新型钙调神经磷酸酶抑制剂——伏环孢素

A novel calcineurin inhibitor:voclosporin

伏环孢素是一种新型钙调磷酸酶抑制剂,2021年1月22日美国FDA批准上市用于治疗成人狼疮性肾炎。伏环孢素经口服给药,与其他钙调磷酸酶抑制剂相比,体内代谢过程个体差异小,无须进行治疗监测。伏环孢素主要经过CYP3A4代谢,合用药物时需注意可能发生的药物相互作用。临床研究显示,在霉酚酸盐和糖皮质激素治疗基础上联合伏环孢素可以更快获得肾脏完全缓解,且缓解比例更高。但该药物可能降低估算肾小球滤过率,增加高血压发生风险,需密切监测患者血压,定期复查肾功能。本文就伏环孢素的药理作用、药动学、临床评价、安全性、用法用量等进行综述,以期为临床合理用药提供参考。

Voclosporin,a newly developed calcineurin inhibitor,received approval from the FDA on January 22,2021,for its use in treating adult lupus nephritis.Voclosporin is administered orally and exhibits minimal interindividual variability in its metabolic process,compared with other calmodulin phosphatase inhibitors,thus obviating the need for therapeutic monitoring.Voclosporin is predominantly metabolized by CYP3A4 and potential drug interactions should be considered when co-administering with other medications.In comparison to the placebo group,voclosporin treatment group demonstrated a higher proportion of patients achieving complete renal remission in a shorter duration.However,this drug may cause a decrease in estimated glomerular filtration rate and increase the risk of hypertension.Therefore,it is necessary to closely monitor patients'blood pressure and regularly assess renal function.This article provides a comprehensive review of the pharmacological effects,pharmacokinetics,clinical evaluation,safety,and dosage of voclosporin,to offer a reference for its rational clinical use.