Drug intelligence / Profile preview

cetuximab + irinotecan + tivantinib

Development stage
Phase 2
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three agents: - **Cetuximab** is a chimeric monoclonal antibody that targets the epidermal growth factor receptor (EGFR), inhibiting its activation and downstream signaling, which leads to reduced tumor cell proliferation and survival. - **Irinotecan** is a small molecule chemotherapeutic agent that inhibits topoisomerase I, an enzyme essential for DNA replication, resulting in DNA damage and apoptosis in rapidly dividing cells. - **Tivantinib** is an oral small molecule inhibitor primarily targeting the MET receptor tyrosine kinase (c-MET), which plays a role in tumor cell growth, survival, and metastasis. Tivantinib may also have additional mechanisms such as tubulin inhibition. This triple combination has been explored for use in advanced or metastatic cancers where EGFR and MET pathways are implicated—most notably colorectal cancer (for cetuximab + irinotecan) and hepatocellular carcinoma or non-small cell lung cancer (for tivantinib). However, there are no major published clinical trials specifically evaluating all three drugs together as a single regimen; each component has established roles individually or in dual combinations within oncology[1][2][3][4][5][6][7].

02

Targets

EGFR (Epidermal growth factor receptor)MET (Mesenchymal-epithelial transition factor receptor)TOP1 (DNA Topoisomerase I)

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