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cetuximab + cilengitide + cisplatin + gemcitabine + vinorelbine

Development stage
Preclinical
Lead developer
Merck KGaA
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Peptides, Small Molecules
Administration
Intravenous
01

Overview

This is a combination regimen consisting of five distinct anticancer agents: - **Cetuximab** is a chimeric monoclonal antibody targeting the epidermal growth factor receptor (EGFR), inhibiting downstream signaling pathways involved in cell proliferation and survival. - **Cilengitide** is a cyclic RGD pentapeptide that selectively inhibits integrins αvβ3 and αvβ5, disrupting angiogenesis and tumor cell adhesion. - **Cisplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks, leading to apoptosis in rapidly dividing cells. - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporation into DNA strands, causing chain termination and apoptosis. - **Vinorelbine** is a semi-synthetic vinca alkaloid that disrupts microtubule formation during mitosis, arresting cell division. This combination has been explored for its potential synergistic antitumor effects in various solid tumors. The triplet of gemcitabine, vinorelbine, and cisplatin has demonstrated efficacy in advanced non-small cell lung cancer (NSCLC) with manageable toxicity profiles[1][4][5]. Cetuximab adds targeted EGFR inhibition; cilengitide contributes antiangiogenic activity. The full five-drug combination represents an investigational regimen not approved as a standard therapy.

02

Targets

αVβ5 (Integrin αVβ5)αVβ3 (Integrin αVβ3)DNA polymerase familyDNATUBB (Tubulin (alpha and beta subunits))EGFR T790M (Epidermal growth factor receptor T790M mutant)

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