Drug intelligence / Profile preview

leuprolide + bicalutamide + abiraterone

Development stage
Unknown
Lead developer
Peking Union Medical College
Modality
Peptides, Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

This combination therapy consists of leuprolide, bicalutamide, and abiraterone, and is currently being investigated in a Phase 2 umbrella trial led by Peking Union Medical College for the treatment of androgen receptor (AR)-positive salivary gland carcinoma. The regimen employs a triple androgen blockade strategy: leuprolide, a gonadotropin-releasing hormone (GnRH) receptor agonist, suppresses the production of luteinizing hormone to reduce testicular testosterone; bicalutamide acts as a competitive antagonist at the androgen receptor; and abiraterone (typically administered as abiraterone acetate) inhibits the CYP17A1 enzyme, thereby blocking androgen synthesis in the testes, adrenal glands, and the tumor microenvironment itself. This intensive androgen deprivation approach is intended to maximize the suppression of androgen-driven growth in salivary gland malignancies, such as salivary duct carcinoma, which frequently overexpress the androgen receptor.

Other names
leuprorelin + bicalutamide + abirateroneTAB regimentriple androgen blockade
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)CYP2C8 (Cytochrome P450 2C8)CYP2D6 (Cytochrome P450 2D6)CYP3A4 (Cytochrome P450 3A4)AR (Adrenergic receptors)

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