Drug intelligence / Profile preview

goserelin + bicalutamide + dutasteride + ketoconazole

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Subcutaneous, Oral
01

Overview

This is a four-drug combination therapy consisting of goserelin, bicalutamide, dutasteride, and ketoconazole. It is used experimentally for the treatment of prostate cancer, particularly to achieve maximal androgen pathway suppression prior to prostatectomy in patients with localized or high-risk disease. - **Goserelin** is a luteinizing hormone-releasing hormone (LHRH) agonist that suppresses testicular androgen production by downregulating pituitary gonadotropin secretion. - **Bicalutamide** is a non-steroidal antiandrogen that blocks the action of androgens at the androgen receptor. - **Dutasteride** inhibits both type 1 and type 2 isoforms of 5-alpha-reductase, reducing conversion of testosterone to dihydrotestosterone (DHT). - **Ketoconazole**, an antifungal agent at higher doses, inhibits steroidogenesis by blocking cytochrome P450 enzymes involved in adrenal and testicular androgen synthesis. The combination aims to lower intratumoral DHT levels beyond what standard castration achieves and more completely suppresses androgen receptor signaling in prostate tissue[1][6]. This regimen has been studied preoperatively before radical prostatectomy for its ability to reduce tumor volume and AR-regulated gene expression[1][6].

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)SRD5A2 (Steroid 5-alpha-reductase type II)AR (Adrenergic receptors)SRD5A1 (Steroid 5-alpha-reductase type 1)

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