Drug intelligence / Profile preview

Simmtecan + 5-fluorouracil + L-leucovorin

Development stage
Unknown
Lead developer
Shanghai Institute of Materia Medica
Modality
Small Molecules
Administration
Intravenous
01

Overview

FOLFSIM is an investigational combination chemotherapy regimen consisting of Simmtecan, 5-fluorouracil (5-FU), and L-leucovorin (l-LV). Simmtecan is a novel derivative of irinotecan developed by the Shanghai Institute of Materia Medica, acting as a topoisomerase I inhibitor to prevent DNA religation and cause double-strand breaks. 5-fluorouracil is an antimetabolite that inhibits thymidylate synthase, thereby disrupting DNA synthesis, while L-leucovorin is a folate analog that enhances the binding of 5-FU to thymidylate synthase, increasing its cytotoxic effect. This regimen is primarily being investigated by Peking University for the treatment of advanced or metastatic neuroendocrine carcinoma, often in combination with the PD-1 checkpoint inhibitor toripalimab.

Other names
Simmtecan + 5-FU + l-LVSimmtecan + 5-fluorouracil + levoleucovorin
02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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