Overview

Generic Name(s):
regorafenib
Trade Name(s):
Stivarga
NCI Definition [1]:
An orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling.

Regorafenib has been investigated in 45 clinical trials, of which 39 are open and 6 are closed. Of the trials investigating regorafenib, 7 are phase 1 (4 open), 8 are phase 1/phase 2 (7 open), 23 are phase 2 (21 open), 1 is phase 2/phase 3 (1 open), 5 are phase 3 (5 open), and 1 is no phase specified (1 open).

KIT Mutation, Deficient DNA Mismatch Repair (dMMR), and MLH1 Deficient Expression are the most frequent biomarker inclusion criteria for regorafenib clinical trials.

Colorectal carcinoma, colorectal adenocarcinoma, and hepatocellular carcinoma are the most common diseases being investigated in regorafenib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Regorafenib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Regorafenib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating regorafenib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
bay 73-4506, Stivarga, 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide, regorafenib, regorafenib (product), bay73-4506, 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide, bay-73-4506, multikinase inhibitor bay 73-4506, regorafenib (substance), regorafenib, regorafenibum
Drug Categories [2]:
BRAF inhibitors, RET inhibitors, Serine/threonine kinase inhibitors, Tyrosine kinase inhibitors, VEGFR-2 inhibitors
Drug Target(s) [2]:
ABL1, BRAF, CSF1R, DDR2, EPHA2, FLT1, FLT4, FRK, KDR, KIT, MAPK11, NTRK1, PDGFRA, PDGFRB, RAF1, RET, TEK
NCIT ID [1]:
C78204
SNOMED ID [1]:
R-FBDC8

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.