Drug intelligence / Profile preview

TAS-102 + irinotecan

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**TAS-102 + irinotecan** is a combination of two chemotherapeutic agents: TAS-102 (an oral nucleoside antitumor medication, containing trifluridine and tipiracil) and irinotecan (an intravenous topoisomerase I inhibitor)[1][3][4]. TAS-102 acts by incorporating trifluridine into DNA to disrupt tumor cell proliferation, while tipiracil prevents rapid breakdown of trifluridine, increasing its efficacy[2][3]. Irinotecan is converted to its active metabolite SN-38, which inhibits topoisomerase I, causing DNA damage and cell death. The combination targets refractory metastatic colorectal cancer and is being explored for other gastrointestinal malignancies, often in patients resistant to standard therapies such as 5-fluorouracil (5-FU) and oxaliplatin[1][2][4]. Recent trials have also investigated this regimen using liposomal irinotecan (Onivyde), which improves circulation half-life and tumor targeting[2][3].

Brand names
Lonsurf + Camptosar
Other names
trifluridine + tipiracil + irinotecanTAS-102 (trifluridine/tipiracil) + irinotecan hydrochlorideTAS-102 + Onivyde
02

Targets

DNATYMP (Thymidine phosphorylase)TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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