The Sound of Evolution
Histrelin
組氨瑞林
Mechanism of action:
Histrelin 是一種促性腺激素釋放激素（gonadotropin-releasing hormone）的類似物，屬於合成胜肽類（synthetic peptide analogue）。在初期，histrelin 會持續刺激腦下垂體前葉的促性腺激素釋放激素受體（GnRH receptor），使黃體成長激素（LH）與濾泡刺激素（FSH）短暫上升，造成性荷爾蒙（睪酮或雌激素）暫時增加。隨著持續提供，促性腺激素釋放激素受體因長期刺激而發生去敏感化與數量下降，腦下垂體對促性腺激素釋放激素反應明顯減弱，使黃體成長激素和濾泡刺激素開始減少，進而降低性荷爾蒙產量。
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.