Drug intelligence / Profile preview

prexasertib + cetuximab

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

Overview

Prexasertib + cetuximab is a **combination therapy** evaluated primarily in the treatment of advanced or metastatic cancers, including head and neck squamous cell carcinoma (HNSCC). Prexasertib is a small molecule inhibitor of checkpoint kinase 1 (CHK1), which disrupts DNA damage response and cell cycle regulation. Cetuximab is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR), inhibiting EGFR-mediated signaling involved in tumor proliferation and survival. The combination aims to enhance anti-tumor efficacy by simultaneously inhibiting DNA repair (through CHK1) and growth signaling (through EGFR). Clinical studies have shown that this combination can be administered together, with hematologic toxicity being the most common dose-limiting effect. Both drugs are administered intravenously, and the combination has shown proof-of-concept in phase 1b studies with dose-limiting toxicities requiring careful dose management[1][2][3][5].

02

Targets

CHEK2 (Checkpoint kinase 2)CHEK1 (Checkpoint kinase 1)EGFR (Epidermal growth factor receptor)

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