Onge Erin St, Phillips Bradley, Miller Lisa
Department of Pharmacotherapy and Translational Research, College of Pharmacy, University of Florida, Orlando, FL, USA.
J Pharm Technol. 2023 Dec;39(6):291-297. doi: 10.1177/87551225231198700. Epub 2023 Sep 16.
To review the safety, efficacy, and tolerability of fezolinetant for the treatment of vasomotor symptoms associated with menopause. A literature search was conducted through PubMed using the following search terms: fezolinetant, ES259564, SKYLIGHT, vasomotor symptoms, and menopause. Selected articles included those which described clinical studies of the pharmacology, pharmacokinetics, efficacy, safety, or tolerability of fezolinetant. Fezolinetant works by inhibiting neurokinin B from binding to its receptor in the hypothalamus, thereby decreasing the occurrence of vasomotor symptoms. Clinical trials have demonstrated fezolinetant is superior to placebo in decreasing the frequency and severity of vasomotor symptoms. Common adverse effects associated with the use of fezolinetant include headache and gastrointestinal disturbances, as well as elevations in liver transaminase levels. Clinical practice guidelines for the treatment of vasomotor symptoms associated with menopause recommend hormone therapy as the most effective treatment option. Risks associated with hormone use may limit the use of this option in some patients. Neurokinin B inhibitors, like fezolinetant, target the physiologic cause of vasomotor symptoms. With the approval of fezolinetant, as well as elinzanetant which is currently in phase 3 clinical trials, providers and patients have additional nonhormonal treatment options for vasomotor symptoms associated with menopause.
评估非唑奈坦治疗绝经相关血管舒缩症状的安全性、有效性和耐受性。通过PubMed进行文献检索,使用以下检索词:非唑奈坦、ES259564、SKYLIGHT、血管舒缩症状和绝经。入选的文章包括那些描述非唑奈坦药理学、药代动力学、有效性、安全性或耐受性的临床研究。非唑奈坦通过抑制神经激肽B在下丘脑与其受体结合发挥作用,从而减少血管舒缩症状的发生。临床试验表明,非唑奈坦在降低血管舒缩症状的频率和严重程度方面优于安慰剂。使用非唑奈坦常见的不良反应包括头痛、胃肠道不适以及肝转氨酶水平升高。绝经相关血管舒缩症状的临床实践指南推荐激素治疗作为最有效的治疗选择。激素使用相关的风险可能会限制该选项在某些患者中的应用。像非唑奈坦这样的神经激肽B抑制剂针对血管舒缩症状的生理原因。随着非唑奈坦的获批,以及目前处于3期临床试验的艾林扎奈坦,医疗服务提供者和患者对于绝经相关血管舒缩症状有了更多的非激素治疗选择。