Daprodustat

Identification

Summary

Daprodustat is a small-molecule hypoxia-inducible factor prolyl hydroxylase inhibitor used for the treatment of anemia in patients with chronic kidney disease.

Brand Names
Jesduvroq
Generic Name
Daprodustat
DrugBank Accession Number
DB11682
Background

Daprodustat is a small-molecule hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor that was developed by GSK.2,3 Patients with CKD cannot induce erythropoietin (EPO) production in response to hypoxia or anemia. As a potent inhibitor of PHD1, PHD2 and PHD3 (≥ 1000-fold selectivity), daprodustat stabilizes cellular HIF1α and HIF2α and the induces erythropoiesis.1 A phase 3 clinical trial (NCT02879305) found that in patients with CKD undergoing dialysis, daprodustat was non-inferior to erythropoiesis-stimulating agents regarding the change in the hemoglobin level from baseline and cardiovascular outcomes.4

In June 2020, daprodustat was first approved in Japan for the treatment of renal anemia.1 On October 2022, the FDA Cardiovascular and Renal Drugs Advisory Committee (CRDAC) supported that the benefit of treatment with daprodustat outweighs the risks for adult dialysis patients with anemia of CKD but not for non-dialysis patients with anemia of CKD.7 On February 1, 2023, daprodustat was fully approved by the FDA as the first oral treatment for anemia caused by chronic kidney disease in patients on dialysis.9 The drug is currently under EMA review.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 393.44
Monoisotopic: 393.189985601
Chemical Formula
C19H27N3O6
Synonyms
  • Daprodustat
  • Glycine, N-((1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl)-
External IDs
  • GSK-1278863
  • GSK1278863

Pharmacology

Indication

Daprodustat is a hypoxia-inducible factor prolyl hydroxylase (HIF PH) inhibitor indicated for the treatment of anemia due to chronic kidney disease in adults who have been receiving dialysis for at least four months.8

The US prescribing information for daprodustat indicates that the drug was not shown to improve quality of life, fatigue, or patient well-being. It is not advised to be used as a substitute for transfusion in patients requiring immediate correction of anemia. It is also not indicated in patients not on dialysis.8

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in treatment ofAnemia•••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Daprodustat is Daprodustat increases endogenous erythropoietin in a dose-dependent manner within six to eight hours after administration. With repeated doses, peak increases in reticulocyte counts occurred in seven to 15 days, with subsequent increases in red blood cell production. New hemoglobin steady-state levels are reached several weeks (approximately four weeks in ESA-users and approximately 16-20 weeks in ESA-non-users) after initial administration.8

Daprodustat also increased serum transferrin and total iron binding capacity (TIBC) and decreased serum ferritin, transferrin saturation, and hepcidin when administered for 52 weeks in adults on dialysis with anemia due to CKD.8

Mechanism of action

Chronic kidney disease (CKD) is associated with several complications, including anemia. The development of anemia in patients with CKD is mostly due to the kidneys' inability to produce a sufficient amount of erythropoietin (EPO).1,3 Daprodustat is a potent reversible inhibitor of hypoxia-inducible factor (HIF)-prolyl hydroxylase (PH) 1, PH2 and PH3, with an IC50 in the low nM range. By inhibiting HIF-PHDs, daprodustat promotes the stabilization and nuclear accumulation of HIF-1α and HIF-2α transcription factors.8 HIF-α translocates to the nucleus and binds to hypoxia response elements (HREs) on DNA 1,3 to promote the production of EPO as well as proteins involved in iron uptake, mobilization, and transport.2 Ultimately, erythropoiesis is increased, iron transport is upregulated, and circulating Hb levels are elevated.1,3,2

TargetActionsOrganism
AEgl nine homolog 1
inhibitor
Humans
AEgl nine homolog 2
inhibitor
Humans
AEgl nine homolog 3
inhibitor
Humans
Absorption

Daprodustat exposure generally increases in a dose-proportional manner over the range of therapeutic doses. Steady-state concentrations are achieved within 24 hours of dosing. Following oral administration, daprodustat is readily absorbed with a median time to peak concentration (Tmax) in healthy subjects ranging from one to four hours. The absolute bioavailability of daprodustat is 65%. Administration of daprodustat with a high-fat or high-calorie meal did not significantly alter daprodustat exposure compared to administration in the fasted state.8

