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Drug intelligence / Profile preview
regorafenib + rosiglitazone
- Development stage
- Unknown
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
The combination of regorafenib and rosiglitazone is an investigational therapeutic regimen being evaluated for the treatment of advanced solid tumors. Regorafenib is a potent multi-kinase inhibitor that targets several pathways involved in tumor angiogenesis (VEGFR1, VEGFR2, VEGFR3, TIE2), oncogenesis (KIT, RET, RAF-1, BRAF), and the tumor microenvironment (PDGFR, FGFR). Rosiglitazone is a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, traditionally used as an antidiabetic agent, which has demonstrated the ability to induce cell cycle arrest and promote differentiation in various cancer cell lines. Preclinical research suggests that PPARγ activation may sensitize tumor cells to the effects of kinase inhibitors like regorafenib, potentially overcoming resistance mechanisms and enhancing anti-tumor efficacy. This combination has been studied in Phase 1 clinical trials to assess safety, tolerability, and the maximum tolerated dose in patients with refractory solid malignancies.
- Other names
- regorafenib and rosiglitazone
02
Targets
BRAF (B-Raf proto-oncogene, serine/threonine kinase)FGFR1 (Fibroblast growth factor receptor 1)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)VEGFR2 (Vascular endothelial growth factor receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Angiopoietin-1 receptor)TEK (Tie2)PPARG (Peroxisome proliferator-activated receptor gamma)
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