Frieri Marianne, Heuser William, Bliss Joshua
Department of Medicine, Nassau University Medical Center, St Johns University, New York, USA.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St Johns University, New York, USA.
J Pharmacol Pharmacother. 2015 Apr-Jun;6(2):71-6. doi: 10.4103/0976-500X.155482.
Recently introduced into the market, belimumab (Benlysta) is a monoclonal antibody that has potential clinically efficacious applications for the treatment of lupus nephritis. Lupus nephritis is a major complication of systemic lupus erythematosus (SLE) that can lead to significant illness or even death without proper intervention and treatment. With vast implications through a novel mechanism, belimumab offers a new standard of treatment for physicians in the complications associated with SLE, specifically lupus nephritis. By targeting B cell signaling and maturation, belimumab is able to mitigate the underlying pathological complications surrounding SLE. Phase 3 clinical trials with belimumab have depicted clinically efficacious applications, suggesting belimumab as a revolutionary breakthrough in the treatment armamentarium for practicing clinicians. This article explains the precise mechanism of action of belimumab on the soluble protein BlyS that plays a major role in the pathogenesis of lupus nephritis. In addition, the extensive pharmacokinetics and clinical implications are exemplified in this review with belimumab's comparison with standard therapeutic guidelines for the treatment of lupus nephritis.
贝利尤单抗(Benlysta)最近被引入市场,它是一种单克隆抗体,在治疗狼疮性肾炎方面具有潜在的临床有效应用。狼疮性肾炎是系统性红斑狼疮(SLE)的一种主要并发症,若不进行适当干预和治疗,可能导致严重疾病甚至死亡。通过一种新机制产生广泛影响,贝利尤单抗为治疗与SLE相关并发症(特别是狼疮性肾炎)的医生提供了一种新的治疗标准。通过靶向B细胞信号传导和成熟,贝利尤单抗能够减轻围绕SLE的潜在病理并发症。贝利尤单抗的3期临床试验已显示出临床有效应用,表明贝利尤单抗是执业临床医生治疗手段中的一项革命性突破。本文解释了贝利尤单抗对在狼疮性肾炎发病机制中起主要作用的可溶性蛋白BlyS的精确作用机制。此外,本综述通过将贝利尤单抗与狼疮性肾炎治疗的标准治疗指南进行比较,举例说明了其广泛的药代动力学和临床意义。