Fisher Jack G, Bartlett Laura G, Kashyap Trinayan, Walker Christopher J, Khakoo Salim I, Blunt Matthew D
Clinical and Experimental Sciences, University of Southampton, SO16 7YD Southampton, UK.
Karyopharm Therapeutics, Newton, MA 02459, USA.
Explor Target Antitumor Ther. 2025 Apr 23;6:1002310. doi: 10.37349/etat.2025.1002310. eCollection 2025.
Exportin-1 (XPO1) is a nuclear export protein that, when overexpressed, can facilitate cancer cell proliferation and survival and is frequently overexpressed or mutated in cancer patients. As such, selective inhibitors of XPO1 (XPO1i) function have been developed to inhibit cancer cell proliferation and induce apoptosis. This review outlines the evidence for the immunomodulatory properties of XPO1 inhibition and discusses the potential for combining and sequencing XPO1i with immunotherapy to improve the treatment of patients with cancer. Selinexor is a first-in-class XPO1i that is FDA-approved for the treatment of patients with relapsed and refractory (RR) multiple myeloma and RR diffuse large B cell lymphoma. In addition to the cancer cell intrinsic pro-apoptotic activity, increasing evidence suggests that XPO1 inhibition has immunomodulatory properties. In this review, we describe how XPO1i can lead to a skewing of macrophage polarisation, inhibition of neutrophil extracellular traps, modulation of immune checkpoint expression, blockade of myeloid-derived suppressor cells (MDSCs) and sensitisation of cancer cells to T cell and NK (natural killer) cell immunosurveillance. As such, there is an opportunity for selinexor to enhance immunotherapy efficacy and thus a need for clinical trials assessing selinexor in combination with immunotherapies such as immune checkpoint inhibitors, direct targeting monoclonal antibodies, chimeric antigen receptor (CAR)-T cells and cereblon E3 ligase modulators (CELMoDs).
核输出蛋白1(XPO1)是一种核输出蛋白,过度表达时可促进癌细胞增殖和存活,在癌症患者中经常过度表达或发生突变。因此,已开发出XPO1(XPO1i)功能的选择性抑制剂来抑制癌细胞增殖并诱导凋亡。本综述概述了XPO1抑制的免疫调节特性的证据,并讨论了将XPO1i与免疫疗法联合使用和进行序贯治疗以改善癌症患者治疗效果的潜力。塞利尼索是首个获批的XPO1i,被美国食品药品监督管理局(FDA)批准用于治疗复发难治性(RR)多发性骨髓瘤和RR弥漫性大B细胞淋巴瘤患者。除了癌细胞固有的促凋亡活性外,越来越多的证据表明XPO1抑制具有免疫调节特性。在本综述中,我们描述了XPO1i如何导致巨噬细胞极化偏向、抑制中性粒细胞胞外陷阱、调节免疫检查点表达、阻断髓源性抑制细胞(MDSC)以及使癌细胞对T细胞和自然杀伤(NK)细胞免疫监视敏感。因此,塞利尼索有机会提高免疫治疗疗效,因此需要进行临床试验来评估塞利尼索与免疫疗法(如免疫检查点抑制剂、直接靶向单克隆抗体、嵌合抗原受体(CAR)-T细胞和脑啡肽E3连接酶调节剂(CELMoD))联合使用的效果。