Drug intelligence / Profile preview

regorafenib + rifampin

Development stage
Unknown
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
StivargaRifadin
Other names
regorafenibrifampicin
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)TEK (Tie2)PDGFRB (Platelet-derived growth factor receptor beta)PDGFRA (Platelet-derived growth factor receptor alpha)CYP3A4 (Cytochrome P450 3A4)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)BRAF V600E

Beyond the preview

Go deeper on regorafenib + rifampin.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Clinical trials

Full profile access

Follow clinical development from study design and recruitment through results.

  • Trial phase
  • Status
  • Readouts

Indications & development

Full profile access

Explore development by indication, patient population, and geography.

  • Indications
  • Development status
  • Countries

Licensing & deals

Full profile access

Trace asset ownership, licensing agreements, and commercial partnerships.

  • Partners
  • Deal terms
  • Milestones

Patents & exclusivity

Full profile access

Explore the patent landscape and regulatory exclusivity around an asset.

  • Patents
  • Expiration dates
  • Exclusivity

Competitive landscape

Full profile access

Compare development programs by target, modality, and indication.

  • Competing assets
  • Targets
  • Development stage

Research & analysis

Full profile access

Connect source evidence and development news to your research questions.

  • Publications
  • News
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on regorafenib + rifampin.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call