Identification
- Summary
Axitinib is an oral VEGFR and kinase inhibitor used for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy.
- Brand Names
- Inlyta
- Generic Name
- Axitinib
- DrugBank Accession Number
- DB06626
- Background
Axitinib is a second generation tyrosine kinase inhibitor that works by selectively inhibiting vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3).7 Through this mechanism of action, axitinib blocks angiogenesis, tumour growth and metastases. It is reported to exhibit potency that is 50-450 times higher than that of the first generation VEGFR inhibitors.7 Axitinib is an indazole derivative.6 It is most commonly marketed under the name Inlyta® and is available in oral formulations.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Axitinib (DB06626)
- Weight
- Average: 386.47
Monoisotopic: 386.120131908 - Chemical Formula
- C22H18N4OS
- Synonyms
- Axitinib
- Axitinibum
- N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
- External IDs
- AG-013736
- AG-13736
- AG013736
Pharmacology
- Indication
Used in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer.
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 Used in combination to treat Advanced renal cell carcinoma (arcc) Regimen in combination with: Pembrolizumab (DB09037) •••••••••••• ••••••••• ••••• •••••• Used in combination to treat Advanced renal cell carcinoma (arcc) Regimen in combination with: Avelumab (DB11945) •••••••••••• ••••••••• ••••• •••••• Treatment of Advanced renal cell carcinoma (arcc) •••••••••••• ••••••• •• •• ••••• ••• ••••• •••••••• ••••••• •••••• Treatment of Advanced thyroid cancer ••• ••••• - Associated Therapies
- 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
Axitinib prevents the progression of cancer by inhibiting angiogenesis and blocking tumor growth.
- Mechanism of action
Axitinib selectively blocks the tyrosine kinase receptors VEGFR-1 (vascular endothelial growth factor receptor), VEGFR-2, and VEGFR-3.
Target Actions Organism AVascular endothelial growth factor receptor 1 inhibitorHumans AVascular endothelial growth factor receptor 2 inhibitorHumans AVascular endothelial growth factor receptor 3 inhibitorHumans - Absorption
After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.
- Volume of distribution
The volume of distribution is 160 L.
- Protein binding
Plasma protein binding for axitinib is high at over 99% with most protein binding to albumin followed by α1-acid glycoprotein.
- Metabolism
Axitinib undergoes mainly hepatic metabolism. CYP3A4 and CYP3A5 are the main hepatic enzymes while CYP1A2, CYP2C19, and UGT1A1 enzymes are secondary.
- Route of elimination
Axitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.
- Half-life
Axitinib has a half life of 2.5 to 6.1 hours.
- Clearance
The average clearance of axitinib is 38 L/h.
- 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
Some of the more serious toxic effects seen in patients taking axitinib include, but are not limited to, hypertension, thrombotic events, hemorrhage, and GI perforation.
- 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 softwareAbametapir The serum concentration of Axitinib can be increased when it is combined with Abametapir. Abatacept The metabolism of Axitinib can be increased when combined with Abatacept. Abiraterone The serum concentration of Axitinib can be increased when it is combined with Abiraterone. Abrocitinib The serum concentration of Axitinib can be increased when it is combined with Abrocitinib. Acalabrutinib The metabolism of Axitinib can be decreased when combined with Acalabrutinib. - Food Interactions
- Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of axitinib.
- Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of axitinib.
- Take with a full glass of water.
- Take 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Inlyta Tablet, film coated 3 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU 
Inlyta Tablet 5 mg Oral Pfizer Canada Ulc 2012-08-17 Not applicable Canada 
Inlyta Tablet, film coated 5 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU Inlyta Tablet, film coated 1 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 2012-01-27 Not applicable US 
Inlyta Tablet, film coated 7 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU
Categories
- ATC Codes
- L01EK01 — Axitinib
- Drug Categories
- Acids, Carbocyclic
- Amides
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Benzamides and benzamide derivatives
- Benzene Derivatives
- Benzoates
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C19 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A5 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- Indazoles
- Kinase Inhibitor
- Narrow Therapeutic Index Drugs
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B1/SLCO1B1 Substrates
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Protein Kinase Inhibitors
- Pyrazoles
- Receptor Tyrosine Kinase Inhibitors
- Tyrosine Kinase Inhibitors
- UGT1A1 Substrates
- UGT1A1 Substrates with a Narrow Therapeutic Index
- Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diarylthioethers. These are organosulfur compounds containing a thioether group that is substituted by two aryl groups.
