Department of Investigational Cancer Therapeutics (Phase I Clinical Trials Program), Division of Cancer Medicine, The University of Texas MD Anderson Cancer Center, 1515 Holcombe Blvd, Houston, TX, 77030, USA.
Division of Hematology and Medical Oncology, Oregon Health and Science University/ Knight Cancer Institute, Portland, OR, USA.
Invest New Drugs. 2021 Oct;39(5):1357-1365. doi: 10.1007/s10637-021-01119-0. Epub 2021 Apr 28.
Background Selinexor, a first-in-class, oral selective inhibitor of nuclear export (SINE) compound inhibits Exportin-1(XPO1), had demonstrated synergistic activity with many chemotherapies and conferred in vivo antitumor efficacy in hematologic as well as solid tumors. Methods This open-label, single-center, multi-arm phase 1b study used a standard 3 + 3 design and a "basket type" expansion. Selinexor with intravenous topotecan was given in one of the 13 parallel arms. Patients with advanced or metastatic relapsed/refractory solid tumors following prior systemic therapy, or in whom the addition of selinexor to standard chemotherapy deemed appropriate, were eligible. Results Fourteen patients with the median age of 61 years (range, 22-68years) were treated, and the most common cancer types were gynecological cancers; ovarian (n = 5), endometrial (n = 2), and 1 each with fallopian tube and vaginal cancers. Of the 14 patients treated, 12 (86 %) had at least one treatment-related adverse event (TRAE). The most common TRAEs were anemia (71 %), thrombocytopenia (57 %), hyponatremia (57 %), vomiting (57 %), fatigue (50 %), nausea (50 %), and neutropenia (36 %). Two patients had dose limiting toxicities. One patient dosed at selinexor 80 mg had grade 3 nausea and vomiting and one patient dosed at selinexor 60 mg experienced grade 4 neutropenia and thrombocytopenia. Of the 13 efficacy evaluable patients, one (8 %) with endometrial cancer achieved unconfirmed partial response (uPR) and the time-to-treatment failure (TTF) was 48 weeks, whereas 6 of the 13 (46 %) patients had stable disease (SD) contributing to the clinical benefit rate of 46 %. The median TTF for all patients was 9 weeks (range, 2-48weeks). Conclusions Once weekly selinexor in combination with topotecan was viable and showed some preliminary tumor efficacy. The recommend phase 2 dose of selinexor was 60 mg once weekly in combination with IV topotecan.Trial registration: NCT02419495. Registered 14 April 2015, https://clinicaltrials.gov/ct2/show/NCT02419495.
Selinexor 是一种首创的、口服的核输出抑制剂(SINE)化合物,可抑制 Exportin-1(XPO1),与许多化疗药物具有协同作用,并在血液系统和实体肿瘤中显示出体内抗肿瘤疗效。
这项开放标签、单中心、多臂 1b 期研究采用标准的 3+3 设计和“篮式”扩展。在其中一个 13 个平行臂中给予静脉注射拓扑替康联合 Selinexor。先前接受过系统治疗的晚期或转移性复发性/难治性实体瘤患者,或认为添加 Selinexor 到标准化疗中合适的患者符合条件。
14 名中位年龄为 61 岁(范围为 22-68 岁)的患者接受了治疗,最常见的癌症类型为妇科癌症;卵巢癌(n=5)、子宫内膜癌(n=2),以及输卵管癌和阴道癌各 1 例。在接受治疗的 14 名患者中,有 12 名(86%)至少有 1 种与治疗相关的不良事件(TRAEs)。最常见的 TRAEs 是贫血(71%)、血小板减少症(57%)、低钠血症(57%)、呕吐(57%)、疲劳(50%)、恶心(50%)和中性粒细胞减少症(36%)。有 2 名患者出现剂量限制毒性。1 名接受 Selinexor 80mg 剂量的患者出现 3 级恶心和呕吐,1 名接受 Selinexor 60mg 剂量的患者出现 4 级中性粒细胞减少症和血小板减少症。在 13 名可评估疗效的患者中,1 名(8%)子宫内膜癌患者获得未确认的部分缓解(uPR),治疗失败时间(TTF)为 48 周,而 13 名患者中有 6 名(46%)病情稳定(SD),临床获益率为 46%。所有患者的中位 TTF 为 9 周(范围为 2-48 周)。
每周一次的 Selinexor 联合拓扑替康是可行的,并显示出一些初步的肿瘤疗效。Selinexor 的推荐 2 期剂量为每周 60mg,联合 IV 拓扑替康。试验注册:NCT02419495。于 2015 年 4 月 14 日注册,https://clinicaltrials.gov/ct2/show/NCT02419495。