Shukla Alpana P, Kumar Rekha B, Aronne Louis J
a Weill Cornell Medical College, Comprehensive Weight Control Center, Division of Endocrinology, Diabetes & Metabolism , NY, USA
Expert Opin Pharmacother. 2015;16(16):2531-8. doi: 10.1517/14656566.2015.1096345. Epub 2015 Oct 15.
Obesity is a major health priority necessitating safe and effective strategies to address the obesity epidemic. Lorcaserin is a serotonergic agonist specific to the 5HT- 2C receptor approved for chronic management of obesity in patients with a BMI ≥ 30 kg/m(2) or a BMI ≥ 27 kg/m(2) with comorbidities related to obesity.
In this paper, the pharmacodynamic and pharmacokinetic properties of lorcaserin are reviewed followed by a discussion of efficacy and safety data from major clinical trials.
Lorcaserin is a unique highly selective serotonergic agonist designed to mitigate the risks associated with previous agents in this class. At therapeutic doses, it is well tolerated and produces modest but clinically meaningful weight loss with significant improvement in cardiometabolic parameters. Therapeutic efficacy should be assessed at 12 weeks (≥ 5% weight loss) to identify responders who will derive maximum weight loss and metabolic benefit from long-term therapy. The results of the ongoing cardiovascular outcomes trial (CAMELLIA TIMI 61) will determine the role of lorcaserin in primary prevention of diabetes in overweight/obese individuals and its use in the high-risk population of patients with established cardiovascular disease or multiple cardiovascular risk factors.
肥胖是一个重大的健康问题，需要采取安全有效的策略来应对肥胖流行。氯卡色林是一种特异性作用于5HT-2C受体的血清素能激动剂，被批准用于体重指数（BMI）≥30 kg/m²或BMI≥27 kg/m²且伴有肥胖相关合并症患者的肥胖慢性管理。
本文回顾了氯卡色林的药效学和药代动力学特性，随后讨论了主要临床试验的疗效和安全性数据。
氯卡色林是一种独特的高选择性血清素能激动剂，旨在降低与该类先前药物相关的风险。在治疗剂量下，它耐受性良好，能产生适度但具有临床意义的体重减轻，并使心脏代谢参数有显著改善。应在12周时评估治疗效果（体重减轻≥5%），以确定能从长期治疗中获得最大体重减轻和代谢益处的反应者。正在进行的心血管结局试验（CAMELLIA TIMI 61）的结果将确定氯卡色林在超重/肥胖个体糖尿病一级预防中的作用，以及其在已确诊心血管疾病或有多种心血管危险因素的高危患者群体中的应用。
