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non-steroidal antiandrogens + luteinizing hormone-releasing hormone agonists

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

Non-steroidal antiandrogens + luteinizing hormone-releasing hormone (LHRH) agonists is a combination pharmaceutical regimen primarily used as hormonal therapy for prostate cancer. Non-steroidal antiandrogens (e.g., bicalutamide, flutamide, nilutamide, enzalutamide) act by competitively inhibiting the androgen receptor in prostate tissue, blocking the effects of testosterone and dihydrotestosterone. LHRH agonists (e.g., leuprolide, goserelin, triptorelin, buserelin) suppress testicular androgen production by downregulating pituitary luteinizing hormone release through continuous stimulation, leading to medical castration. The combination reduces testosterone from both testicular and adrenal sources, preventing androgen-mediated tumor progression and counteracting testosterone surge ("flare") seen with LHRH agonist monotherapy. This combined approach—often called combined androgen blockade—has demonstrated improved treatment efficacy over monotherapy in several clinical contexts, particularly advanced and metastatic prostate cancer[1][3][5][6].

Other names
combined androgen blockadenon-steroidal antiandrogen + LHRH agonist combinationnon-steroidal antiandrogen + gonadotropin-releasing hormone agonist
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)

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