Drug intelligence / Profile preview

TAS-102 + bevacizumab + irinotecan

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

Overview

TAS-102 + bevacizumab + irinotecan is a combination regimen used primarily as a second-line therapy for metastatic colorectal cancer, particularly in patients who have progressed after standard first-line treatments such as oxaliplatin and fluoropyrimidines. TAS-102 is an oral antimetabolite composed of trifluridine and tipiracil; trifluridine incorporates into DNA, causing dysfunction and cell death, while tipiracil inhibits thymidine phosphorylase to maintain effective levels of trifluridine. Bevacizumab is a monoclonal antibody that targets vascular endothelial growth factor A (VEGF-A), inhibiting angiogenesis required for tumor growth. Irinotecan is a topoisomerase I inhibitor that prevents DNA unwinding and replication, leading to cell death. This combination has demonstrated antitumor activity with manageable toxicity profiles in phase I/II studies for metastatic colorectal cancer refractory to first-line therapies[1][2][5].

Brand names
Lonsurf (for TAS-102)Avastin (for bevacizumab)Campto (for irinotecan)
Other names
trifluridine/tipiracil + bevacizumab + irinotecan
02

Targets

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

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