Cabozantinib

Identification

Summary

Cabozantinib is a tyrosine kinase inhibitor used to treat advanced renal cell carcinoma, hepatocellular carcinoma, and medullary thyroid cancer.

Brand Names
Cabometyx, Cometriq
Generic Name
Cabozantinib
DrugBank Accession Number
DB08875
Background

Cabozantinib was first approved in 2012 and is a non-specific tyrosine kinase inhibitor. It was initially approved in the US under the brand name Cometriq, which is indicated for the treatment of metastatic medullary thyroid cancer.6 In 2016, a capsule formulation (Cabometyx) was approved for the treatment of advanced renal cell carcinoma, and this same formulation gained additional approval in both the US and Canada in 2019 for the treatment of hepatocellular carcinoma in previously treated patients.7,8

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 501.514
Monoisotopic: 501.169999048
Chemical Formula
C28H24FN3O5
Synonyms
  • Cabozantinib
External IDs
  • BMS 907351
  • BMS907351
  • XL 184
  • XL-184
  • XL184

Pharmacology

Indication

Cabozantinib is indicated for the treatment of progressive, metastatic medullary thyroid cancer.6 It is also indicated for the treatment of advanced renal cell carcinoma and for hepatocellular carcinoma in patients previously treated with sorafenib.7,8

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAdvanced renal cell carcinomaRegimen in combination with: Nivolumab (DB09035)•••••••••••••••••••• ••••••
Treatment ofAdvanced renal cell carcinoma••••••••••••••••••
Treatment ofAdvanced renal cell carcinoma••••••••••••••••••••• •• •••••••••••• ••••• ••••••••• •••••••••••
Treatment ofAdvanced renal cell carcinoma•••••••••••••••••••••• ••••••• •••• •••••••••••••••
Treatment ofHepatocellular carcinoma•••••••••••••••••••••• ••••••• •••• •••••••••••••••
Contraindications & Blackbox Warnings
Prevent Adverse Drug Events Today
Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events with our Clinical API
Learn more
Pharmacodynamics

Cabozantinib suppresses metastasis, angiogenesis, and oncognesis by inhibiting receptor tyrosine kinases.

Mechanism of action

Cabozantinib inhibits specific receptor tyrosine kinases such as VEGFR-1, -2 and -3, KIT, TRKB, FLT-3, AXL, RET, MET, and TIE-2.

TargetActionsOrganism
AHepatocyte growth factor receptor
antagonist
Humans
AVascular endothelial growth factor receptor 2
antagonist
Humans
AProto-oncogene tyrosine-protein kinase receptor Ret
antagonist
Humans
Absorption

After oral administration, peak plasma concentration was achieved in 2-5 hours.

Volume of distribution

The volume of distribution is 349L.

Protein binding

Cabozantinib has extensive plasma protein binding (≥ 99.7%).

Metabolism

Cabozantinib is metabolized mostly by CYP3A4 and, to a minor extent, by CYP2C9. Both enzyme produce an N-oxide metabolite.

Route of elimination

Cabozantinib is eliminated mostly by the feces (54%) and also by the urine (27%).

Half-life

Cabozantinib has a long half-life of 55 hours.

Clearance

At steady state, the clearance is 4.4 L/hr.

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!
See the data
Improve decision support & research outcomes with our structured adverse effects data.
See a data sample
Toxicity

Cabozantinib carries a warning of serious gastrointestinal fistulas and perforations, and potentially fatal hemoptysis and gastrointestinal hemorrhage.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Cabozantinib can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Cabozantinib can be increased when combined with Abatacept.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Cabozantinib.
AcenocoumarolThe metabolism of Cabozantinib can be decreased when combined with Acenocoumarol.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Cabozantinib.
Food Interactions
  • Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase levels of cabozantinib.
  • Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce serum levels of cabozantinib.
  • Take on an empty stomach. Separate the administration of cabozantinib from food by at least 1 hour before or 2 hours after eating.
  • Take with a full glass of water.

