NAV

Vadadustat

Identification

Summary

Vadadustat is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor used to treat symptomatic anemia associated with chronic kidney disease in adults on chronic maintenance dialysis.

Brand Names
Vafseo
Generic Name
Vadadustat
DrugBank Accession Number
DB12255
Background

One of the most common symptoms of advanced renal disease is anemia, caused primarily by the inability of the kidney to respond to anemic conditions with a corresponding increase in erythropoietin (EPO) production.4 The treatment of anemia associated with chronic kidney disease (CKD) has traditionally involved the administration of exogenous erythropoiesis-stimulating agents (ESAs), such as darbepoetin alfa, to counter the decrease in endogenous EPO production. While efficacious, the overuse of ESAs has been associated with cardiovascular complications, progression of CKD, and increases in overall mortality.4

A relatively new and alternative treatment option for patients with anemia associated with CKD is the use of small molecule inhibitors of hypoxia-inducible factor prolyl-hydroxylase (HIF-PH). These agents inhibit prolyl-hydroxylase domain oxygen sensors, mimicking hypoxic conditions and activating hypoxia-inducible factors. These transcription factors serve a multitude of roles, including the stimulation of erythropoiesis.4

Vadadustat is an orally administered inhibitor of HIF-PH with a safety and efficacy profile non-inferior to darbepoetin alfa for the treatment of anemia in patients with CKD undergoing dialysis.1,3 It was first approved in Japan, and in April 2023, it was approved by the EMA for the treatment of symptomatic anemia associated with CKD in adults on chronic maintenance dialysis.7,8,9 Vadadustat is currently awaiting a regulatory decision by the FDA.6 Vadadustat did not meet the prespecified noninferiority criterion for cardiovascular safety in patients with non-dialysis-dependent CKD.2

Type
Small Molecule
Groups
Approved, Investigational
Structure
3D
Similar Structures
Weight
Average: 306.7
Monoisotopic: 306.0407345
Chemical Formula
C14H11ClN2O4
Synonyms
  • Glycine, N-((5-(3-chlorophenyl)-3-hydroxy-2-pyridinyl)carbonyl)-
  • N-(5-(3-Chlorophenyl)-3-hydroxypyridine-2-carbonyl)glycine
  • Vadadustat
External IDs
  • AKB 6548
  • AKB-6548
  • B-506
  • B506
  • PG-1016548
  • PG1016548
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Pharmacology

Indication

Vadadustat is indicated for the treatment of symptomatic anemia associated with chronic kidney disease (CKD) in adults on chronic maintenance dialysis.8

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofSymptomatic anemia•••••••••••••••••••••••• ••••••••••• ••••••••••••••• •••• ••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

The use of vadadustat was compared to darbepoetin alfa for the treatment of anemia in adult patients with dialysis-dependent chronic kidney disease. Vadadustat was non-inferior to darbepoetin alfa and met the primary hemoglobin level endpoint. In healthy subjects given 600 mg to 1200 mg of vadadustat, the use of this drug was not associated with clinically significant QTc prolongation. Compared to darbepoetin alfa, patients with dialysis-dependent chronic kidney disease treated with vadadustat have similar risks for death, myocardial infarction and stroke. The use of vadadustat may also lead to the development of thromboembolic events, hepatic impairment, hepatotoxicity, convulsions, as well as an increase in blood pressure.8

Mechanism of action

Hypoxia-inducible factors (HIFs) are transcription factors responsible for cellular survival under hypoxic conditions. They regulate a number of processes including angiogenesis, cell growth and differentiation, various metabolic processes, and erythropoiesis.4 Under normoxic conditions, HIFs are degraded via hydroxylation by prolyl-hydroxylase dioxygenases.

Vadadustat is an inhibitor of HIF-prolyl-hydroxylases (HIF-PHI), that facilitates increased HIF activity in the absence of hypoxic conditions.4,5 The increased levels of HIF prompted by vadadustat stimulate endogenous erythropoietin production, increasing iron mobilization and contributing to the gradual rise of hemoglobin levels and the correction of iron metabolism.8 In patients with anemia of chronic kidney disease, in whom normal erythropoiesis is dysfunctional, this leads to the correction of anemia.

