Drug intelligence / Profile preview

favezelimab + pembrolizumab + irinotecan + leucovorin + fluorouracil

Development stage
Unknown
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This is a combination regimen comprising five agents: favezelimab, pembrolizumab, irinotecan, leucovorin, and fluorouracil. Favezelimab is a human anti–LAG-3 (lymphocyte activation gene-3) monoclonal antibody that blocks the LAG-3 immune checkpoint receptor on lymphocytes, aiming to restore antitumor T-cell activity. Pembrolizumab is a humanized monoclonal antibody targeting PD-1 (programmed cell death protein 1) on T cells, releasing the "brakes" on the immune system to enhance antitumor response. Irinotecan is a topoisomerase I inhibitor that prevents DNA unwinding, leading to cytotoxicity in rapidly dividing cells. Leucovorin (folinic acid) is a reduced form of folic acid used to enhance the efficacy of fluorouracil and mitigate related toxicities. Fluorouracil (5-FU) is a pyrimidine antimetabolite that inhibits thymidylate synthase, disrupting DNA synthesis in cancer cells. This combination is being evaluated in metastatic solid tumors, including colorectal cancer, leveraging immunomodulatory and cytotoxic mechanisms. The principal developer and manufacturer for favezelimab and pembrolizumab is Merck. Irinotecan, leucovorin, and fluorouracil are widely available generics manufactured by numerous companies globally.

02

Targets

TS (Thymidylate synthase)PDCD1 (Programmed cell death protein 1 receptor)TOP1 (DNA Topoisomerase I)

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