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Bicalutamide + anastrozole is a **combination therapy** of two oral small-molecule drugs: bicalutamide, a non-steroidal anti-androgen, and anastrozole, a non-steroidal aromatase inhibitor. This drug combination has been primarily investigated for **gonadotropin-independent (peripheral) precocious puberty in boys with testotoxicosis (familial male-limited precocious puberty)**, a rare disorder caused by mutations in the luteinizing hormone receptor leading to excess androgen production. **Bicalutamide** competitively antagonizes androgen receptors, reducing the effects of dihydrotestosterone (DHT) and testosterone, thereby suppressing virilization and secondary sexual development. **Anastrozole** inhibits the aromatase enzyme, blocking the conversion of anrogens to estrogens, thus lowering estrogen levels and preventing bone age acceleration and early epiphyseal closure[2][1][3][4]. This combination is used off-label and has been studied in clinical trials (not approved for any indication) in pediatric male patients.
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