Products

Drug product information from 10+ global regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
Product Ingredients
IngredientUNIICASInChI Key
Cabozantinib malateDR7ST46X581140909-48-3HFCFMRYTXDINDK-WNQIDUERSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CabometyxTablet40 mgOralIpsen Biopharmaceuticals Canada Inc2018-10-10Not applicableCanada flag
CabometyxTablet40 mg/1OralExelixis, Inc.2016-04-25Not applicableUS flag
CabometyxTablet, film coated40 mgOralIpsen Pharma2020-12-16Not applicableEU flag
CabometyxTablet20 mgOralIpsen Biopharmaceuticals Canada Inc2018-10-10Not applicableCanada flag
CabometyxTablet60 mg/1OralExelixis, Inc.2016-04-25Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
COMETRIQCabozantinib malate (20 MG) + Cabozantinib malate (80 MG)CapsuleOralIpsen Pharma2014-10-06Not applicableItaly flag
CometriqCabozantinib malate (80 mg/1) + Cabozantinib malate (20 mg/1)Capsule; KitOralExelixis, Inc.2012-11-29Not applicableUS flag
CometriqCabozantinib malate (80 mg/1) + Cabozantinib malate (20 mg/1)Capsule; KitOralExelixis, Inc.2012-11-29Not applicableUS flag
CometriqCabozantinib malate (20 mg/1) + Cabozantinib malate (80 mg/1)KitOralCatalent Pharma Solutions, Llc2012-11-292018-01-19US flag
COMETRIQCabozantinib malate (20 MG) + Cabozantinib malate (80 MG)CapsuleOralIpsen Pharma2016-05-06Not applicableItaly flag

Categories

ATC Codes
L01EX07 — Cabozantinib
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Ethers
Direct Parent
Diarylethers
Alternative Parents
Quinolines and derivatives / Anilides / Phenoxy compounds / Anisoles / N-arylamides / Alkyl aryl ethers / Fluorobenzenes / Pyridines and derivatives / Aryl fluorides / Cyclopropanecarboxylic acids and derivatives
show 8 more
Substituents
Alkyl aryl ether / Anilide / Anisole / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Benzenoid / Carbonyl group / Carboxamide group
show 21 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, dicarboxylic acid diamide, aromatic ether, quinolines (CHEBI:72317)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
1C39JW444G
CAS number
849217-68-1
InChI Key
ONIQOQHATWINJY-UHFFFAOYSA-N
InChI
InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
IUPAC Name
N'1-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
SMILES
COC1=CC2=C(C=C1OC)C(OC1=CC=C(NC(=O)C3(CC3)C(=O)NC3=CC=C(F)C=C3)C=C1)=CC=N2

References

General References
  1. Durante C, Russo D, Verrienti A, Filetti S: XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413. doi: 10.1517/13543784.2011.559163. [Article]
  2. Choueiri TK, Escudier B, Powles T, Mainwaring PN, Rini BI, Donskov F, Hammers H, Hutson TE, Lee JL, Peltola K, Roth BJ, Bjarnason GA, Geczi L, Keam B, Maroto P, Heng DY, Schmidinger M, Kantoff PW, Borgman-Hagey A, Hessel C, Scheffold C, Schwab GM, Tannir NM, Motzer RJ: Cabozantinib versus Everolimus in Advanced Renal-Cell Carcinoma. N Engl J Med. 2015 Nov 5;373(19):1814-23. doi: 10.1056/NEJMoa1510016. Epub 2015 Sep 25. [Article]
  3. Krajewska J, Olczyk T, Jarzab B: Cabozantinib for the treatment of progressive metastatic medullary thyroid cancer. Expert Rev Clin Pharmacol. 2016;9(1):69-79. doi: 10.1586/17512433.2016.1102052. Epub 2015 Nov 4. [Article]
  4. Grullich C: Cabozantinib: a MET, RET, and VEGFR2 tyrosine kinase inhibitor. Recent Results Cancer Res. 2014;201:207-14. doi: 10.1007/978-3-642-54490-3_12. [Article]
  5. Escudier B, Lougheed JC, Albiges L: Cabozantinib for the treatment of renal cell carcinoma. Expert Opin Pharmacother. 2016 Dec;17(18):2499-2504. doi: 10.1080/14656566.2016.1258059. Epub 2016 Nov 22. [Article]
  6. FDA Approved Drug Products: Cometriq (cabozantinib) oral capsules [Link]
  7. FDA Approved Drug Products: Cabometyx (cabozantinib) oral tablets [Link]
  8. Health Canada Product Monograph: Cabometyx (cabozantinib) oral tablets [Link]
KEGG Drug
D10062
PubChem Compound
25102847
PubChem Substance
347827806
ChemSpider
25948202
BindingDB
50021574
RxNav
1363268
ChEBI
72317
ChEMBL
CHEMBL2105717
ZINC
ZINC000070466416
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cabozantinib
FDA label
Download (194 KB)

