Regorafenib Monohydrate

IUPAC name

4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrate

CAS No.

1019206-88-2

Molecular Weight

500.8 g·mol−1

Molecular Formula

C21H17ClF4N4O4

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Mechanism Of Action:

Regorafenib is an inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes including, oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E , SAPK2, PTK5, and Abl at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib showed anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma.

Indication:

It is indicated for:

  • The treatment of colon or rectal cancer that has spread to other parts of the body and for which they have received previous treatment with certain chemotherapy medicines.
  • The treatment of a rare stomach, bowel, or esophagus cancer called GIST (gastrointestinal stromal tumor) which can’t be treated with surgery or that has spread to other parts of the body and for which they have received previous treatment with certain medicines.
  • The treatment of a type of liver cancer called hepatocellular carcinoma (HCC) in people who have been previously treated with sorafenib.