Drug intelligence / Profile preview

cetuximab + trifluridine tipiracil

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

Overview

Cetuximab + trifluridine tipiracil is a combination therapy used primarily in the treatment of metastatic colorectal cancer (mCRC), particularly in patients with RAS wild-type tumors who have progressed after standard therapies. Cetuximab is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR), inhibiting downstream signaling pathways involved in cell proliferation and survival. Trifluridine tipiracil (also known as TAS-102) is an oral antineoplastic agent composed of two components: trifluridine, a thymidine-based nucleoside analog that incorporates into DNA and disrupts DNA synthesis, and tipiracil, which inhibits thymidine phosphorylase to increase the bioavailability of trifluridine. The combination has been investigated as a rechallenge strategy for patients previously treated with anti-EGFR agents and standard chemotherapies[1][2][3]. Clinical studies suggest this regimen can improve disease control rates in refractory mCRC.

Brand names
ErbituxLonsurf
Other names
cetuximab + trifluridine/tipiracilcetuximab plus TAS-102FTD/TPI plus cetuximab
02

Targets

DNATYMP (Thymidine phosphorylase)EGFR T790M (Epidermal growth factor receptor T790M mutant)TS (Thymidylate synthase)

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