Clinical Trials

Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package
PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
4Active Not RecruitingTreatmentThyroid Gland Medullary Carcinoma1somestatusstop reasonjust information to hide
4CompletedTreatmentHepatocellular Carcinoma1somestatusstop reasonjust information to hide
3Active Not RecruitingTreatmentAdenocarcinoma of Prostate / Metastatic Prostate Cancer1somestatusstop reasonjust information to hide
3Active Not RecruitingTreatmentAdvanced Bladder Urothelial Carcinoma / Advanced Renal Pelvis Urothelial Carcinoma / Advanced Ureter Urothelial Carcinoma / Advanced Urethral Urothelial Carcinoma / Metastatic Renal Pelvis Urothelial Carcinoma / Metastatic Ureter Urothelial Carcinoma / Metastatic Urethral Urothelial Carcinoma / Metastatic Urothelial Carcinoma of the Bladder / Stage III Bladder Cancer AJCC v8 / Stage III Renal Pelvis and Ureter Cancer AJCC v8 / Stage III Renal Pelvis Cancer AJCC v8 / Stage III Ureter Cancer AJCC v8 / Stage III Urethral Cancer AJCC v8 / Stage IV Bladder Cancer AJCC v8 / Stage IV Renal Pelvis and Ureter Cancer AJCC v8 / Stage IV Renal Pelvis Cancer AJCC v8 / Stage IV Ureter Cancer AJCC v8 / Stage IV Urethral Cancer AJCC v81somestatusstop reasonjust information to hide
3Active Not RecruitingTreatmentCarcinoid Tumors / Functioning Pancreatic Neuroendocrine Tumor / Intermediate Grade Lung Neuroendocrine Neoplasm / Locally Advanced Digestive System Neuroendocrine Neoplasm / Locally Advanced Digestive System Neuroendocrine Tumor G1 / Locally Advanced Lung Neuroendocrine Neoplasm / Locally Advanced Pancreatic Neuroendocrine Tumor / Low Grade Lung Neuroendocrine Neoplasm / Lung Neuroendocrine Tumor / Lung Neuroendocrine Tumor G2 / Metastatic Digestive System Neuroendocrine Neoplasm / Metastatic Digestive System Neuroendocrine Tumor G1 / Metastatic Lung Neuroendocrine Neoplasm / Metastatic Lung Neuroendocrine Tumor / Metastatic Pancreatic Neuroendocrine Neoplasm / Metastatic Pancreatic Neuroendocrine Tumors / Metastatic Thymic Neuroendocrine Neoplasm / Neuroendocrine Tumor G2 / Neuroendocrine Tumors / Non-Functional Pancreatic Neuroendocrine Tumor / Serotonin-Producing Pancreatic Neuroendocrine Tumor / Thymic Neuroendocrine Tumors / Unresectable Digestive System Neuroendocrine Neoplasm / Unresectable Digestive System Neuroendocrine Tumor G1 / Unresectable Lung Neuroendocrine Neoplasm / Unresectable Pancreatic Neuroendocrine Neoplasm / Unresectable Thymic Neuroendocrine Neoplasm / Unresectable, locally advanced Neuroendocrine Tumors of the Digestive System1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral25.340 mg
TabletOral20 mg
TabletOral20 mg/1
TabletOral40 mg/1
TabletOral40 mg
TabletOral60 mg
TabletOral60 mg/1
Tablet, film coatedOral20 mg
Tablet, film coatedOral40 mg
Tablet, film coatedOral60 mg
CapsuleOral
CapsuleOral20 mg/1
CapsuleOral20 MG
Capsule; kitOral
KitOral
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8877776No2014-11-042030-10-08US flag
US7579473No2009-08-252024-09-24US flag
US8497284No2013-07-302024-09-24US flag
US9724342No2017-08-082033-07-09US flag
US9717720No2017-08-012032-02-10US flag
US10039757No2018-08-072031-07-18US flag
US10034873No2018-07-312031-07-18US flag
US11098015No2021-08-242030-01-15US flag
US11091439No2021-08-172030-01-15US flag
US11091440No2021-08-172030-01-15US flag
US11141413No2021-10-122037-04-17US flag
US11298349No2012-02-102032-02-10US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityCOMETRIQ is practically insoluble in water.From FDA label.
Predicted Properties
PropertyValueSource
Water Solubility0.00199 mg/mLALOGPS
logP4.01ALOGPS
logP4.66Chemaxon
logS-5.4ALOGPS
pKa (Strongest Acidic)13.46Chemaxon
pKa (Strongest Basic)5.9Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area98.78 Å2Chemaxon
Rotatable Bond Count8Chemaxon
Refractivity136.12 m3·mol-1Chemaxon
Polarizability51.49 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0139180000-20096332e7e989d72392
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udl-0018090000-f02b7154b60e594f6ec2