TargetActionsOrganism
AEgl nine homolog 1
inhibitor
Humans
AEgl nine homolog 2
inhibitor
Humans
AEgl nine homolog 3
inhibitor
Humans
UHypoxia-inducible factor 1-alpha
stabilization
Humans
UEndothelial PAS domain-containing protein 1
stabilization
Humans
Absorption

Following single and repeated doses, vadadustat is rapidly absorbed. The Tmax of vadadustat ranges between 2 and 3 hr. No significant accumulation was detected in healthy subjects given repeated doses of vadadustat. Compared to fasted conditions, the administration of a 450 mg vadadustat tablet with a standard high-fat meal decreased the Cmax and AUC by 27% and 6%, respectively. Vadadustat may be taken with or without food. The mean blood-to-plasma ratio of vadadustat went from 0.50 to 0.55, suggesting that the sequestration of vadadustat into red blood cells is minimal.8

Volume of distribution

The apparent volume of distribution of vadadustat in patients with chronic kidney disease is 11.6 L.8

Protein binding

The protein binding of vadadustat is greater than or equal to 99.5% in human plasma.8

Metabolism

Vadadustat is mainly metabolized by UDP-glucuronosyltransferase (UGT) enzymes, forming O-glucuronide conjugates via direct glucuronidation. The metabolism of vadadustat via cytochrome P450s (CYPs) is minimal. The major metabolite of vadadustat is vadadustat-O-glucuronide, which has 15% of the AUC of plasma radioactivity, and it is catalyzed by multiple UGT enzymes, including UGT1A1, UGT1A7, UGT1A8 and UGT1A9. Vadadustat acyl glucuronide is a minor metabolite with 0.047% of the total radioactivity in plasma. None of the vadadustat metabolites are active.8

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Route of elimination

In healthy subjects given a single dose of 650 mg of radiolabelled vadadustat, 85.9% of the dose was recovered, with 58.9% appearing in urine and 26.9% in feces. Small amounts of the unchanged form of vadadustat are excreted in urine and feces (<1% and 9%, respectively).8

Half-life

In patients with dialysis-dependent chronic kidney disease, the half-life of vadadustat was 9.2 hours.8

Clearance

In healthy subjects given a single dose of 300 mg of vadadustat, the apparent total body clearance ranged from 1.7 L/h to 1.9 L/h.5 In patients with chronic kidney disease, the clearance of vadadustat is 0.8 L/h.10

Adverse Effects
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Toxicity

An overdose of vadadustat may lead to extensions of the pharmacologic effects, such as increased hemoglobin levels and secondary polycythemia. In case of overdose, patients should be managed with clinically appropriate measures, such as dose reduction or treatment discontinuation. Patients should be carefully monitored and treated as clinically indicated. Approximately 16% of the vadadustat dose is removed by dialysis.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.
DrugInteraction
Integrate drug-drug
interactions in your software
1,2-BenzodiazepineThe serum concentration of 1,2-Benzodiazepine can be increased when it is combined with Vadadustat.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Vadadustat.
AbirateroneThe serum concentration of Abiraterone can be increased when it is combined with Vadadustat.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Vadadustat.
AcalabrutinibThe serum concentration of Acalabrutinib can be increased when it is combined with Vadadustat.
Food Interactions
  • Take with or without food. The administration of a standard high-fat meal decreases the AUC of vadadustat by 6%, relative to fasted conditions; however, it may be administered with or without food.

Products

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International/Other Brands
Vafseo (Akebia Therapeutics)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
VafseoTablet, film coated450 mgOralAkebia Europe Limited2023-06-09Not applicableEU flag
VafseoTablet, film coated150 mgOralAkebia Europe Limited2023-06-09Not applicableEU flag
VafseoTablet, film coated300 mgOralAkebia Europe Limited2023-06-09Not applicableEU flag
VafseoTablet, film coated150 mgOralAkebia Europe Limited2023-06-09Not applicableEU flag
VafseoTablet, film coated450 mgOralAkebia Europe Limited2023-06-09Not applicableEU flag

Categories

ATC Codes
B03XA08 — Vadadustat
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
Phenylpyridines / Pyridinecarboxylic acids and derivatives / 2-heteroaryl carboxamides / Chlorobenzenes / Hydroxypyridines / Aryl chlorides / Vinylogous acids / Heteroaromatic compounds / Secondary carboxylic acid amides / Azacyclic compounds
show 7 more
Substituents
2-heteroaryl carboxamide / 3-phenylpyridine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Carbonyl group / Carboxamide group / Carboxylic acid
show 20 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
I60W9520VV
CAS number
1000025-07-9
InChI Key
JGRXMPYUTJLTKT-UHFFFAOYSA-N
InChI
InChI=1S/C14H11ClN2O4/c15-10-3-1-2-8(4-10)9-5-11(18)13(16-6-9)14(21)17-7-12(19)20/h1-6,18H,7H2,(H,17,21)(H,19,20)
IUPAC Name
2-{[5-(3-chlorophenyl)-3-hydroxypyridin-2-yl]formamido}acetic acid
SMILES
OC(=O)CNC(=O)C1=C(O)C=C(C=N1)C1=CC(Cl)=CC=C1

