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 |
|
No information available. |
Summary of Clinical Use |
Regorafenib is used to treat metastatic colorectal cancer and advanced gastrointestinal stromal tumours. In April 2017 the US FDA expanded approval to include treatment of patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib. |
Pharmacokinetics |
Absorption/Distribution |
Regorafenib circulates in the enterohepatic system and is almost completely bound to plasma proteins (99.5%). |
Biotransformation/Metabolism |
CYP3A4 and UGT1A9 generate the metabolites of regorafenib, M-2 (N-oxide; BAY 75-7495) and M-5 (N-oxide and N-desmethyl; BAY 81-8752) which have similar in vitro pharmacological activities and steady-state concentrations as regorafenib [1]. |
Elimination |
In vivo excretion of radiolabelled regorafinib indicates that after 12 days a total of 90% was eliminated (71% in feces and 19% in urine). |
External links |
For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |