Drug intelligence / Profile preview

gefitinib + tremelimumab

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
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Overview

Gefitinib + tremelimumab is a combination therapy that pairs two distinct mechanisms of action for the treatment of non-small cell lung cancer (NSCLC). Gefitinib is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase that blocks ATP binding to EGFR, inhibiting downstream signaling pathways involved in cancer cell proliferation and survival. Tremelimumab is a human monoclonal antibody that targets cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), blocking its activity and contributing to T-cell activation, thereby enhancing immune response against cancer cells. This combination was specifically studied in EGFR-mutant NSCLC patients who had progressed after first-generation EGFR-TKI therapy.

02

Targets

CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)EGFR (Epidermal growth factor receptor)

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