Drug intelligence / Profile preview

ibrutinib + cetuximab

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

Ibrutinib + cetuximab is a combination therapy of two anticancer agents: ibrutinib, an oral small molecule inhibitor of Bruton's tyrosine kinase (BTK), and cetuximab, a monoclonal antibody that targets the epidermal growth factor receptor (EGFR). This combination is being investigated, particularly in phase 1b/2 trials, for the treatment of advanced gastrointestinal and genitourinary malignancies, most notably metastatic colorectal cancer (CRC) and other advanced solid tumors that have failed multiple lines of therapy. Both agents have independent antineoplastic effects and overlapping toxicity (notably, cutaneous toxicity/rash), possibly due to both directly or indirectly affecting the EGFR pathway. Ibrutinib is developed by Pharmacyclics and Janssen; cetuximab is developed by ImClone and Merck KGaA. No unique brand or code names exist for the combination. This regimen is not currently approved for any indication.

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Targets

BTK (Bruton tyrosine kinase)EPHA2 (Ephrin type-A receptor 2)ITK (Interleukin 2-inducible T-cell kinase)EGFR (Epidermal growth factor receptor)

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