Medical Pharmacology Practice Questions: Tyrosine Kinase Inhibitor (VEGFR-1,2,3 and many other kinases) : regorafenib (Stivarga)
Click on the correct answer.
Regorafinib is a protein kinase inhibitor, inhibiting the kinase enzyme activity of VEGFR1-3 as well as many other kinases.
True
Falls
Regorafinib inhibits some kinases that:
Appear involved in pathologic angiogenesis
Appear to promote progression of malignant disease
Both
Neither
Regorafinib and clinical use:
Regorafinib may be used in treating certain patients diagnosed with metastatic colorectal cancer (mCRC).
Regorafinib and sorafenib may be used in management of hepatocellular carcinoma.
Both
Neither
In patients with hepatocellular carcinoma (HCC) whose disease progressed during treatment with sorafenib, regorafinib may be an appropriate alternative.
True
False
Broader kinase inhibition profile (will inhibit more different kinases):
Sorafenib
Regorafinib
Regorafinib is been approved as second-line treatment for advanced gastrointestinal stromal tumors (GIST) when:
Disease has become imatinib-resistant.
Disease has progressed despite treatment with sunitinib.
Both
Neither
Regorafinib pharmacokinetic/pharmacodynamics:
This agent is orally bioavailable.
Regorafinib is metabolized by the cytochrome P450 drug metabolizing system, mainly by CYP3A4 isoform.
The drug half-life is about 28 hours.
A & B
B & C
A & C
A, B & C
Regorafinib has been approved for use in patients with advanced hepatocellular carcinoma, previously treated with sorafenib.
True
Major adverse effects/effects associated with regorafinib administration:
Hepatotoxicity
Macular degeneration
Both
Neither
Because of possible fetal injury, based on animal studies, females with reproductive potential should employ effective contraception during regorafinib administration and for two months after the last dose. Males with female partners of reproductive potential should also use effective contraception during the same timeframe.