Volume of distribution

Daprodustat has an approximately equal distribution between plasma and blood cells (blood:plasma ratio of 1.23). Following intravenous dosing, the volume of distribution at steady-state in healthy subjects is 14.3 L.8

Protein binding

In vitro, plasma protein binding of daprodustat is >99%.8

Metabolism

In vitro, daprodustat is primarily metabolized by CYP2C8 (95% contribution), with a minor contribution by CYP3A4 (5%). Following oral or intravenous administration of radiolabeled daprodustat to healthy adults, approximately 40% of the total circulating radioactivity in plasma was daprodustat, and the remaining 60% was metabolites.8

The parent drug is the principal circulating component in plasma.8 Of the six metabolites of daprodustat that were characterized, the major metabolites were M2 (GSK2391220), M3 (GSK2506104), and M13 (GSK2531401), with each metabolite accounting for more than 10% of circulating radioactivity in plasma.5 In humans, each metabolite circulates primarily as a single stereoisomeric form.6 In vitro and non-clinical studies suggest that these identified metabolites have a comparable pharmacological activity to the parent drug; however, the extent of the pharmacological contribution of each metabolite is unknown.5,8

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Route of elimination

Within seven days of an oral dose of radiolabeled daprodustat, 74% of the radioactivity was recovered in the feces, and 21% of the radioactivity was recovered in the urine. Approximately 99.5% of the dose was excreted as oxidative metabolites, with the remaining fraction representing the unchanged parent drug.8

Half-life

The terminal elimination half-life of daprodustat ranges from one to four hours.8

Clearance

Mean clearance from plasma was 18.9 L/h, which correlates to blood clearance of 15 L/h and equates to a hepatic extraction of approximately 18%.8

Adverse Effects
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Toxicity

Headache and gastrointestinal adverse reactions (e.g., nausea) may be seen with acute overdose with daprodustat. There is no specific antidote. Hemodialysis will not substantially remove daprodustat because it is highly protein bound.8

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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
AbataceptThe metabolism of Daprodustat can be increased when combined with Abatacept.
AbirateroneThe metabolism of Daprodustat can be decreased when combined with Abiraterone.
AdalimumabThe metabolism of Daprodustat can be increased when combined with Adalimumab.
AlmotriptanThe metabolism of Daprodustat can be decreased when combined with Almotriptan.
AlpelisibThe metabolism of Daprodustat can be decreased when combined with Alpelisib.
Food Interactions
  • Take with or without food. Food does not affect drug absorption or exposure. Daprodustat can be taken without regard to concomitant administration of iron or phosphate binders, and it can be administered without regard to the timing or type of dialysis.

Products

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International/Other Brands
Duvroq (GlaxoSmithKline)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
JesduvroqTablet, film coated8 mg/1OralGlaxoSmithKline LLC2023-02-01Not applicableUS flag
JesduvroqTablet, film coated2 mg/1OralGlaxoSmithKline LLC2023-02-01Not applicableUS flag
JesduvroqTablet, film coated6 mg/1OralGlaxoSmithKline LLC2023-02-01Not applicableUS flag
JesduvroqTablet, film coated1 mg/1OralGlaxoSmithKline LLC2023-02-01Not applicableUS flag
JesduvroqTablet, film coated4 mg/1OralGlaxoSmithKline LLC2023-02-01Not applicableUS flag

Categories

ATC Codes
B03XA07 — Daprodustat
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as n-acyl-alpha amino acids. These are compounds containing an alpha amino acid which bears an acyl group at its terminal nitrogen atom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
N-acyl-alpha amino acids
Alternative Parents
Barbituric acid derivatives / N-acyl ureas / Diazinanes / 1,3-dicarbonyl compounds / Dicarboximides / Secondary carboxylic acid amides / Monocarboxylic acids and derivatives / Carboxylic acids / Azacyclic compounds / Organopnictogen compounds
show 3 more
Substituents
1,3-diazinane / 1,3-dicarbonyl compound / Aliphatic heteromonocyclic compound / Azacycle / Barbiturate / Carbonic acid derivative / Carbonyl group / Carboxamide group / Carboxylic acid / Dicarboximide
show 16 more
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
JVR38ZM64B
CAS number
960539-70-2
InChI Key
RUEYEZADQJCKGV-UHFFFAOYSA-N
InChI
InChI=1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,15H,1-11H2,(H,20,25)(H,23,24)
IUPAC Name
2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinan-5-yl)formamido]acetic acid
SMILES
OC(=O)CNC(=O)C1C(=O)N(C2CCCCC2)C(=O)N(C2CCCCC2)C1=O