- Kingdom
- Organic compounds
- Super Class
- Organosulfur compounds
- Class
- Thioethers
- Sub Class
- Aryl thioethers
- Direct Parent
- Diarylthioethers
- Alternative Parents
- O-sulfanylbenzoic acids and derivatives / Benzamides / Indazoles / Thiophenol ethers / Benzoyl derivatives / Vinylogous thioesters / Pyridines and derivatives / Pyrazoles / Heteroaromatic compounds / Secondary carboxylic acid amides show 7 more
- Substituents
- Aromatic heteropolycyclic compound / Azacycle / Azole / Benzamide / Benzenoid / Benzoic acid or derivatives / Benzopyrazole / Benzoyl / Carboxamide group / Carboxylic acid derivative show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- aryl sulfide, benzamides, pyridines, indazoles (CHEBI:66910)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- C9LVQ0YUXG
- CAS number
- 319460-85-0
- InChI Key
- RITAVMQDGBJQJZ-FMIVXFBMSA-N
- InChI
- InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+
- IUPAC Name
- N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide
- SMILES
- CNC(=O)C1=C(SC2=CC=C3C(NN=C3\C=C\C3=CC=CC=N3)=C2)C=CC=C1
References
- Synthesis Reference
Hu-Lowe D, Hallin M, Feeley R, Zou H, Rewolinski D, Wickman G, Chen E, Kim Y, Riney S, Reed J, Heller D, Simmons B, Kania R, McTigue M, Niesman M, Gregory S, Shalinsky D, Bender S. Characterization of potency and activity of the VEGF/PDGF receptor tyrosine kinase inhibitor AG013736. Proc Am Assoc Cancer Res. 2002;43:A5357.
- General References
- Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [Article]
- Inai T, Mancuso M, Hashizume H, Baffert F, Haskell A, Baluk P, Hu-Lowe DD, Shalinsky DR, Thurston G, Yancopoulos GD, McDonald DM: Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts. Am J Pathol. 2004 Jul;165(1):35-52. [Article]
- Rugo HS, Herbst RS, Liu G, Park JW, Kies MS, Steinfeldt HM, Pithavala YK, Reich SD, Freddo JL, Wilding G: Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol. 2005 Aug 20;23(24):5474-83. Epub 2005 Jul 18. [Article]
- Rini BI: SU11248 and AG013736: current data and future trials in renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):175-80. [Article]
- Gilbert JA, Adhikari LJ, Lloyd RV, Halfdanarson TR, Muders MH, Ames MM: Molecular markers for novel therapeutic strategies in pancreatic endocrine tumors. Pancreas. 2013 Apr;42(3):411-21. doi: 10.1097/MPA.0b013e31826cb243. [Article]
- Gross-Goupil M, Francois L, Quivy A, Ravaud A: Axitinib: a review of its safety and efficacy in the treatment of adults with advanced renal cell carcinoma. Clin Med Insights Oncol. 2013 Oct 29;7:269-77. doi: 10.4137/CMO.S10594. [Article]
- DRUG NAME: Axitinib - BC Cancer [Link]
- External Links
- KEGG Drug
- D03218
- PubChem Compound
- 6450551
- PubChem Substance
- 347827779
- ChemSpider
- 4953153
- BindingDB
- 25117
- 1242999
- ChEBI
- 66910
- ChEMBL
- CHEMBL1289926
- ZINC
- ZINC000003816287
- PharmGKB
- PA164924493
- PDBe Ligand
- AXI
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Axitinib
- PDB Entries
- 4ag8 / 4agc / 4twp / 4wa9
- FDA label
- Download (307 KB)
- MSDS
- Download (36.8 KB)
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 Active Not Recruiting Treatment Primary Disease: Unresectable or Metastatic Renal Cell Carcinoma Focus of the Study:PFS Assessed by IRC Per RECIST 1.1 1 3 Active Not Recruiting Treatment Renal Cell Carcinoma (RCC) 2 3 Completed Treatment Pancreatic Ductal Adenocarcinoma (PDAC) 1 3 Completed Treatment Renal Neoplasms 2 3 Recruiting Treatment Advanced Malignant Neoplasm / Non-Small Cell Lung Cancer (NSCLC) / Ovarian Cancer / Solid Tumors / Urothelial Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 1.000 mg Tablet, film coated Oral 1 mg Tablet, film coated Oral 3 mg Tablet, film coated Oral 5 mg Tablet, film coated Oral 7 mg Tablet Oral 1.00 mg Tablet Oral 1 mg Tablet Oral 3 mg Tablet Oral 5 mg Tablet Oral 5.000 mg