Drug intelligence / Profile preview

gefitinib + bicalutamide

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Gefitinib + bicalutamide is an investigational combination therapy comprising two small-molecule drugs: gefitinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and bicalutamide, a nonsteroidal antiandrogen and androgen receptor antagonist. Gefitinib inhibits EGFR-mediated signaling, thereby blocking pathways involved in cell proliferation and survival. Bicalutamide binds androgen receptors, preventing androgen-driven tumor growth primarily in prostate tissue. The combination is being studied for its additive or synergistic antitumor effects, particularly in prostate cancer, by concurrently inhibiting AR- and EGFR-mediated growth pathways. Dual blockade is of interest for delaying the onset of androgen independence in prostate cancer, where monotherapy with either agent may be insufficient[1][3].

02

Targets

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

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