Department of Hematology and Oncology, Nagoya City University Graduate School of Medical Sciences, 1, Kawasumi, Mizuho-cho, Mizuho-ku, Nagoya, Aichi, 467-8601, Japan.
Department of Hematology, National Hospital Organization Okayama Medical Center, Okayama, Japan.
Int J Hematol. 2021 Jun;113(6):797-806. doi: 10.1007/s12185-021-03096-9. Epub 2021 Feb 27.
PIM447, a pan-proviral integration site for Moloney leukemia (PIM) kinase inhibitor, has shown preclinical activity in multiple myeloma (MM). This phase I, open-label, multicenter, dose-escalation study aimed to determine the maximum tolerated dose (MTD) and recommended dose for expansion (RDE) of PIM447 in Japanese patients with relapsed and/or refractory (R/R) MM. The study included 13 patients (250 mg once daily (QD), [n = 7]; 300 mg QD, [n = 6]). The sole dose-limiting toxicity observed was grade 3 QTc prolongation in one patient from the 300 mg group, and the MTD and RDE was not determined. The most common suspected PIM447-related adverse events (AEs) included thrombocytopenia (76.9%), anemia (53.8%), and leukopenia (53.8%). All patients experienced at least one grade 3 or 4 AE, most frequently thrombocytopenia or leukopenia (61.5% each). The overall response rate was 15.4%, disease control rate 69.2%, clinical benefit rate 23.1%, and two patients had a partial response (one in each dose group). Two patients treated with 250 mg QD had a progression-free survival > 6 months. PIM447 250 mg or 300 mg QD was tolerated in Japanese patients with R/R MM. Further studies are required to evaluate clinical outcomes of PIM447 in combination with other drugs for the treatment of MM.Trial registration: clinicaltrials.gov: (NCT02160951).
PIM447 是一种泛原病毒整合位点,可抑制 Moloney 白血病激酶,在多发性骨髓瘤(MM)中显示出临床前活性。这项 I 期、开放性、多中心、剂量递增研究旨在确定 PIM447 在复发和/或难治性(R/R)MM 日本患者中的最大耐受剂量(MTD)和扩展推荐剂量(RDE)。该研究纳入了 13 名患者(250mg 每日一次(QD),[n=7];300mg QD,[n=6])。唯一观察到的剂量限制毒性是 300mg 组 1 名患者的 3 级 QTc 延长,未确定 MTD 和 RDE。最常见的疑似 PIM447 相关不良事件(AE)包括血小板减少症(76.9%)、贫血(53.8%)和白细胞减少症(53.8%)。所有患者均发生至少 1 次 3 级或 4 级 AE,最常见的是血小板减少症或白细胞减少症(各占 61.5%)。总缓解率为 15.4%,疾病控制率为 69.2%,临床获益率为 23.1%,2 名患者有部分缓解(每组各 1 例)。2 名接受 250mg QD 治疗的患者的无进展生存期>6 个月。PIM447 250mg 或 300mg QD 在 R/R MM 日本患者中可耐受。需要进一步研究评估 PIM447 与其他药物联合治疗 MM 的临床结局。
clinicaltrials.gov:(NCT02160951)。