Tablet Oral 7 mg Tablet, film coated Oral Tablet, film coated Oral 1 mg/1 Tablet, film coated Oral 5 mg/1 Tablet, coated Oral 1 mg Tablet, coated Oral 5 mg Tablet, film coated Oral 1.000 mg Tablet, film coated Oral 5.000 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6534524 No 2003-03-18 2020-06-30 US US7141581 No 2006-11-28 2020-06-30 US US8791140 No 2014-07-29 2030-08-05 US US10570202 No 2020-02-25 2035-02-03 US US10869924 No 2020-12-22 2036-11-05 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility In aqueous media with a pH between 1.1 to 7.8, axitinib has a solubility of over 0.2 μg/mL. From FDA label. pKa 4.8 From FDA label. - Predicted Properties
Property Value Source Water Solubility 0.000551 mg/mL ALOGPS logP 4.17 ALOGPS logP 4.15 Chemaxon logS -5.8 ALOGPS pKa (Strongest Acidic) 13.07 Chemaxon pKa (Strongest Basic) 4.59 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 70.67 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 115.14 m3·mol-1 Chemaxon Polarizability 42.58 Å3 Chemaxon Number of Rings 4 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
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 221.6922979 predictedDarkChem Lite v0.1.0 [M-H]- 188.54451 predictedDeepCCS 1.0 (2019) [M+H]+ 222.4074979 predictedDarkChem Lite v0.1.0 [M+H]+ 190.94005 predictedDeepCCS 1.0 (2019) [M+Na]+ 221.5336979 predictedDarkChem Lite v0.1.0 [M+Na]+ 196.9267 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Vegf-b-activated receptor activity
- Specific Function
- Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell ...
- Gene Name
- FLT1
- Uniprot ID
- P17948
- Uniprot Name
- Vascular endothelial growth factor receptor 1
- Molecular Weight
- 150767.185 Da
References
- Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Vascular endothelial growth factor-activated receptor activity
- Specific Function
- Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...
- Gene Name
- KDR
- Uniprot ID
- P35968
- Uniprot Name
- Vascular endothelial growth factor receptor 2
- Molecular Weight
- 151525.555 Da
References
- Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Vascular endothelial growth factor-activated receptor activity
- Specific Function
- Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFC and VEGFD, and plays an essential role in adult lymphangiogenesis and in the development of the vascular network and the cardi...
- Gene Name
- FLT4
- Uniprot ID
- P35916
- Uniprot Name
- Vascular endothelial growth factor receptor 3
- Molecular Weight
- 152755.94 Da
References
- Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [Article]
Enzymes
- 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
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [Article]
- INLYTA® (axitinib) FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxygen binding
- 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
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [Article]
- INLYTA® (axitinib) FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- 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
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [Article]
- Axitinib FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [Article]
- INLYTA® (axitinib) FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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. 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
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [Article]
- INLYTA® (axitinib) FDA Label [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [Article]
- Hu S, Mathijssen RH, de Bruijn P, Baker SD, Sparreboom A: Inhibition of OATP1B1 by tyrosine kinase inhibitors: in vitro-in vivo correlations. Br J Cancer. 2014 Feb 18;110(4):894-8. doi: 10.1038/bjc.2013.811. Epub 2014 Jan 7. [Article]
Drug created at March 19, 2008 16:41 / Updated at February 20, 2024 23:54