Drug intelligence / Profile preview

futuximab + modotuximab + trifluridine + tipiracil

Development stage
Discontinued
Lead developer
Servier
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination therapy consisting of two monoclonal antibodies, futuximab and modotuximab, administered together with the oral fixed-dose combination of trifluridine and tipiracil. Futuximab and modotuximab are anti-EGFR (epidermal growth factor receptor) monoclonal antibodies that bind to different epitopes on EGFR, leading to inhibition of EGFR signaling pathways involved in tumor cell proliferation and survival. Trifluridine is a nucleoside analog that incorporates into DNA during replication, causing DNA dysfunction and cell death; tipiracil inhibits thymidine phosphorylase, thereby increasing the bioavailability of trifluridine. This regimen has been investigated for use in patients with metastatic colorectal cancer who have wild-type KRAS/NRAS/BRAF genes and have progressed after standard therapies including prior anti-EGFR treatment[2][5][9]. The rationale for combining these agents is to enhance antitumor efficacy by targeting both EGFR-mediated signaling (with futuximab/modotuximab) and DNA synthesis (with trifluridine/tipiracil)[2].

02

Targets

TYMP (Thymidine phosphorylase)EGFR (Epidermal growth factor receptor)DNA

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