- Guide to PHARMACOLOGY
Synonyms: BMS907351 | Cabometyx® | Cometriq® | XL-184 | XL184
cabozantinib is an approved drug (FDA (2012), EMA (2014))
Compound class: Synthetic organic
Comment: Cabozantinib is a Type-1, oral, small-molecule tyrosine kinase inhibitor.
Marketed formulations contain cabozantinib S-malate (PubChem CID 25102846).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: cabozantinib
1. Abou-Alfa GK, Meyer T, Cheng AL, El-Khoueiry AB, Rimassa L, Ryoo BY, Cicin I, Merle P, Chen Y, Park JW et al.. (2018)
Cabozantinib in Patients with Advanced and Progressing Hepatocellular Carcinoma.
N Engl J Med, 379 (1): 54-63. [PMID:29972759]
2. Choueiri TK, Escudier B, Powles T, Mainwaring PN, Rini BI, Donskov F, Hammers H, Hutson TE, Lee JL, Peltola K et al.. (2015)
Cabozantinib versus Everolimus in Advanced Renal-Cell Carcinoma.
N Engl J Med, 373 (19): 1814-23. [PMID:26406150]
FDA approves cabozantinib for hepatocellular carcinoma.
Accessed on 16/01/2019. Modified on 16/01/2019. www.fda.gov, https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm629512.htm?utm_campaign=Oncology%201%2F15%2F2019%20cabozantinib&utm_medium=email&utm_source=Eloqua&elqTrackId=f0cd47cbe0e04a7e88308645f7d66a61&elq=249a34ffaff94fdb97f2d843ed80fa79&elqaid=6487&elqat=1&elqCampaignId=5289
FDA grants regular approval to Cabometyx for first-line treatment of advanced renal cell carcinoma.
Accessed on 03/01/2018. Modified on 03/01/2018. fda.gov, https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm589842.htm?utm_campaign=Oncology%2012%2F20&utm_medium=email&utm_source=Eloqua&elqTrackId=9bc32150b77e4929b686ed8a82ffbb6e&elq=70477587f45543ad83873a1367bab364&elqaid=1850&elqat=1&elqCampaignId=1227
5. Subbiah V, Gainor JF, Rahal R, Brubaker JD, Kim JL, Maynard M, Hu W, Cao Q, Sheets MP, Wilson D et al.. (2018)
Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.
Cancer Discov, 8 (7): 836-849. [PMID:29657135]
6. Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, Qian F, Chu F, Bentzien F, Cancilla B et al.. (2011)
Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.
Mol Cancer Ther, 10 (12): 2298-308. [PMID:21926191]