Histrelin (Vantas)
Overview
Histrelin is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH) that functions as a GnRH agonist. The peptide is administered via a subcutaneous implant that delivers continuous drug release over 12 months, inducing initial gonadotropin stimulation followed by sustained receptor downregulation and suppression of testicular androgen production. It is indicated for palliative treatment of advanced prostate cancer and management of central precocious puberty. Amino acid modifications at positions 6 and 10 enhance receptor binding and resistance to peptidase degradation.
Key Research Findings
Histrelin acetate received FDA approval in 2004 (Vantas implant for prostate cancer) and 2007 (Supprelin LA for central precocious puberty). Pivotal phase 3 trials demonstrated that over 90% of patients achieved and maintained castrate testosterone levels throughout the 52-week implant duration. The implant delivery system offers the advantage of eliminating the need for monthly or quarterly injections, improving adherence in long-term androgen deprivation therapy.
Subcutaneous implant
FDA Approved
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