Drug intelligence / Profile preview

trifluridine + cetuximab

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

Overview

Trifluridine + cetuximab is a combination therapy being investigated for the treatment of RAS wild-type metastatic colorectal cancer (mCRC). Trifluridine, a thymidine-based nucleoside analogue, exerts its antineoplastic effect by being phosphorylated into a metabolite that inhibits thymidylate synthase and incorporates into DNA, leading to DNA dysfunction and cell death. Cetuximab is a recombinant human/mouse chimeric monoclonal antibody that binds specifically to the extracellular domain of the epidermal growth factor receptor (EGFR), competitively inhibiting the binding of epidermal growth factor (EGF) and other ligands. This blockade inhibits downstream signaling pathways, such as MAPK and PI3K/Akt, which are critical for tumor growth, progression, and survival. In clinical trials, such as those conducted by Hunan Cancer Hospital, trifluridine is typically administered as part of the TAS-102 (trifluridine/tipiracil) fixed-dose combination to enhance its bioavailability and therapeutic efficacy.

Other names
trifluridine/cetuximabTAS-102 + cetuximabFTD + cetuximab
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TS (Thymidylate synthase)DNA

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