Sparsentan

Identification

Summary

Sparsentan is an endothelin and angiotensin II receptor antagonist indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy at risk of rapid disease progression.

Brand Names
Filspari
Generic Name
Sparsentan
DrugBank Accession Number
DB12548
Background

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).2,5 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.2

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.5,7 Sparsentan was initially developed for the treatment of hypertension;4 however, it has shown to be efficient in the reduction of proteinuria in patients with IgAN and focal segmental glomerulosclerosis (FSGS).1,3,6 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.7 The use of sparsentan may cause hepatotoxicity and embryo-fetal toxicity.5

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 592.76
Monoisotopic: 592.271941578
Chemical Formula
C32H40N4O5S
Synonyms
  • Sparsentan
External IDs
  • PS-433540
  • PS433540
  • RE-021

Pharmacology

Indication

Sparsentan is indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy (IgAN) at risk of rapid disease progression, generally a urine protein-to-creatinine ratio (UPCR) ≥1.5 g/g.5

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Symptomatic treatment ofProteinuria••••••••••••••••••• •••• •• ••••• ••••••• •••••••••••••••••
Contraindications & Blackbox Warnings
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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.5

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.5

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).5 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.2 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.6 By acting as both an angiotensin receptor blocker (ARB) and an endothelin receptor antagonist (ERA), sparsentan reduces proteinuria in patients with IgAN.1,3,6 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.5

TargetActionsOrganism
AEndothelin-1 receptor
antagonist
Humans
AType-2 angiotensin II receptor
antagonist
Humans
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.5

Volume of distribution

At the approved recommended dosage, sparsentan has an apparent volume of distribution at steady state of 61.4 L.5

Protein binding

Sparsentan is more than 99% bound to human plasma proteins.5

Metabolism

Sparsentan is mainly metabolized by cytochrome P450 3A.5

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.5

Half-life

Sparsentan has an estimated half-life of 9.6 hours at steady state.5

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.5

Adverse Effects
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Toxicity

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.5 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.5

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Sparsentan can be increased when it is combined with Abametapir.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Sparsentan.
AbrocitinibThe serum concentration of Abrocitinib can be decreased when it is combined with Sparsentan.
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Sparsentan.
AcemetacinThe risk or severity of adverse effects can be increased when Acemetacin is combined with Sparsentan.
Food Interactions
  • 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.

Products

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International/Other Brands
Filspari (Travere Therapeutics)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FilspariTablet, film coated200 mg/1OralTravere Therapeutics, Inc.2023-02-17Not applicableUS flag
FilspariTablet, film coated400 mg/1OralTravere Therapeutics, Inc.2023-02-17Not applicableUS flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Biphenyls and derivatives
Direct Parent
Biphenyls and derivatives
Alternative Parents
Alpha amino acids and derivatives / Benzenesulfonamides / Benzenesulfonyl compounds / Benzylethers / Organosulfonamides / Imidazolinones / Imidolactams / Heteroaromatic compounds / Aminosulfonyl compounds / Isoxazoles
show 9 more
Substituents
2-imidazoline / Alpha-amino acid or derivatives / Amidine / Aminosulfonyl compound / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenesulfonamide / Benzenesulfonyl group / Benzylether
show 26 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
9242RO5URM
CAS number
254740-64-2
InChI Key
WRFHGDPIDHPWIQ-UHFFFAOYSA-N
InChI
InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35)
IUPAC Name
4'-({2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl}methyl)-N-(4,5-dimethyl-1,2-oxazol-3-yl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide
SMILES
CCCCC1=NC2(CCCC2)C(=O)N1CC1=CC=C(C(COCC)=C1)C1=CC=CC=C1S(=O)(=O)NC1=NOC(C)=C1C

References

General References
  1. Komers R, Gipson DS, Nelson P, Adler S, Srivastava T, Derebail VK, Meyers KE, Pergola P, MacNally ME, Hunt JL, 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 Int Rep. 2017 Mar 4;2(4):654-664. doi: 10.1016/j.ekir.2017.02.019. eCollection 2017 Jul. [Article]
  2. Davenport AP, Kuc RE, Southan C, Maguire JJ: New drugs and emerging therapeutic targets in the endothelin signaling pathway and prospects for personalized precision medicine. Physiol Res. 2018 Jun 27;67(Suppl 1):S37-S54. doi: 10.33549/physiolres.933872. [Article]
  3. Komers R, Diva U, Inrig JK, Loewen A, Trachtman H, Rote WE: Study Design of the Phase 3 Sparsentan Versus Irbesartan (DUPLEX) Study in Patients With Focal Segmental Glomerulosclerosis. Kidney Int Rep. 2020 Jan 8;5(4):494-502. doi: 10.1016/j.ekir.2019.12.017. eCollection 2020 Apr. [Article]
  4. Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R, Macor JE: Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. doi: 10.1021/jm049548x. [Article]
  5. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
  6. EMJ: The Dual Role of Endothelin-1 and Angiotensin II in Disease Progression of Focal Segmental Glomerulosclerosis and IgA Nephropathy (Symposium Review) [Link]
  7. Globe News Wire: Travere Therapeutics Announces FDA Accelerated Approval of FILSPARI (sparsentan), the First and Only Non-immunosuppressive Therapy for the Reduction of Proteinuria in IgA Nephropathy [Link]
PubChem Compound
10257882
PubChem Substance
347828773
ChemSpider
8433365
BindingDB
50175523
ChEMBL
CHEMBL539423
Wikipedia
Sparsentan

