volume of distribution at steady state of 61.4 L.
[L45300]
[L45300]
Metabolism
Sparsentan is mainly metabolized by cytochrome P450 3A.
[L45300]
[L45300]
Route of elimination
Sparsentan is mainly excreted through feces and urine. In healthy subjects given a single dose (400 mg) of radiolabeled sparsentan, approximately 80% of the dose was recovered in feces (9% unchanged) and 2% in urine (negligible amount unchanged). Within a 10-day collection period, 82% of the dosed radioactivity was recovered.
[L45300]
[L45300]
Clearance
Sparsentan has a time-dependent clearance, possibly due to it inducing its own metabolism over time. Following the initial 400 mg dose, sparsentan has an apparent clearance of 3.88 L/h. At steady state, the apparent clearance increases to 5.11 L/h.
[L45300]
[L45300]
Drug targets(3)
Proteins and enzymes this drug interacts with in the body
Endothelin-1 receptor
EDNRA
antagonist
Specific functionendothelin receptor activity
Cellular location
Cell membrane
General function & pharmacology
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3
Type-1 angiotensin II receptor
AGTR1
antagonist
Specific functionangiotensin type I receptor activity
Cellular location
Cell membrane
General function & pharmacology
Receptor for angiotensin II, a vasoconstricting peptide, which acts as a key regulator of blood pressure and sodium retention by the kidney .
PMID:15611106 PMID:1567413 PMID:25913193 PMID:26420482 PMID:30639100 PMID:32079768 PMID:8987975
The activated receptor in turn couples to G-alpha proteins G(q) (GNAQ, GNA11, GNA14 or GNA15) and thus activates phospholipase C and increases the cytosolic Ca(2+) concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C PMID:15611106
PMID:15611106 PMID:1567413 PMID:25913193 PMID:26420482 PMID:30639100 PMID:32079768 PMID:8987975
The activated receptor in turn couples to G-alpha proteins G(q) (GNAQ, GNA11, GNA14 or GNA15) and thus activates phospholipase C and increases the cytosolic Ca(2+) concentrations, which in turn triggers cellular responses such as stimulation of protein kinase C PMID:15611106
Type-2 angiotensin II receptor
AGTR2
antagonist
Specific functionangiotensin type II receptor activity
Cellular location
Cell membrane
General function & pharmacology
Receptor for angiotensin II, a vasoconstricting peptide .
PMID:28379944 PMID:29967536 PMID:31899086 PMID:8185599
Signals primarily via a non-canonical G-protein- and beta-arrestin independent pathways .
PMID:28379944
Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation PMID:15123706
PMID:28379944 PMID:29967536 PMID:31899086 PMID:8185599
Signals primarily via a non-canonical G-protein- and beta-arrestin independent pathways .
PMID:28379944
Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation PMID:15123706
Metabolizing enzymes(4)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CYP3A4Cytochrome P450 3A4
substrate
inhibitor
inducer
CYP2B6Cytochrome P450 2B6
inducer
CYP2C9Cytochrome P450 2C9
inducer
CYP2C19Cytochrome P450 2C19
inducer
Transporters(4)
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
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
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
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)
Scientific references(4)
Komers R., Gipson D.S., Nelson P., Adler S., Srivastava T., Derebail V.K., Meyers K.E., Pergola P., MacNally M.E., Hunt J.L., Shih A., Trachtman H.
Efficacy and Safety of Sparsentan Compared With Irbesartan in Patients With Primary Focal Segmental Glomerulosclerosis: Randomized, Controlled Trial Design (DUET).
Kidney International Reports
2017 Mar 42(4):654-664. doi: 10.1016/j.ekir.2017.02.019. eCollection 2017 Jul
Davenport A.P., Kuc R.E., Southan C., Maguire J.J.
New drugs and emerging therapeutic targets in the endothelin signaling pathway and prospects for personalized precision medicine.
Physiology Research
2018 Jun 2767(Suppl 1):S37-S54. doi: 10.33549/physiolres.933872
Komers R., Diva U., Inrig J.K., Loewen A., Trachtman H., Rote W.E.
Study Design of the Phase 3 Sparsentan Versus Irbesartan (DUPLEX) Study in Patients With Focal Segmental Glomerulosclerosis.
Kidney International Reports
2020 Jan 85(4):494-502. doi: 10.1016/j.ekir.2019.12.017. eCollection 2020 Apr
Murugesan N., Gu Z., Fadnis L., Tellew J.E., Baska R.A., Yang Y., Beyer S.M., Monshizadegan H., Dickinson K.E., Valentine M.T., Humphreys W.G., Lan S.J., Ewing W.R., Carlson K.E., Kowala M.C., Zahler R., Macor J.E.
Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
Journal of Medicinal Chemistry
2005 Jan 1348(1):171-9. doi: 10.1021/jm049548x
ATC classification(1 code)
ATC C09XX01
Affected organisms(1)
Humans and other mammals
International brands(1)
Experimental properties(1)
Commercial products(2)
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)
Sparsentan
Additional database identifiers
ChemSpider
8433365
BindingDB
50175523
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3179
GenAtlas
EDNRA
GeneCards
EDNRA
GenBank Gene Database
S63938
GenBank Protein Database
238636
Guide to Pharmacology
219
UniProt Accession
EDNRA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:336
GenAtlas
AGTR1
GeneCards
AGTR1
GenBank Gene Database
M91464
GenBank Protein Database
179122
Guide to Pharmacology
34
UniProt Accession
AGTR1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:338
GenAtlas
AGTR2
GeneCards
AGTR2
GenBank Gene Database
U20860
Guide to Pharmacology
35
UniProt Accession
AGTR2_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:2615
GeneCards
CYP2B6
GenBank Gene Database
M29874
GenBank Protein Database
181296
Guide to Pharmacology
1324
UniProt Accession
CP2B6_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: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: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: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:10961
GeneCards
SLCO1B3
GenBank Gene Database
AJ251506
GenBank Protein Database
9187497
Guide to Pharmacology
1221
UniProt Accession
SO1B3_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
Patent information
1 active patent
9993461
United States
Approved 12 Jun 2018 · Expires 29 Mar 2030
3y 12m
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 30 days ago(4 Mar 2026)