Drug intelligence / Profile preview

irinotecan + leucovorin + fluorouracil + docetaxel + cisplatin

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a multi-agent chemotherapy regimen composed of five drugs—irinotecan, leucovorin (folinic acid), fluorouracil (5-FU), docetaxel, and cisplatin. Each drug has a distinct mechanism of action: - Irinotecan is a topoisomerase I inhibitor that disrupts DNA replication in cancer cells. - Leucovorin enhances the cytotoxic effect of fluorouracil by stabilizing its binding to thymidylate synthase. - Fluorouracil is an antimetabolite that inhibits thymidylate synthase, thereby blocking DNA synthesis. - Docetaxel is a taxane that inhibits microtubule depolymerization, disrupting cell division. - Cisplatin forms DNA crosslinks and induces apoptosis in rapidly dividing cells. This combination targets multiple pathways involved in cancer cell proliferation and survival. Regimens containing subsets of these drugs are used primarily for advanced gastric cancer and other gastrointestinal malignancies[1][4][6]. The addition of all five agents represents an intensive approach aimed at maximizing tumor response but may be associated with significant toxicity.

02

Targets

TOP1 (DNA Topoisomerase I)DNATUBB (Tubulin (alpha and beta subunits))TS (Thymidylate synthase)

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