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Histrelin Acetate is the acetate salt form of histrelin, a long-acting, synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) with potential anti-tumor activity. Upon administration, histrelin binds to and activates GnRH receptors; prolonged administration results in pituitary GnRH receptor desensitization and inhibition of follicle stimulating hormone (FSH) and luteinizing hormone (LH) secretion, leading to a significant decline in testosterone production in males and may inhibit androgen receptor-positive tumor progression; in females, prolonged administration results in decreased estradiol production.
The once-yearly histrelin implant maintained testosterone suppression for repeated treatment cycles and was generally well tolerated. The histrelin implant provides a clinically attractive option for long-term androgen deprivation therapy in patients with advanced prostate cancer seeking fewer office visits and repeated injections.
Shore, N., Cookson, M. S., & Gittelman, M. C. (2012). Long‐term efficacy and tolerability of once‐yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU international, 109(2), 226-232.
The LHRH agonist histrelin acetate is the only available sustained-release hydrogel implant for once-yearly administration. The once-yearly implant allows patients to receive fewer cycles of implanting and replanting to maintain continuous ADT therapy. The histrelin acetate implant is 3.5 cm long, is 3 mm in diameter, and is administered subcutaneously into the inner aspect of the upper arm or abdomen. The inner aspect of the upper arm can clinically be difficult for the surgeon as it is a mobile insertion site and difficult for elderly patients limited by strength/arthritis to maintain the necessary abducted and extended arm position. Thus, the arm compared to the abdomen site is more difficult for surgeon and is less tolerated by patients.
Woolen, S., Holzmeyer, C., Nesbitt, E., & Siami, P. F. (2014). Long-term efficacy and tolerability of abdominal once-yearly histrelin acetate subcutaneous implants in patients with advanced prostate cancer. Prostate cancer, 2014.