Drug intelligence / Profile preview

irinotecan + cisplatin + fluorouracil

Development stage
Phase 1
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules
Administration
Intravenous
01

Overview

This combination chemotherapy regimen consists of irinotecan, cisplatin, and fluorouracil (5-FU). It was evaluated in a Phase I dose-escalation study led by Memorial Sloan Kettering Cancer Center for the treatment of locally advanced or metastatic solid tumors, particularly gastric, esophageal, and pancreatic cancers. Fluorouracil is an antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis. Irinotecan is a topoisomerase I inhibitor that prevents DNA religation, leading to double-strand breaks, and cisplatin is a platinum-based DNA alkylating agent that forms cross-links to inhibit replication. The combination aims to enhance anti-tumor activity through multiple synergistic mechanisms, although it is associated with dose-limiting toxicities such as neutropenia and diarrhea.

Other names
5-FU + irinotecan + cisplatinweekly irinotecan, cisplatin, and fluorouracil
02

Targets

DNATOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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