Poulakos Mara N, Cargill Shawna M, Waineo Melissa F, Wolford Allen L
Lloyd L. Gregory School of Pharmacy, Palm Beach Atlantic University, West Palm Beach, FL.
University of Utah, Salt Lake City, UT.
Am J Health Syst Pharm. 2017 Jul 1;74(13):963-969. doi: 10.2146/ajhp160291.
Published data on the pharmacology, pharmacokinetics and pharmacodynamics, and clinical efficacy and safety of the interleukin-5 antagonist mepolizumab are reviewed.
Asthma of the eosinophilic phenotype is characterized by persistent eosinophilic airway inflammation promoted primarily by T-helper type 2 cytokines, the key regulator of eosinophils. Patients with severe eosinophilic asthma are burdened by the need to administer high doses of corticosteroids to help manage their symptoms. In November 2015, mepolizumab (Nucala, GlaxoSmithKline) gained U.S. marketing approval for use as an add-on maintenance treatment for severe eosinophilic asthma in patients 12 years of age or older, making it the first personalized targeted therapy for this population. Efficacy results from clinical trials provided evidence of the corticosteroid-sparing effects of mepolizumab and its ability to reduce both blood and sputum eosinophil counts. Safety data from several Phase II or III studies involving a total of more than 1,300 patients indicated that mepolizumab was generally well tolerated, and types and rates of adverse events in mepolizumab recipients were comparable to those reported with placebo use; the only mepolizumab-associated serious adverse drug events were asthma exacerbations in 2 patients. The recommended dosage of mepolizumab is 100 mg administrated via subcutaneous injection every 4 weeks.
Mepolizumab is a safe and efficacious novel add-on therapy for a small subgroup of patients with severe eosinophilic asthma whose asthma is not adequately controlled by standard regimens for asthma treatment.
对白细胞介素-5拮抗剂美泊利珠单抗的药理学、药代动力学和药效学以及临床疗效和安全性的已发表数据进行综述。
嗜酸性粒细胞表型哮喘的特征是主要由2型辅助性T细胞细胞因子（嗜酸性粒细胞的关键调节因子）促进的持续性嗜酸性粒细胞气道炎症。重度嗜酸性粒细胞哮喘患者因需要使用高剂量皮质类固醇来控制症状而负担沉重。2015年11月，美泊利珠单抗（Nucala，葛兰素史克公司）获得美国市场批准，用作12岁及以上重度嗜酸性粒细胞哮喘患者的附加维持治疗药物，使其成为该人群的首个个性化靶向治疗药物。临床试验的疗效结果证明了美泊利珠单抗具有节省皮质类固醇的作用及其降低血液和痰液嗜酸性粒细胞计数的能力。来自几项总共涉及1300多名患者的II期或III期研究的安全性数据表明，美泊利珠单抗总体耐受性良好，接受美泊利珠单抗治疗的患者不良事件的类型和发生率与使用安慰剂报告的情况相当；仅2例与美泊利珠单抗相关的严重药物不良事件为哮喘加重。美泊利珠单抗的推荐剂量为每4周皮下注射100mg。
对于一小部分重度嗜酸性粒细胞哮喘患者，其哮喘不能通过标准哮喘治疗方案得到充分控制，美泊利珠单抗是一种安全有效的新型附加治疗药物。
