Drug intelligence / Profile preview

EMD 1201081 + fluorouracil + cisplatin + cetuximab

Development stage
Discontinued
Lead developer
Merck KGaA
Modality
Small Molecules, MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Subcutaneous, Intravenous
01

Overview

A combination regimen consisting of **EMD 1201081**, a synthetic phosphorothioate oligodeoxynucleotide and Toll-like receptor 9 (TLR9) agonist, plus **fluorouracil** (5-FU), **cisplatin**, and **cetuximab**—all administered for the first-line treatment of patients with recurrent or metastatic squamous cell carcinoma of the head and neck (SCCHN). - **EMD 1201081** stimulates innate immunity by binding TLR9 on plasmacytoid dendritic cells and B cells, promoting cytokine and chemokine release and a Th1-type immune response, which has potential antitumor effects. - **Fluorouracil** is an antimetabolite that inhibits thymidylate synthase, impairing DNA synthesis. - **Cisplatin** is a platinum-based alkylating agent, crosslinking DNA and causing apoptosis. - **Cetuximab** is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR), blocking downstream signaling leading to inhibited tumor growth and apoptosis. This combination was investigated for improved efficacy in recurrent/metastatic SCCHN but the trial was terminated.

Other names
5-FU + cisplatin + cetuximab + EMD 1201081
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TLR9 (Toll-like receptor 9)DNATS (Thymidylate synthase)

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