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
Structure for Daprodustat (DB11682)
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in treatment of Anemia •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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
Target Actions Organism AEgl nine homolog 1 inhibitorHumans AEgl nine homolog 2 inhibitorHumans AEgl nine homolog 3 inhibitorHumans - 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
Hover over products below to view reaction partners
- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The metabolism of Daprodustat can be increased when combined with Abatacept. Abiraterone The metabolism of Daprodustat can be decreased when combined with Abiraterone. Adalimumab The metabolism of Daprodustat can be increased when combined with Adalimumab. Almotriptan The metabolism of Daprodustat can be decreased when combined with Almotriptan. Alpelisib The 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Duvroq (GlaxoSmithKline)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Jesduvroq Tablet, film coated 6 mg/1 Oral GlaxoSmithKline LLC 2023-02-01 Not applicable US 
Jesduvroq Tablet, film coated 1 mg/1 Oral GlaxoSmithKline LLC 2023-02-01 Not applicable US Jesduvroq Tablet, film coated 4 mg/1 Oral GlaxoSmithKline LLC 2023-02-01 Not applicable US Jesduvroq Tablet, film coated 8 mg/1 Oral GlaxoSmithKline LLC 2023-02-01 Not applicable US Jesduvroq Tablet, film coated 2 mg/1 Oral GlaxoSmithKline LLC 2023-02-01 Not applicable US
Categories
- ATC Codes
- B03XA07 — Daprodustat
- Drug Categories
- Amino Acids
- Amino Acids, Peptides, and Proteins
- Antianemic Preparations
- BCRP/ABCG2 Substrates
- Blood and Blood Forming Organs
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Hypoxia-Inducible Factor-Proline Dioxygenases, antagonists & inhibitors
- OAT1/SLC22A6 Substrates
- OAT3/SLC22A8 Substrates
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- Pyrimidines
- Pyrimidinones
- 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
- Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
- 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]
- 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]
- 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]
- 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]
- 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]
- GSK: GSK reports outcome from US FDA Advisory Committee meeting on daprodustat for anaemia of CKD [Link]
- FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
- FDA News Release: FDA Approves First Oral Treatment for Anemia Caused by Chronic Kidney Disease for Adults on Dialysis [Link]
- External Links
- Human Metabolome Database
- HMDB0250863
- PubChem Compound
- 91617630
- PubChem Substance
- 347828049
- ChemSpider
- 33427356
- 2628210
- ChEMBL
- CHEMBL3544988
- ZINC
- ZINC000231226004
- PharmGKB
- PA166280581
- Wikipedia
- Daprodustat
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Anemia / Renal Anemia / Renal Insufficiency,Chronic 1 3 Completed Treatment Allergic Bronchopulmonary Aspergillosis / Anemia 1 3 Completed Treatment Anemia 7 3 Recruiting Treatment Anemia 1 2 Completed Basic Science Peripheral Vascular Disease Patient 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 1 mg/1 Tablet, film coated Oral 2 mg/1 Tablet, film coated Oral 4 mg/1 Tablet, film coated Oral 6 mg/1 Tablet, film coated Oral 8 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US11117871 No 2021-09-14 2038-03-13 US US8815884 No 2014-08-26 2027-06-22 US US8557834 No 2013-10-15 2027-06-22 US US8324208 No 2012-12-04 2028-12-11 US US11649217 No 2018-03-13 2038-03-13 US US11643397 No 2003-06-27 2023-06-27 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.345 mg/mL ALOGPS logP 1.48 ALOGPS logP 1.4 Chemaxon logS -3.1 ALOGPS pKa (Strongest Acidic) 0.35 Chemaxon pKa (Strongest Basic) -9.1 Chemaxon Physiological Charge -2 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 124.09 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 96.89 m3·mol-1 Chemaxon Polarizability 40.18 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0006-0009000000-938053288e33b65500b4 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0006-0009000000-e27878de2ada0ad47953 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-00y0-0049000000-e2f9e8180c74a9e05cd5 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-00dm-8129000000-247065103a710be9d1fc Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-00xu-0295000000-31746c63bbbd7ccff858 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0kmj-5149000000-70c82c5c213fcbaefdbe Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 188.21883 predictedDeepCCS 1.0 (2019) [M+H]+ 190.57683 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.37788 predictedDeepCCS 1.0 (2019)
Targets
- 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
- Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
- 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]
- 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
- Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
- 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]
- 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
- Dhillon S: Daprodustat: First Approval. Drugs. 2020 Sep;80(14):1491-1497. doi: 10.1007/s40265-020-01384-y. [Article]
- 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]
- FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- 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]
- 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
- 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
- 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
- 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
- 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
- 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
- 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