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依洛珠单抗的临床药理学。

The Clinical Pharmacology of Elotuzumab.

机构信息

Clinical Pharmacology and Pharmacometrics, Bristol-Myers Squibb, 3551 Lawrenceville Road, Princeton, NJ, 08540, USA.

出版信息

Clin Pharmacokinet. 2018 Mar;57(3):297-313. doi: 10.1007/s40262-017-0585-6.

Abstract

Novel treatment options are needed to improve long-term outcomes for patients with multiple myeloma (MM). In this article, we comprehensively review the clinical pharmacology of elotuzumab, a first-in-class monoclonal anti-SLAMF7 antibody approved in combination with lenalidomide and dexamethasone (ELd) for the treatment of patients with MM and one to three prior therapies. Elotuzumab has a dual mechanism of action to specifically kill myeloma cells: binding SLAMF7 on myeloma cells facilitates natural killer (NK) cell-mediated antibody-dependent cellular cytotoxicity (ADCC), and direct engagement of SLAMF7 on NK cells further enhances NK cell activity. Elotuzumab administration causes transient elevations of selected cytokines (tumor necrosis factor-α, interferon-γ-induced protein-10 and monocyte chemoattractant protein-1). The temporary nature of these elevations (greatest after the first dose, with a trend to return to baseline by day 7) suggests a low likelihood of facilitating clinically meaningful drug-drug interactions. Elotuzumab exposure increases more than proportionally to dose and >80% SLAMF7 receptor occupancy is achieved with the approved elotuzumab 10 mg/kg regimen. Population pharmacokinetic data from 375 patients demonstrated weight-based dosing is appropriate for elotuzumab, and that ethnicity and hepatic/renal function have minimal effects on exposure. Exposure-response analysis of patients treated with ELd demonstrated that increased elotuzumab exposure does not elevate the risk of grade 3+ adverse events (AEs) or AEs leading to discontinuation/death. Elotuzumab antidrug antibodies occurred in 18.5% of patients treated with ELd or elotuzumab plus bortezomib and dexamethasone, but were generally transient and did not affect elotuzumab efficacy or safety. A monotherapy study indicated elotuzumab does not have clinically relevant effects on QT intervals.

摘要

需要新的治疗选择来改善多发性骨髓瘤(MM)患者的长期预后。本文全面综述了埃罗妥珠单抗的临床药理学,该药是一种首创的 SLAMF7 单克隆抗体,与来那度胺和地塞米松联合用于治疗接受过 1-3 线治疗的 MM 患者。埃罗妥珠单抗具有双重作用机制,可特异性杀伤骨髓瘤细胞:与骨髓瘤细胞上的 SLAMF7 结合促进自然杀伤(NK)细胞介导的抗体依赖性细胞毒性(ADCC),并直接与 NK 细胞上的 SLAMF7 结合进一步增强 NK 细胞活性。埃罗妥珠单抗给药会导致选定细胞因子(肿瘤坏死因子-α、干扰素-γ诱导蛋白-10 和单核细胞趋化蛋白-1)的短暂升高。这些升高的暂时性(首次剂量后最大,第 7 天有趋势回到基线)表明,促进有临床意义的药物相互作用的可能性较低。埃罗妥珠单抗暴露量与剂量不成比例地增加,并且批准的 10mg/kg 埃罗妥珠单抗方案可实现>80%的 SLAMF7 受体占有率。来自 375 名患者的群体药代动力学数据表明,埃罗妥珠单抗的剂量应基于体重,种族和肝/肾功能对暴露量的影响最小。ELd 治疗患者的暴露-反应分析表明,增加埃罗妥珠单抗暴露量不会增加 3 级及以上不良事件(AE)或导致停药/死亡的 AE 的风险。接受 ELd 或埃罗妥珠单抗联合硼替佐米和地塞米松治疗的患者中有 18.5%发生埃罗妥珠单抗抗药物抗体,但通常是短暂的,并不影响埃罗妥珠单抗的疗效或安全性。一项单药治疗研究表明,埃罗妥珠单抗对 QT 间期没有临床相关影响。

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