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0uk9-0818290000-46f7beab97994099a1f5
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-02t9-2009010000-3fd00a48b8b4cc61c3c3
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-00kf-9025020000-dd73221d97d68a870406
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0w4i-1409340000-f5539cadca01ccab399a
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-00g0-0901000000-9f43de968564cfe8c124
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-208.07274
predicted
DeepCCS 1.0 (2019)
[M+H]+210.4683
predicted
DeepCCS 1.0 (2019)
[M+Na]+216.38084
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
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to hepatocyte growth factor/HGF ligand. Regulates many physiological processes including...
Gene Name
MET
Uniprot ID
P08581
Uniprot Name
Hepatocyte growth factor receptor
Molecular Weight
155540.035 Da
References
  1. Kurzrock R, Sherman SI, Ball DW, Forastiere AA, Cohen RB, Mehra R, Pfister DG, Cohen EE, Janisch L, Nauling F, Hong DS, Ng CS, Ye L, Gagel RF, Frye J, Muller T, Ratain MJ, Salgia R: Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer. J Clin Oncol. 2011 Jul 1;29(19):2660-6. doi: 10.1200/JCO.2010.32.4145. Epub 2011 May 23. [Article]
  2. Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, Qian F, Chu F, Bentzien F, Cancilla B, Orf J, You A, Laird AD, Engst S, Lee L, Lesch J, Chou YC, Joly AH: Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011 Dec;10(12):2298-308. doi: 10.1158/1535-7163.MCT-11-0264. Epub 2011 Sep 16. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
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
  1. Kurzrock R, Sherman SI, Ball DW, Forastiere AA, Cohen RB, Mehra R, Pfister DG, Cohen EE, Janisch L, Nauling F, Hong DS, Ng CS, Ye L, Gagel RF, Frye J, Muller T, Ratain MJ, Salgia R: Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer. J Clin Oncol. 2011 Jul 1;29(19):2660-6. doi: 10.1200/JCO.2010.32.4145. Epub 2011 May 23. [Article]
  2. Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, Qian F, Chu F, Bentzien F, Cancilla B, Orf J, You A, Laird AD, Engst S, Lee L, Lesch J, Chou YC, Joly AH: Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011 Dec;10(12):2298-308. doi: 10.1158/1535-7163.MCT-11-0264. Epub 2011 Sep 16. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation upon binding with glial cell de...
Gene Name
RET
Uniprot ID
P07949
Uniprot Name
Proto-oncogene tyrosine-protein kinase receptor Ret
Molecular Weight
124317.465 Da
References
  1. Kurzrock R, Sherman SI, Ball DW, Forastiere AA, Cohen RB, Mehra R, Pfister DG, Cohen EE, Janisch L, Nauling F, Hong DS, Ng CS, Ye L, Gagel RF, Frye J, Muller T, Ratain MJ, Salgia R: Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer. J Clin Oncol. 2011 Jul 1;29(19):2660-6. doi: 10.1200/JCO.2010.32.4145. Epub 2011 May 23. [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
  1. Nguyen L, Holland J, Miles D, Engel C, Benrimoh N, O'Reilly T, Lacy S: Pharmacokinetic (PK) drug interaction studies of cabozantinib: Effect of CYP3A inducer rifampin and inhibitor ketoconazole on cabozantinib plasma PK and effect of cabozantinib on CYP2C8 probe substrate rosiglitazone plasma PK. J Clin Pharmacol. 2015 Sep;55(9):1012-23. doi: 10.1002/jcph.510. Epub 2015 Jun 2. [Article]
  2. Gerendash BS, Creel PA: Practical management of adverse events associated with cabozantinib treatment in patients with renal-cell carcinoma. Onco Targets Ther. 2017 Oct 19;10:5053-5064. doi: 10.2147/OTT.S145295. eCollection 2017. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Cabozantinib FDA Label [File]
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. Escudier B, Lougheed JC, Albiges L: Cabozantinib for the treatment of renal cell carcinoma. Expert Opin Pharmacother. 2016 Dec;17(18):2499-2504. doi: 10.1080/14656566.2016.1258059. Epub 2016 Nov 22. [Article]

Drug created at May 13, 2013 00:12 / Updated at November 01, 2023 04:04