Drug intelligence / Profile preview

exemestane + bicalutamide

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

Overview

Exemestane + bicalutamide is a combination of two small molecule drugs, each with distinct mechanisms of action targeting hormone-dependent cancers. Exemestane is an aromatase inhibitor that irreversibly blocks the enzyme aromatase, leading to decreased estrogen production. It is primarily used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. Bicalutamide is a nonsteroidal antiandrogen that acts as an antagonist at androgen receptors, blocking the effects of androgens such as testosterone and dihydrotestosterone; it is mainly indicated for prostate cancer therapy, often in combination with other agents or surgical castration[1][5][7]. The rationale for combining these agents would be to simultaneously suppress both estrogenic and androgenic hormonal pathways, potentially relevant in certain hormone-driven malignancies or research settings.

02

Targets

CYP19A1 (Aromatase)AR (Adrenergic receptors)

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