亚盛医药-B(06855.HK)：Bcl-2抑制剂APG-2575获美国FDA临床试验许可
格隆汇6月15日丨亚盛医药-B(06855.HK)公布，公司在研原创新药Bcl-2抑制剂APG-2575的临床试验申请获美国食品药品管理局（美国FDA）许可，将展开单药或与抗癌药物联合治疗晚期ER+乳腺癌或实体瘤的研究。
该研究是一项全球多中心、开放性、Ib/II期临床研究，旨在评估APG-2575单药治疗晚期实体瘤患者，或联合CDK4/6抑制剂palbociclib治疗CDK4/6抑制剂治疗后进展或复发的ER+/HER2-转移性乳腺癌患者的安全性、耐受性、药代动力学特征及初步疗效。
乳腺癌是女性最常见的恶性肿瘤之一，大约75%的乳腺癌患者为激素受体阳性(HR+)乳腺癌，主要为雌激素受体阳性(ER+)，该亚型中约85%为Bcl-2过表达。内分泌治疗是早期和转移阶段HR+/HER2-乳腺癌治疗的基石。在转移性ER+乳腺癌的一綫治疗中，CDK4/6抑制剂（包括palbociclib、ribociclib和abemaciclib）联合激素疗法通过靶向CCND1-CDK4/6-RB通路与单用激素疗法相比，可延长无进展生存期(PFS)和最终总生存(OS)3,4；而在二线治疗中，PI3K抑制剂联合氟维司群与依维莫司联合内分泌治疗可以通过靶向PI3K-AKT-mTOR通路克服既往治疗的选择压力。然而，内分泌治疗和靶向治疗的耐药性较难避免，并最终需要化疗，因此探索其他新的靶向治疗阻断现有的突变途径和推迟化疗是亟待解决的临床问题。
据悉，APG-2575是亚盛医药在研的新型口服Bcl-2选择性小分子抑制剂，通过选择性抑制Bcl-2蛋白来恢复肿瘤细胞程序性死亡机制（细胞凋亡），从而诱导肿瘤细胞凋亡，达到治疗肿瘤的目的。APG-2575是首个在中国进入临床阶段的、本土研发的Bcl-2选择性抑制剂，目前已获得中国、美国、澳大利亚及欧洲的多项Ib/II期临床试验许可，正在全球同步推进多个血液肿瘤适应症的临床开发。作为单药，APG-2575对于Bcl-2依赖的肿瘤细胞具有强的抗肿瘤活性，并且与其他抗癌药物组合表现出更广泛的抗肿瘤活性。
此前，APG-2575联合palbociclib的临床前研究结果显示，palbociclib通过诱导细胞周期阻滞而导致细胞衰老，而APG-2575增加促凋亡蛋白BIM等表达，下调ER水平，降低磷酸化的Rb蛋白、细胞周期蛋白D1和E的蛋白水平。因此，Bcl-2抑制剂和CDK4/6抑制剂联合用药不仅可以协同增强诱导细胞周期停滞，还可以促进ER+乳腺癌细胞凋亡。
Follow us
Find us on
Facebook,
Twitter ,
Instagram, and
YouTube or frequent updates on all things investing.Have a financial topic you would like to discuss? Head over to the
uSMART Community to share your thoughts and insights about the market! Click the picture below to download and explore uSMART app！
Disclaimers
uSmart Securities Limited (“uSmart”) is based on its internal research and public third party information in preparation of this article. Although uSmart uses its best endeavours to ensure the content of this article is accurate, uSmart does not guarantee the accuracy, timeliness or completeness of the information of this article and is not responsible for any views/opinions/comments in this article. Opinions, forecasts and estimations reflect uSmart’s assessment as of the date of this article and are subject to change. uSmart has no obligation to notify you or anyone of any such changes. You must make independent analysis and judgment on any matters involved in this article. uSmart and any directors, officers, employees or agents of uSmart will not be liable for any loss or damage suffered by any person in reliance on any representation or omission in the content of this article. The content of the article is for reference only and does not constitute any offer, solicitation, recommendation, opinion or guarantee of any securities, virtual assets, financial products or instruments. Regulatory authorities may restrict the trading of virtual asset-related ETFs to only investors who meet specified requirements. Any calculations or images in the article are for illustrative purposes only.
Investment involves risks and the value and income from securities may rise or fall. Past performance is not indicative of future performance. Please carefully consider your personal risk tolerance, and consult independent professional advice if necessary.
