Goldstein Rebecca L, Goyos Ana, Li Chi-Ming, Deegen Petra, Bogner Pamela, Sternjak Alexander, Thomas Oliver, Klinger Matthias, Wahl Joachim, Friedrich Matthias, Rattel Benno, Lamas Edwin, Min Xiaoshan, Sudom Athena, Farshbaf Mozhgan, Coxon Angela, Balazs Mercedesz, Arvedson Tara
Amgen Research, Amgen Inc., South San Francisco, CA.
Amgen Research (Munich) GmbH, Munich, Germany; and.
Blood Adv. 2020 Sep 8;4(17):4180-4194. doi: 10.1182/bloodadvances.2020002565.
Multiple myeloma (MM) is a hematologic malignancy that is characterized by the accumulation of abnormal plasma cells (PCs) in the bone marrow (BM). Patient outcome may be improved with BiTE (bispecific T-cell engager) molecules, which redirect T cells to lyse tumor cells. B-cell maturation antigen (BCMA) supports PC survival and is highly expressed on MM cells. A half-life extended anti-BCMA BiTE molecule (AMG 701) induced selective cytotoxicity against BCMA-expressing MM cells (average half-maximal effective concentration, 18.8 ± 14.8 pM), T-cell activation, and cytokine release in vitro. In a subcutaneous mouse xenograft model, at all doses tested, AMG 701 completely inhibited tumor formation (P < .001), as well as inhibited growth of established tumors (P ≤ .001) and extended survival in an orthotopic MM model (P ≤ .01). To evaluate AMG 701 bioactivity in cynomolgus monkeys, a PC surface phenotype and specific genes were defined to enable a quantitative digital droplet polymerase chain reaction assay (sensitivity, 0.1%). Dose-dependent pharmacokinetic and pharmacodynamic behavior was observed, with depletion of PC-specific genes reaching 93% in blood and 85% in BM. Combination with a programmed cell death protein 1 (PD-1)-blocking antibody significantly increased AMG 701 potency in vitro. A model of AMG 701 binding to BCMA and CD3 indicates that the distance between the T-cell and target cell membranes (ie, the immunological synapse) is similar to that of the major histocompatibility complex class I molecule binding to a T-cell receptor and suggests that the synapse would not be disrupted by the half-life extending Fc domain. These data support the clinical development of AMG 701.
多发性骨髓瘤(MM)是一种血液系统恶性肿瘤,其特征是骨髓(BM)中异常浆细胞(PCs)的积累。双特异性T细胞衔接器(BiTE)分子可使T细胞重新定向裂解肿瘤细胞,从而改善患者预后。B细胞成熟抗原(BCMA)支持PC存活,并在MM细胞上高表达。一种半衰期延长的抗BCMA BiTE分子(AMG 701)在体外诱导了对表达BCMA的MM细胞的选择性细胞毒性(平均半数最大有效浓度,18.8±14.8 pM)、T细胞活化和细胞因子释放。在皮下小鼠异种移植模型中,在所有测试剂量下,AMG 701完全抑制肿瘤形成(P<.001),并抑制已建立肿瘤的生长(P≤.001),在原位MM模型中延长生存期(P≤.01)。为了评估AMG 701在食蟹猴中的生物活性,定义了PC表面表型和特定基因,以进行定量数字液滴聚合酶链反应分析(灵敏度,0.1%)。观察到剂量依赖性药代动力学和药效学行为,PC特异性基因的耗竭在血液中达到93%,在骨髓中达到85%。与程序性细胞死亡蛋白1(PD-1)阻断抗体联合使用可在体外显著提高AMG 701的效力。AMG 701与BCMA和CD3结合的模型表明,T细胞与靶细胞膜之间的距离(即免疫突触)与主要组织相容性复合体I类分子与T细胞受体结合的距离相似,并表明该突触不会被半衰期延长的Fc结构域破坏。这些数据支持AMG 701的临床开发。