References

General References
  1. Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
  2. Zheng Q, Wang Y, Yang H, Sun L, Fu X, Wei R, Liu YN, Liu WJ: Efficacy and Safety of Daprodustat for Anemia Therapy in Chronic Kidney Disease Patients: A Systematic Review and Meta-Analysis. Front Pharmacol. 2021 Jan 12;11:573645. doi: 10.3389/fphar.2020.573645. eCollection 2020. [Article]
  3. Becker KA, Jones JJ: An Emerging Treatment Alternative for Anemia in Chronic Kidney Disease Patients: A Review of Daprodustat. Adv Ther. 2018 Jan;35(1):5-11. doi: 10.1007/s12325-017-0655-z. Epub 2017 Dec 28. [Article]
  4. Singh AK, Carroll K, Perkovic V, Solomon S, Jha V, Johansen KL, Lopes RD, Macdougall IC, Obrador GT, Waikar SS, Wanner C, Wheeler DC, Wiecek A, Blackorby A, Cizman B, Cobitz AR, Davies R, Dole J, Kler L, Meadowcroft AM, Zhu X, McMurray JJV: Daprodustat for the Treatment of Anemia in Patients Undergoing Dialysis. N Engl J Med. 2021 Dec 16;385(25):2325-2335. doi: 10.1056/NEJMoa2113379. Epub 2021 Nov 5. [Article]
  5. Mahar KM, Caltabiano S, Andrews S, Ramanjineyulu B, Chen L, Young G, Pereira A, Lindsay AC, van den Berg F, Cobitz AR: Clinical Pharmacokinetics of Daprodustat: Results of an Absorption, Distribution, and Excretion Study With Intravenous Microtracer and Concomitant Oral Doses for Bioavailability Determination. Clin Pharmacol Drug Dev. 2021 Dec;10(12):1419-1431. doi: 10.1002/cpdd.1029. Epub 2021 Oct 28. [Article]
  6. Licea Perez H, Knecht D, Evans CA: Overcoming bioanalytical challenges associated with the separation and quantitation of GSK1278863, a HIF-prolyl hydroxylase inhibitor, and its 14 stereoisomeric metabolites. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Jan 15;1009-1010:7-16. doi: 10.1016/j.jchromb.2015.11.057. Epub 2015 Dec 4. [Article]
  7. GSK: GSK reports outcome from US FDA Advisory Committee meeting on daprodustat for anaemia of CKD [Link]
  8. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
  9. FDA News Release: FDA Approves First Oral Treatment for Anemia Caused by Chronic Kidney Disease for Adults on Dialysis [Link]
Human Metabolome Database
HMDB0250863
PubChem Compound
91617630
PubChem Substance
347828049
ChemSpider
33427356
RxNav
2628210
ChEMBL
CHEMBL3544988
ZINC
ZINC000231226004
PharmGKB
PA166280581
Wikipedia
Daprodustat

