Synonyms: BAY 73-4506 | Stivarga®
regorafenib is an approved drug (FDA (2012), EMA (2013))
Compound class:
Synthetic organic
Comment: Regorafenib is an inhibitor of multiple membrane-bound and intracellular kinases. Although the drug is approved it must carry a Boxed Warning alerting patients and clinicians that severe and fatal liver toxicity was observed in some patients in regorafenib clinical studies. Regorafenib is a Type-2 kinase inhibitor.
Ligand Activity Visualisation ChartsThese 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: regorafenib |
|
References |
1. Hafner FT, Werner D, Kaiser M. (2014)
Determination of regorafenib (BAY 73-4506) and its major human metabolites BAY 75-7495 (M-2) and BAY 81-8752 (M-5) in human plasma by stable-isotope dilution liquid chromatography-tandem mass spectrometry. Bioanalysis, 6 (14): 1923-37. [PMID:25158964] |
2. Wilhelm SM, Dumas J, Adnane L, Lynch M, Carter CA, Schütz G, Thierauch KH, Zopf D. (2011)
Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 129 (1): 245-55. [PMID:21170960] |
3. Zambon A, Niculescu-Duvaz I, Niculescu-Duvaz D, Marais R, Springer CJ. (2012)
Small molecule inhibitors of BRAF in clinical trials. Bioorg Med Chem Lett, 22 (2): 789-92. [PMID:22222036] |