Drug intelligence / Profile preview

cilengitide + cetuximab + 5-fluorouracil + cisplatin

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

Overview

This is a **combination regimen** comprising **cilengitide** (a cyclic RGD pentapeptide integrin αvβ3/αvβ5 inhibitor), **cetuximab** (an epidermal growth factor receptor [EGFR] monoclonal antibody), **5-fluorouracil** (a pyrimidine antimetabolite), and **cisplatin** (a platinum-based DNA-damaging agent). This combination has been evaluated in clinical studies as a first-line therapy for advanced non-small-cell lung cancer (NSCLC), particularly in patients with high EGFR expression, and potentially other solid tumors. Cilengitide inhibits tumor angiogenesis and cell adhesion by blocking integrins αvβ3 and αvβ5, thus impeding tumor growth and metastasis; cetuximab blocks EGFR, inhibiting proliferation and inducing apoptosis; 5-fluorouracil disrupts DNA synthesis; and cisplatin induces DNA cross-linking, leading to apoptosis. The combination aims for synergistic anti-tumor effects by targeting complementary pathways in cancer biology[1][2][5][6].

02

Targets

TS (Thymidylate synthase)αVβ3 (Integrin αVβ3)ITGA5:ITGB1 (Integrin α5β1)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)αVβ5 (Integrin αVβ5)

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