Karyopharm Therapeutics, Department of Neurofegenerative and Infectious Diseases, Newton, Massachussets, United States of America.
PLoS One. 2018 Oct 17;13(10):e0200043. doi: 10.1371/journal.pone.0200043. eCollection 2018.
Infection of immunocompromised individuals with normally benign opportunistic viruses is a major health burden globally. Infections with viruses such as Epstein-Barr virus (EBV), human cytomegalovirus (HCMV), Kaposi's sarcoma virus (KSHV), adenoviruses (AdV), BK virus (BKPyV), John Cunningham virus (JCPyV), and human papillomavirus (HPV) are significant concerns for the immunocompromised, including when these viruses exist as a co-infection with human immunodeficiency virus (HIV). These viral infections are more complicated in patients with a weakened immune system, and often manifest as malignancies resulting in significant morbidity and mortality. Vaccination is not an attractive option for these immune compromised individuals due to defects in their adaptive immune response. Verdinexor is part of a novel class of small molecules known as SINE (Selective Inhibitor of Nuclear Export) compounds. These small molecules demonstrate specificity for the nuclear export protein XPO1, to which they bind and block function, resulting in sequestration of XPO1-dependent proteins in the nucleus of the cell. In antiviral screening, verdinexor demonstrated varying levels of efficacy against all of the aforementioned viruses including previously with HIV. Studies by other labs have discussed likely mechanisms of action for verdinexor (ie. XPO1-dependence) against each virus. GLP toxicology studies suggest that anti-viral activity can be achieved at a tolerable dose range, based on the safety profile of a previous phase 1 clinical trial of verdinexor in healthy human volunteers. Taken together, these results indicate verdinexor has the potential to be a broad spectrum antiviral for immunocompromised subjects for which vaccination is a poor option.
免疫功能低下个体感染通常为良性机会性病毒,这是全球范围内的一个主要健康负担。免疫功能低下个体感染如 EBV(Epstein-Barr 病毒)、HCMV(人类巨细胞病毒)、KSHV(卡波济肉瘤相关疱疹病毒)、腺病毒(AdV)、BKPyV(BK 病毒)、JCPyV(约翰-坎宁安病毒)和 HPV(人乳头瘤病毒)等病毒,是一个重大的健康隐患,当这些病毒与 HIV(人类免疫缺陷病毒)共同感染时更是如此。在免疫系统较弱的患者中,这些病毒感染更为复杂,通常表现为恶性肿瘤,导致发病率和死亡率显著增加。由于这些免疫低下个体的适应性免疫反应存在缺陷,因此疫苗接种并不是一个有吸引力的选择。Verdinexor 是一类新型小分子药物,属于 SINE(选择性核输出抑制剂)化合物。这些小分子对核输出蛋白 XPO1 具有特异性,与 XPO1 结合并阻断其功能,导致 XPO1 依赖性蛋白在细胞核内被隔离。在抗病毒筛选中,Verdinexor 对上述所有病毒(包括之前对 HIV 的研究)表现出不同程度的疗效。其他实验室的研究讨论了 verdinexor(即 XPO1 依赖性)针对每种病毒的可能作用机制。GLP 毒理学研究表明,基于 verdinexor 在健康人类志愿者中的先前 1 期临床试验的安全性概况,可以在可耐受的剂量范围内实现抗病毒活性。综上所述,这些结果表明 verdinexor 有可能成为免疫功能低下患者的广谱抗病毒药物,而疫苗接种对这些患者来说是一个较差的选择。