关键词: antiretroviral drugs bladder cancer efficacy evaluation etravirine personalized medicine repurposing possibilities synergy

来  源:   DOI:10.3390/biomedicines12030647   PDF(Pubmed)

Abstract:
This research explores the therapeutic efficacy of Darunavir (DRV), Rilpivirine (RPV), and Etravirine (ETV) against UM-UC-5 bladder cancer cells, addressing the critical need for innovative treatments in bladder cancer research. Through a comprehensive assessment of their individual and combined effects across diverse time intervals, ETV emerges as the most potent drug, with a lowest IC50 of 5.9 µM, closely followed by RPV (lowest IC50 of 9.6 µM), while DRV exhibits the least effectiveness (lowest IC50 of 25.6 µM). Notably, a significant synergistic effect is evident in the ETV and RPV combination, especially at 48 and 72 h for low concentrations. Synergies are also observed with ETV and DRV, albeit to a lesser extent and primarily at 48 h. Conversely, the DRV and RPV combination yields minimal effects, predominantly additive in nature. In summary, this pre-clinical investigation underscores the promising therapeutic potential of ETV and RPV, both as standalone treatments and in combination, hinting at repurposing opportunities in bladder cancer therapy, which could give a new treatment method for this disease that is faster and without as severe side effects as anticancer drugs. These findings represent a substantial stride in advancing personalized medicine within cancer research and will be further scrutinized in forthcoming studies.
摘要:
这项研究探讨了达鲁那韦(DRV)的治疗效果,利匹韦林(RPV),和ETV(ETV)对UM-UC-5膀胱癌细胞,解决膀胱癌研究中创新治疗的关键需求。通过全面评估他们在不同时间间隔内的个体和组合效应,ETV成为最有效的药物,最低IC50为5.9µM,紧随其后的是RPV(最低IC50为9.6µM),而DRV表现出最小的有效性(最低IC50为25.6µM)。值得注意的是,ETV和RPV组合具有明显的协同作用,特别是在48和72小时的低浓度。ETV和DRV也观察到了协同作用,尽管程度较小,主要是在48小时。相反,DRV和RPV组合产生的效果最小,在自然界中主要是添加剂。总之,这项临床前调查强调了ETV和RPV的有希望的治疗潜力,作为独立治疗和组合治疗,暗示膀胱癌治疗的再利用机会,这可以为这种疾病提供一种新的治疗方法,该方法更快,并且没有抗癌药物那样严重的副作用。这些发现代表了在癌症研究中推进个性化医学的实质性进展,并将在即将进行的研究中进一步审查。
公众号