Drug intelligence / Profile preview

TAS-102 + oxaliplatin + irinotecan + bevacizumab

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a multi-agent chemotherapy regimen combining four drugs: **TAS-102 (trifluridine/tipiracil)** is an oral antimetabolite composed of a thymidine-based nucleoside analog (trifluridine) and a thymidine phosphorylase inhibitor (tipiracil). It disrupts DNA synthesis in tumor cells. **Oxaliplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks, inhibiting DNA replication and transcription. **Irinotecan** is a topoisomerase I inhibitor that prevents DNA unwinding necessary for replication. **Bevacizumab** is a monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis required for tumor growth. This combination has been studied primarily in metastatic colorectal cancer patients who have progressed after standard therapies including fluoropyrimidines, oxaliplatin, irinotecan, anti-EGFR agents, and antiangiogenic therapy[1][2][6][10]. The rationale for the combination leverages non-overlapping mechanisms of action to overcome resistance seen with prior lines of therapy.

Brand names
Lonsurf
Other names
trifluridine and tipiracil plus oxaliplatin, irinotecan, and bevacizumab
02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)VEGFA (Vascular endothelial growth factor A)TYMP (Thymidine phosphorylase)DNA

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