Buserelin (Suprefact)
Overview
Buserelin is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH) that acts as a potent GnRH agonist. It binds with high affinity to pituitary GnRH receptors, initially stimulating gonadotropin release before inducing receptor desensitization and downregulation, ultimately suppressing sex hormone production. The peptide is used primarily in the management of hormone-dependent prostate cancer and endometriosis. Structural modifications include substitution of glycine at position 6 with D-serine and replacement of the C-terminal glycine amide with an ethylamide group to enhance potency and duration of action.
Key Research Findings
Buserelin has been approved in multiple international markets, including Europe and Canada, since the 1980s for prostate cancer and assisted reproductive technology applications, though it is not FDA-approved in the United States. Clinical trials have demonstrated castration rates exceeding 85% in prostate cancer patients, with efficacy comparable to other GnRH agonists. It is available in multiple formulations including subcutaneous depot, intranasal, and subcutaneous injection forms to accommodate different clinical scenarios.
Subcutaneous injection, Intranasal
In Clinical Trials
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