Leuprorelin (Leuprolide) is a gonadotropin-releasing hormone (GnRH) analog that acts as an agonist at the pituitary GnRH receptor[1]. Leuprorelin is primarily used to treat various sex hormone-related diseases, including advanced prostate cancer, endometriosis, and precocious puberty[2]. Continuous administration of Leuprorelin can induce pituitary desensitization and/or receptor downregulation, thereby suppressing the levels of gonadotropins and sex hormones in the blood circulation, leading to hypogonadism[3, 4]. Leuprorelin is more stable than natural GnRH and has a stronger receptor affinity[5].
References:
[1] Casati L, Ciceri S, Maggi R, et al. Physiological and pharmacological overview of the gonadotropin releasing hormone[J]. Biochemical pharmacology, 2023, 212: 115553.
[2] Plosker G L, Brogden R N. Leuprorelin: a review of its pharmacology and therapeutic use in prostatic cancer, endometriosis and other sex hormone-related disorders[J]. Drugs, 1994, 48(6): 930-967.
[3] Wu H M, Chang H M, Leung P C K. Gonadotropin-releasing hormone analogs: Mechanisms of action and clinical applications in female reproduction[J]. Frontiers in neuroendocrinology, 2021, 60: 100876.
[4] Wuttke W, Jarry H, Feleder C, et al. The neurochemistry of the GnRH pulse generator[J]. Acta neurobiologiae experimentalis, 1996, 56(3): 707-713.
[5] Periti P, Mazzei T, Mini E. Clinical pharmacokinetics of depot leuprorelin[J]. Clinical pharmacokinetics, 2002, 41: 485-504.
Leuprorelin (Leuprolide)是一种促性腺激素释放激素（GnRH）类似物 ，在垂体GnRH受体中起激动剂的作用[1]。Leuprorelin主要用于治疗各种性激素相关疾病，包括晚期前列腺癌、子宫内膜异位症和性早熟[2]。Leuprorelin持续给药可诱导垂体脱敏和/或受体下调，从而抑制血液循环中的促性腺激素和性激素水平，导致性腺功能低下[3, 4]。Leuprorelin比天然GnRH更稳定，具有更强的受体亲和力[5]。