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAnemia / Renal Anemia / Renal Insufficiency,Chronic1
3CompletedTreatmentAllergic Bronchopulmonary Aspergillosis / Anemia1
3CompletedTreatmentAnemia7
3RecruitingTreatmentAnemia1
2CompletedBasic SciencePeripheral Vascular Disease Patient1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral4 mg/1
Tablet, film coatedOral6 mg/1
Tablet, film coatedOral8 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US11117871No2021-09-142038-03-13US flag
US8815884No2014-08-262027-06-22US flag
US8557834No2013-10-152027-06-22US flag
US8324208No2012-12-042028-12-11US flag
US11649217No2018-03-132038-03-13US flag
US11643397No2003-06-272023-06-27US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.345 mg/mLALOGPS
logP1.48ALOGPS
logP1.4Chemaxon
logS-3.1ALOGPS
pKa (Strongest Acidic)0.35Chemaxon
pKa (Strongest Basic)-9.1Chemaxon
Physiological Charge-2Chemaxon
Hydrogen Acceptor Count6Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area124.09 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity96.89 m3·mol-1Chemaxon
Polarizability40.18 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
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/MSsplash10-0006-0009000000-938053288e33b65500b4
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0009000000-e27878de2ada0ad47953
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-00y0-0049000000-e2f9e8180c74a9e05cd5
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-00dm-8129000000-247065103a710be9d1fc
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-00xu-0295000000-31746c63bbbd7ccff858
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0kmj-5149000000-70c82c5c213fcbaefdbe
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-188.21883
predicted
DeepCCS 1.0 (2019)
[M+H]+190.57683
predicted
DeepCCS 1.0 (2019)
[M+Na]+197.37788
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Peptidyl-proline dioxygenase activity
Specific Function
Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins. Hydroxylates a specific prol...
Gene Name
EGLN1
Uniprot ID
Q9GZT9
Uniprot Name
Egl nine homolog 1
Molecular Weight
46020.585 Da
References
  1. Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
  2. Zheng Q, Wang Y, Yang H, Sun L, Fu X, Wei R, Liu YN, Liu WJ: Efficacy and Safety of Daprodustat for Anemia Therapy in Chronic Kidney Disease Patients: A Systematic Review and Meta-Analysis. Front Pharmacol. 2021 Jan 12;11:573645. doi: 10.3389/fphar.2020.573645. eCollection 2020. [Article]
  3. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Peptidyl-proline 4-dioxygenase activity
Specific Function
Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins. Hydroxylates a specific prol...
Gene Name
EGLN2
Uniprot ID
Q96KS0
Uniprot Name
Egl nine homolog 2
Molecular Weight
43650.03 Da
References
  1. Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
  2. Zheng Q, Wang Y, Yang H, Sun L, Fu X, Wei R, Liu YN, Liu WJ: Efficacy and Safety of Daprodustat for Anemia Therapy in Chronic Kidney Disease Patients: A Systematic Review and Meta-Analysis. Front Pharmacol. 2021 Jan 12;11:573645. doi: 10.3389/fphar.2020.573645. eCollection 2020. [Article]
  3. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Peptidyl-proline 4-dioxygenase activity
Specific Function
Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins. Hydroxylates a specific prol...
Gene Name
EGLN3
Uniprot ID
Q9H6Z9
Uniprot Name
Egl nine homolog 3
Molecular Weight
27261.06 Da
References
  1. Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
  2. Zheng Q, Wang Y, Yang H, Sun L, Fu X, Wei R, Liu YN, Liu WJ: Efficacy and Safety of Daprodustat for Anemia Therapy in Chronic Kidney Disease Patients: A Systematic Review and Meta-Analysis. Front Pharmacol. 2021 Jan 12;11:573645. doi: 10.3389/fphar.2020.573645. eCollection 2020. [Article]
  3. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
Curator comments
Daprodustat is primarily metabolized by CYP2C8. In in vitro studies using human liver microsomes, daprodustat inhibited CYP2C8 with an IC50 value of 21 μmol/L; however, daprodustat is unlikely to affect the metabolism of drugs metabolized by CYP2C8.
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
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Caltabiano S, Mahar KM, Lister K, Tenero D, Ravindranath R, Cizman B, Cobitz AR: The drug interaction potential of daprodustat when coadministered with pioglitazone, rosuvastatin, or trimethoprim in healthy subjects. Pharmacol Res Perspect. 2018 Mar 9;6(2):e00327. doi: 10.1002/prp2.327. eCollection 2018 Apr. [Article]
  2. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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: JESDUVROQ (daprodustat) tablets, for oral use [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
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: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
Some oxidative metabolites of daprodustat are substrates of Organic Anion Transporter (OAT)1.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Curator comments
Some oxidative metabolites of daprodustat are substrates of Organic Anion Transporter (OAT)3.
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: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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: JESDUVROQ (daprodustat) tablets, for oral use [Link]

Drug created at October 20, 2016 20:39 / Updated at February 08, 2023 21:47