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
- 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
Pharmacology
- Indication
Vadadustat is indicated for the treatment of symptomatic anemia associated with chronic kidney disease (CKD) in adults on chronic maintenance 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 Treatment of Symptomatic 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
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.
Target Actions Organism AEgl nine homolog 1 inhibitorHumans AEgl nine homolog 2 inhibitorHumans AEgl nine homolog 3 inhibitorHumans UHypoxia-inducible factor 1-alpha stabilizationHumans UEndothelial PAS domain-containing protein 1 stabilizationHumans - 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
- 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
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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The serum concentration of 1,2-Benzodiazepine can be increased when it is combined with Vadadustat. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Vadadustat. Abiraterone The serum concentration of Abiraterone can be increased when it is combined with Vadadustat. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Vadadustat. Acalabrutinib The 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
- 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
- Vafseo (Akebia Therapeutics)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Vafseo Tablet, film coated 450 mg Oral Akebia Europe Limited 2023-06-09 Not applicable EU Vafseo Tablet, film coated 150 mg Oral Akebia Europe Limited 2023-06-09 Not applicable EU Vafseo Tablet, film coated 300 mg Oral Akebia Europe Limited 2023-06-09 Not applicable EU Vafseo Tablet, film coated 150 mg Oral Akebia Europe Limited 2023-06-09 Not applicable EU Vafseo Tablet, film coated 450 mg Oral Akebia Europe Limited 2023-06-09 Not applicable EU
Categories
- ATC Codes
- B03XA08 — Vadadustat
- Drug Categories
- Amino Acids
- Amino Acids, Peptides, and Proteins
- Antianemic Preparations
- BCRP/ABCG2 Inhibitors
- Blood and Blood Forming Organs
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (weak)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Erythropoiesis-Stimulating Agents
- Hypoxia-Inducible Factor-Proline Dioxygenases, antagonists & inhibitors
- OAT3/SLC22A8 Inhibitors
- OAT3/SLC22A8 Substrates
- Pyridines
- UGT1A1 Inducers
- UGT1A1 Substrates
- UGT1A9 Substrates
- UGT2B7 substrates
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- BioPharma Dive: 5 FDA approval decisions to watch in the first quarter (2022) [Link]
- 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]
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- 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]
- EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- External Links
- 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);">
Phase Status Purpose Conditions Count 3 Completed Other Healthy Subjects (HS) 1 3 Completed Treatment Anemia 1 3 Completed Treatment Anemia Associated With Chronic Kidney Disease (CKD) 1 3 Completed Treatment Anemia; Non-dialysis Dependent Chronic Kidney Disease 1 3 Completed Treatment Anemia; Peritoneal Dialysis Dependent Chronic Kidney Disease 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 150 mg Tablet, film coated Oral 300 mg Tablet, film coated Oral 450 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 0.041 mg/ml EMA Assessment Report - Predicted Properties
Property Value Source Water Solubility 0.0436 mg/mL ALOGPS logP 2.53 ALOGPS logP 2.2 Chemaxon logS -3.8 ALOGPS pKa (Strongest Acidic) 3.12 Chemaxon pKa (Strongest Basic) 1.15 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 99.52 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 75.51 m3·mol-1 Chemaxon Polarizability 29.63 Å3 Chemaxon Number of Rings 2 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 GC-MS Spectrum - GC-MS Predicted GC-MS splash10-001i-1090000000-9f4910edaee2dfdf5001 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-053r-0094000000-9c949bb7487015af18ef Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-1090000000-8349e4af5f5b1996e797 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0f89-2090000000-9f579bf31d19cff684f1 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0535-1490000000-a0a72af2c0ce41066f5b Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-9040000000-d53f8ee03acfaad6d189 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-9410000000-4d26f266695f6a4764ce 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]- 161.76668 predictedDeepCCS 1.0 (2019) [M+H]+ 164.12468 predictedDeepCCS 1.0 (2019) [M+Na]+ 170.22792 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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
- 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
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- 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
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- 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
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- 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
- 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
- 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
- Pharmaceuticals and Medical Devices Agency: Report on the Deliberation Results for Vadadustat [Link]
- 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
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- 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
Carriers
- 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
- EMA Assessment Report: Vafseo (vadadustat) film-coated tablets for oral use [Link]
Transporters
- 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
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- EMA Summary of Product Characteristics: Vafseo (vadadustat) film-coated tablets for oral use [Link]
- 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
- 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