Drug intelligence / Profile preview

cabozantinib + trifluridine + tipiracil

Development stage
Unknown
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

Cabozantinib + trifluridine + tipiracil is an investigational combination therapy studied primarily for refractory metastatic colorectal carcinoma (mCRC). Cabozantinib is a small molecule multikinase inhibitor targeting several tyrosine kinases involved in tumor growth and angiogenesis, including MET, VEGFRs, AXL, RET, and others. Trifluridine/tipiracil (also known as TAS-102) is an oral antitumor agent combining a nucleoside metabolic inhibitor (trifluridine) with a thymidine phosphorylase inhibitor (tipiracil), which increases the bioavailability of trifluridine by preventing its degradation. The combination aims to enhance antitumor activity through both targeted inhibition of oncogenic signaling pathways and cytotoxic effects on DNA synthesis. Early-phase clinical trials have shown that this regimen is feasible and tolerable at standard doses with supportive care such as growth factors; it has demonstrated encouraging disease control rates in heavily pretreated mCRC patients[1][2][4][7].

Other names
cabozantinib and trifluridine/tipiracilcabozantinib plus TAS-102cabo + FTD/TPI
02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)DNATYMP (Thymidine phosphorylase)RET (Rearranged during transfection receptor tyrosine kinase)

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