Drug intelligence / Profile preview

Lonsurf + irinotecan

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

Overview

Lonsurf + irinotecan is a combination chemotherapy regimen being evaluated for the treatment of advanced or metastatic gastric and gastroesophageal junction (GEJ) adenocarcinoma. Lonsurf (TAS-102) is an oral fixed-dose combination of trifluridine, a thymidine-based nucleoside analog, and tipiracil, a thymidine phosphorylase inhibitor. Trifluridine's primary mechanism involves incorporation into viral and mammalian DNA, leading to DNA dysfunction and cytotoxic effects, while tipiracil prevents the rapid degradation of trifluridine by thymidine phosphorylase, thereby increasing its systemic exposure. Irinotecan is a semi-synthetic derivative of camptothecin that acts as a topoisomerase I inhibitor, stabilizing the cleavable complex between the enzyme and DNA, which results in double-strand DNA breaks during replication. The University of California, Irvine, has sponsored Phase Ib multicenter studies to determine the safety and efficacy of this combination in patients who have previously failed standard fluoropyrimidine and platinum-based therapies.

Brand names
LonsurfCamptosar
Other names
trifluridine + tipiracil + irinotecan
02

Targets

DNATOP1 (DNA Topoisomerase I)TYMP (Thymidine phosphorylase)

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