Drug intelligence / Profile preview

goserelin + bicalutamide + dutasteride

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

Overview

Goserelin + bicalutamide + dutasteride is a combination therapy used primarily in the treatment of advanced or metastatic prostate cancer. Goserelin is a gonadotropin-releasing hormone (GnRH) agonist that suppresses testicular androgen production by downregulating pituitary luteinizing hormone secretion. Bicalutamide is a non-steroidal antiandrogen that selectively antagonizes the androgen receptor, blocking the action of androgens like testosterone and dihydrotestosterone (DHT) at their receptor sites[6][1]. Dutasteride is a dual 5α-reductase inhibitor that blocks the conversion of testosterone to DHT, thereby reducing intraprostatic DHT levels and further suppressing androgenic stimulation of prostate tissue[8]. The combination aims to achieve maximal androgen blockade by targeting multiple points in the androgen axis—suppressing production, blocking receptor binding, and inhibiting local conversion to more potent androgens. This regimen has been studied for its ability to delay disease progression, improve immune function, reduce tumor volume, relieve symptoms such as pain, and potentially overcome resistance seen with standard combined androgen blockade therapies[2][1][8].

02

Targets

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

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