Drug intelligence / Profile preview

TAS-102 + regorafenib + fruquintinib

Development stage
Unknown
Lead developer
Shanghai Jinmante Biotechnology
Modality
Small Molecules
Administration
Oral
01

Overview

TAS-102 + regorafenib + fruquintinib refers to the physician's choice comparator arm used in clinical trials for advanced colorectal cancer, most notably the Phase 3 JSKN003-005 trial sponsored by Shanghai JMT-Bio Inc. This arm allows investigators to select one of three standard-of-care small molecule therapies for patients who have failed prior chemotherapy with oxaliplatin, fluorouracil, and irinotecan. TAS-102 (trifluridine/tipiracil) is a cytotoxic combination of a nucleoside analog and a thymidine phosphorylase inhibitor. Regorafenib is a multi-kinase inhibitor that targets angiogenic, stromal, and oncogenic pathways. Fruquintinib is a highly selective inhibitor of VEGFR-1, -2, and -3. These agents are typically utilized as third-line or later treatments for metastatic colorectal cancer.

Brand names
Lonsurf
Other names
Trifluridine/tipiracilTrifluridine and tipiracil hydrochloridePhysician's choice treatment
02

Targets

TS (Thymidylate synthase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)RAF1 (c-Raf-1 (Y340D/Y341D))BRAF (B-Raf proto-oncogene, serine/threonine kinase)PDGFRB (Platelet-derived growth factor receptor beta)TYMP (Thymidine phosphorylase)VEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)TEK (Tie2)RET (Rearranged during transfection receptor tyrosine kinase)

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