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentFocal Segmental Glomerulosclerosis (FSGS)1
3Active Not RecruitingTreatmentImmunoglobulin A Nephropathy1
2Active Not RecruitingTreatmentAutoimmune Disorder / Glomerulonephritis / Glomerulonephritis , IGA / Immune System Diseases / Immunoglobulin A Nephropathy / Kidney Diseases1
2Active Not RecruitingTreatmentFocal Segmental Glomerulosclerosis (FSGS)1
2CompletedTreatmentHypertension2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral200 mg/1
Tablet, film coatedOral400 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9993461No2018-06-122030-03-29US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.055 mg/mLFDA label
Predicted Properties
PropertyValueSource
Water Solubility0.0122 mg/mLALOGPS
logP5.56ALOGPS
logP6.06Chemaxon
logS-4.7ALOGPS
pKa (Strongest Acidic)5.69Chemaxon
pKa (Strongest Basic)3.52Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count6Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area114.1 Å2Chemaxon
Rotatable Bond Count11Chemaxon
Refractivity164.45 m3·mol-1Chemaxon
Polarizability66.65 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability0Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0005-0001290000-a80649d638bc833855f9
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0007-0000190000-fc30f25bf6cb1267f50a
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0075-0004190000-5ade5f5dd326d36618e5
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-00di-7200290000-71ea87e8d12175ebe8ae
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0k9l-0609780000-21cb7e5ac06c8a0c2591
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0f6x-0201970000-a9431c26faa1ad4079fc
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-242.77936
predicted
DeepCCS 1.0 (2019)
[M+H]+244.78932
predicted
DeepCCS 1.0 (2019)
[M+Na]+250.70229
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
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:...
Gene Name
EDNRA
Uniprot ID
P25101
Uniprot Name
Endothelin-1 receptor
Molecular Weight
48721.76 Da
References
  1. Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R, Macor JE: Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. doi: 10.1021/jm049548x. [Article]
  2. Komers R, Gipson DS, Nelson P, Adler S, Srivastava T, Derebail VK, Meyers KE, Pergola P, MacNally ME, Hunt JL, 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 Int Rep. 2017 Mar 4;2(4):654-664. doi: 10.1016/j.ekir.2017.02.019. eCollection 2017 Jul. [Article]
  3. Davenport AP, Kuc RE, Southan C, Maguire JJ: New drugs and emerging therapeutic targets in the endothelin signaling pathway and prospects for personalized precision medicine. Physiol Res. 2018 Jun 27;67(Suppl 1):S37-S54. doi: 10.33549/physiolres.933872. [Article]
  4. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor antagonist activity
Specific Function
Receptor for angiotensin II. Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation.
Gene Name
AGTR2
Uniprot ID
P50052
Uniprot Name
Type-2 angiotensin II receptor
Molecular Weight
41183.45 Da
References
  1. Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R, Macor JE: Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. doi: 10.1021/jm049548x. [Article]
  2. Komers R, Gipson DS, Nelson P, Adler S, Srivastava T, Derebail VK, Meyers KE, Pergola P, MacNally ME, Hunt JL, 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 Int Rep. 2017 Mar 4;2(4):654-664. doi: 10.1016/j.ekir.2017.02.019. eCollection 2017 Jul. [Article]
  3. Davenport AP, Kuc RE, Southan C, Maguire JJ: New drugs and emerging therapeutic targets in the endothelin signaling pathway and prospects for personalized precision medicine. Physiol Res. 2018 Jun 27;67(Suppl 1):S37-S54. doi: 10.33549/physiolres.933872. [Article]
  4. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. FDA Approved Drug Products: FILSPARI (sparsentan) tablets for oral use (February 2023) [Link]

Drug created at October 20, 2016 22:48 / Updated at February 27, 2023 22:24