Drug intelligence / Profile preview

enzalutamide + anastrozole

Development stage
Phase 1
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Enzalutamide + anastrozole is a **combination drug** consisting of enzalutamide, a nonsteroidal antiandrogen that acts as a selective antagonist of the androgen receptor, and anastrozole, an aromatase inhibitor that blocks estrogen biosynthesis. The combination is being investigated, especially in breast cancer and prostate cancer settings, for synergistic effects: enzalutamide inhibits androgen signaling, while anastrozole suppresses estrogen synthesis. This is particularly relevant since certain hormone receptor-positive breast cancers express both androgen and estrogen receptors, and the combination may help overcome resistance to single-agent hormonal therapies by dual pathway blockade. However, strong drug-drug pharmacokinetic interactions have been observed; enzalutamide induces CYP3A4 and can decrease anastrozole plasma exposure by approximately 90%, potentially compromising its efficacy[3][5]. The combination has been explored primarily in early-phase breast cancer clinical trials.

Other names
enzalutamide plus anastrozoleenzalutamide and anastrozoleenzalutamide-anastrozole combination
02

Targets

AR (Adrenergic receptors)CYP19A1 (Aromatase)

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