The Sound of Evolution
Histrelin
Mechanism of action:
Histrelin is a gonadotropin-releasing hormone analogue and belongs to the class of synthetic peptide analogues. Initially, histrelin continuously stimulates gonadotropin-releasing hormone receptors (GnRH receptors) in the anterior pituitary, causing a transient increase in luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which temporarily raises sex hormone levels (testosterone or estrogen). With continued administration, prolonged stimulation causes desensitization and downregulation of GnRH receptors, markedly weakening the pituitary response to gonadotropin-releasing hormone. As a result, LH and FSH levels begin to decline, leading to reduced sex hormone production.
Reference(s):
1. Lewis KA et al. (2009). Experience with the once-yearly histrelin (GnRHa) subcutaneous implant in the treatment of central precocious puberty. Drug Des Devel Ther.
2. Shore N et al. (2012). Long-term efficacy and tolerability of once-yearly histrelin acetate subcutaneous implant in patients with advanced prostate cancer. BJU Int.
3. Djavan B et al. (2010). Analysis of testosterone suppression in men receiving histrelin, a novel GnRH agonist for the treatment of prostate cancer. Can J Urol.