References

Synthesis Reference

Shengde, W., et al. (2012). Prolyl hydroxylase inhibitors and methods of use (U.S. Patent No. US 8,323,671 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/3d/62/ce/4a3024a944d334/US8323671.pdf

General References
  1. Eckardt KU, Agarwal R, Aswad A, Awad A, Block GA, Bacci MR, Farag YMK, Fishbane S, Hubert H, Jardine A, Khawaja Z, Koury MJ, Maroni BJ, Matsushita K, McCullough PA, Lewis EF, Luo W, Parfrey PS, Pergola P, Sarnak MJ, Spinowitz B, Tumlin J, Vargo DL, Walters KA, Winkelmayer WC, Wittes J, Zwiech R, Chertow GM: Safety and Efficacy of Vadadustat for Anemia in Patients Undergoing Dialysis. N Engl J Med. 2021 Apr 29;384(17):1601-1612. doi: 10.1056/NEJMoa2025956. [Article]
  2. Chertow GM, Pergola PE, Farag YMK, Agarwal R, Arnold S, Bako G, Block GA, Burke S, Castillo FP, Jardine AG, Khawaja Z, Koury MJ, Lewis EF, Lin T, Luo W, Maroni BJ, Matsushita K, McCullough PA, Parfrey PS, Roy-Chaudhury P, Sarnak MJ, Sharma A, Spinowitz B, Tseng C, Tumlin J, Vargo DL, Walters KA, Winkelmayer WC, Wittes J, Eckardt KU: Vadadustat in Patients with Anemia and Non-Dialysis-Dependent CKD. N Engl J Med. 2021 Apr 29;384(17):1589-1600. doi: 10.1056/NEJMoa2035938. [Article]
  3. Nangaku M, Kondo K, Ueta K, Kokado Y, Kaneko G, Matsuda H, Kawaguchi Y, Komatsu Y: Efficacy and safety of vadadustat compared with darbepoetin alfa in Japanese anemic patients on hemodialysis: a Phase 3, multicenter, randomized, double-blind study. Nephrol Dial Transplant. 2021 Aug 27;36(9):1731-1741. doi: 10.1093/ndt/gfab055. [Article]
  4. Sanghani NS, Haase VH: Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Adv Chronic Kidney Dis. 2019 Jul;26(4):253-266. doi: 10.1053/j.ackd.2019.04.004. [Article]
  5. Paulson SK, Martinez J, Sawant R, Burke SK, Chavan A: Effect of Phosphate Binders and a Dietary Iron Supplement on the Pharmacokinetics of a Single Dose of Vadadustat in Healthy Adults. Clin Pharmacol Drug Dev. 2022 Apr;11(4):475-485. doi: 10.1002/cpdd.1033. Epub 2022 Feb 16. [Article]
  6. BioPharma Dive: 5 FDA approval decisions to watch in the first quarter (2022) [Link]
  7. Akebia Therapeutics Press Release: Akebia Therapeutics Announces Top-Line Results from its PRO2TECT Global Phase 3 Program of Vadadustat for Treatment of Anemia Due to Chronic Kidney Disease in Adult Patients Not on Dialysis [Link]
  8. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
  9. PR NewsWire: Akebia Receives European Commission Approval for Vafseo (vadadustat) for the Treatment of Symptomatic Anaemia Associated with Chronic Kidney Disease in Adults on Chronic Maintenance Dialysis [Link]
  10. EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]
PubChem Compound
23634441
PubChem Substance
347828530
ChemSpider
34958379
BindingDB
107704
ChEMBL
CHEMBL3646221
ZINC
ZINC000117532869
PDBe Ligand
A1Z
Wikipedia
Vadadustat
PDB Entries
5opc / 5ox6 / 7ump

