Drug intelligence / Profile preview

gefitinib + trastuzumab

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

Overview

Gefitinib + trastuzumab is an investigational combination therapy consisting of two targeted agents used primarily in oncology research. Gefitinib is a small molecule tyrosine kinase inhibitor that selectively inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to its ATP-binding site, thereby blocking downstream signaling pathways involved in cell proliferation and survival. Trastuzumab is a monoclonal antibody that binds to the extracellular domain of the human epidermal growth factor receptor 2 (HER2/ErbB-2), inhibiting HER2-mediated signaling and inducing antibody-dependent cellular cytotoxicity. The rationale for combining these agents lies in their complementary mechanisms targeting both EGFR and HER2 pathways, which are often co-expressed or dysregulated in certain cancers such as HER2-positive breast cancer and hormone-refractory prostate cancer. Clinical studies have evaluated this combination for safety and efficacy; while some antitumor activity has been observed, toxicity (notably gastrointestinal side effects) can be significant at higher doses[6][1]. This combination remains investigational without regulatory approval as a fixed regimen.

Other names
gefitinib-trastuzumab combination
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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