Goserelin (DB00014): A Comprehensive Monograph on its Pharmacology, Clinical Efficacy, and Safety Profile

Section 1: Introduction and Drug Identification

Executive Summary

Goserelin is a synthetic peptide therapeutic agent that functions as a potent agonist of the gonadotropin-releasing hormone (GnRH) receptor. Marketed principally under the brand name Zoladex®, it has become a cornerstone therapy in the management of hormone-sensitive malignancies, most notably prostate cancer and breast cancer, as well as several benign gynecological disorders such as endometriosis.[1] The therapeutic strategy of goserelin is predicated on its ability to induce a profound, sustained, and reversible suppression of sex hormone production. Through continuous, non-pulsatile stimulation of pituitary GnRH receptors, goserelin paradoxically leads to receptor downregulation and desensitization, effectively halting the downstream production of testosterone in males and estrogen in females. This induction of a "medical castration" state deprives hormone-dependent tumors of their essential growth signals. The clinical viability of this mechanism is fundamentally enabled by its formulation as a long-acting, biodegradable subcutaneous depot implant, which overcomes the inherent limitations of its peptide structure, namely oral inactivity and a short biological half-life. First patented in 1976 and approved for medical use in 1987, goserelin's established efficacy and safety profile have earned it a place on the World Health Organization's List of Essential Medicines.[1]

Consolidated Identification Data

Goserelin is a well-characterized synthetic decapeptide. While sometimes broadly categorized as a small molecule, its peptide nature is its defining chemical and pharmacological characteristic.[1] The following table provides a consolidated summary of its key identifiers.

Table 1: Goserelin Drug Identification and Chemical Properties