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
3CompletedOtherHealthy Subjects (HS)1
3CompletedTreatmentAnemia1
3CompletedTreatmentAnemia Associated With Chronic Kidney Disease (CKD)1
3CompletedTreatmentAnemia; Non-dialysis Dependent Chronic Kidney Disease1
3CompletedTreatmentAnemia; Peritoneal Dialysis Dependent Chronic Kidney Disease1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral150 mg
Tablet, film coatedOral300 mg
Tablet, film coatedOral450 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.041 mg/mlEMA Assessment Report
Predicted Properties
PropertyValueSource
Water Solubility0.0436 mg/mLALOGPS
logP2.53ALOGPS
logP2.2Chemaxon
logS-3.8ALOGPS
pKa (Strongest Acidic)3.12Chemaxon
pKa (Strongest Basic)1.15Chemaxon
Physiological Charge-1Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area99.52 Å2Chemaxon
Rotatable Bond Count4Chemaxon
Refractivity75.51 m3·mol-1Chemaxon
Polarizability29.63 Å3Chemaxon
Number of Rings2Chemaxon
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 GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-001i-1090000000-9f4910edaee2dfdf5001
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-053r-0094000000-9c949bb7487015af18ef
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-1090000000-8349e4af5f5b1996e797
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0f89-2090000000-9f579bf31d19cff684f1
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0535-1490000000-a0a72af2c0ce41066f5b
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-9040000000-d53f8ee03acfaad6d189
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-9410000000-4d26f266695f6a4764ce
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]-161.76668
predicted
DeepCCS 1.0 (2019)
[M+H]+164.12468
predicted
DeepCCS 1.0 (2019)
[M+Na]+170.22792
predicted
DeepCCS 1.0 (2019)

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Details1. Egl nine homolog 1
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. Sanghani NS, Haase VH: Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Adv Chronic Kidney Dis. 2019 Jul;26(4):253-266. doi: 10.1053/j.ackd.2019.04.004. [Article]
Details2. Egl nine homolog 2
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. Sanghani NS, Haase VH: Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Adv Chronic Kidney Dis. 2019 Jul;26(4):253-266. doi: 10.1053/j.ackd.2019.04.004. [Article]
Details3. Egl nine homolog 3
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. Sanghani NS, Haase VH: Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Adv Chronic Kidney Dis. 2019 Jul;26(4):253-266. doi: 10.1053/j.ackd.2019.04.004. [Article]
Details4. Hypoxia-inducible factor 1-alpha
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Stabilization
General Function
Ubiquitin protein ligase binding
Specific Function
Functions as a master transcriptional regulator of the adaptive response to hypoxia. Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transp...
Gene Name
HIF1A
Uniprot ID
Q16665
Uniprot Name
Hypoxia-inducible factor 1-alpha
Molecular Weight
92669.595 Da
References
  1. Sanghani NS, Haase VH: Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Adv Chronic Kidney Dis. 2019 Jul;26(4):253-266. doi: 10.1053/j.ackd.2019.04.004. [Article]
Details5. Endothelial PAS domain-containing protein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Stabilization
General Function
Transcription factor involved in the induction of oxygen regulated genes. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation requires recruitment of transcriptional coactivators such as CREBBP and probably EP300. Interaction with redox regulatory protein APEX seems to activate CTAD (By similarity).
Specific Function
Dna binding
Gene Name
EPAS1
Uniprot ID
Q99814
Uniprot Name
Endothelial PAS domain-containing protein 1
Molecular Weight
96458.235 Da
References
  1. Sanghani NS, Haase VH: Hypoxia-Inducible Factor Activators in Renal Anemia: Current Clinical Experience. Adv Chronic Kidney Dis. 2019 Jul;26(4):253-266. doi: 10.1053/j.ackd.2019.04.004. [Article]

Enzymes

Details1. UDP-glucuronosyltransferase 1-1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
  2. EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details2. UDP-glucuronosyltransferase 1-7
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A7
Uniprot ID
Q9HAW7
Uniprot Name
UDP-glucuronosyltransferase 1-7
Molecular Weight
59818.315 Da
References
  1. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details3. UDP-glucuronosyltransferase 1-8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A8
Uniprot ID
Q9HAW9
Uniprot Name
UDP-glucuronosyltransferase 1-8
Molecular Weight
59741.035 Da
References
  1. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details4. UDP-glucuronosyltransferase 1-9
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details5. UDP-glucuronosyltransferase 2B7
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. Pharmaceuticals and Medical Devices Agency: Report on the Deliberation Results for Vadadustat [Link]
  2. EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details6. Cytochrome P450 2B6
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. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
  2. EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details7. Cytochrome P450 2C8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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. Pharmaceuticals and Medical Devices Agency: Report on the Deliberation Results for Vadadustat [Link]
Details8. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Downregulator
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. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details9. Cytochrome P450 2C9
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
  2. Pharmaceuticals and Medical Devices Agency: Report on the Deliberation Results for Vadadustat [Link]

Carriers

Details1. Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]

Transporters

Details1. ATP-binding cassette sub-family G member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
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. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details2. Solute carrier family 22 member 8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Details3. Solute carrier family 22 member 6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]

Drug created at October 20, 2016 21:44 / Updated at June 27, 2023 01:10