Drug intelligence / Profile preview

regorafenib + rifampin

Development stage
Phase 1
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Regorafenib is an orally administered small molecule multikinase inhibitor used primarily for the treatment of metastatic colorectal cancer, unresectable or metastatic gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma. It works by inhibiting multiple membrane-bound and intracellular kinases involved in oncogenesis (tumor growth), angiogenesis (formation of new blood vessels that supply tumors), and maintenance of the tumor microenvironment. Key targets include VEGFR1/2/3, RET, KIT, PDGFR-alpha/beta, FGFR1/2, TIE2, DDR2, TrkA, Eph2A, RAF-1/BRAF/BRAFV600E among others[5][6][8]. Regorafenib is developed by Bayer and marketed under the brand name Stivarga[5]. Rifampin is a well-known antibiotic primarily used to treat tuberculosis and other bacterial infections. It acts as a potent inducer of cytochrome P450 enzymes (notably CYP3A4) in the liver. The combination "regorafenib + rifampin" is not an approved therapy but may be referenced in drug interaction studies because co-administration can significantly reduce plasma concentrations of regorafenib due to induction of its metabolism by rifampin.

Brand names
Rifadin
Other names
regorafenibrifampicin
02

Targets

BRAF V600EFGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)RNAP (Bacterial dna-dependent RNA polymerase)DDR2 (Discoidin domain receptor tyrosine kinase 2)EPHA2 (Ephrin type-A receptor 2)FGFR2 (Keratinocyte growth factor receptor)NTRK1 (Tropomyosin-related receptor kinase A)

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