Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48202, USA.
Int J Mol Sci. 2023 Jan 31;24(3):2645. doi: 10.3390/ijms24032645.
Therapy for multiple myeloma (MM), a hematologic neoplasm of plasma cells, has undergone remarkable changes over the past 25 years. Small molecules (molecular weight of less than one kDa), together with newer immunotherapies that include monoclonal antibodies, antibody-drug conjugates, and most recently, chimeric antigen receptor (CAR) T-cells, have combined to double the disease's five-year survival rate to over 50% during the past few decades. Despite these advances, the disease is still considered incurable, and its treatment continues to pose substantial challenges, since therapeutic refractoriness and patient relapse are exceedingly common. This review focuses on the current pipeline, along with the contemporary roles and future prospects for small molecules in MM therapy. While small molecules offer prospective benefits in terms of oral bioavailability, cellular penetration, simplicity of preparation, and improved cost-benefit considerations, they also pose problems of toxicity due to off-target effects. Highlighted in the discussion are recent developments in the applications of alkylating agents, immunomodulators, proteasome inhibitors, apoptosis inducers, kinesin spindle protein inhibitors, blockers of nuclear transport, and drugs that affect various kinases involved in intracellular signaling pathways. Molecular and cellular targets are described for each class of agents in relation to their roles as drivers of MM.
多发性骨髓瘤(MM)是一种浆细胞的血液系统恶性肿瘤,在过去 25 年中,其治疗方法发生了显著变化。小分子(分子量小于 1 kDa),加上新型免疫疗法,包括单克隆抗体、抗体药物偶联物,以及最近的嵌合抗原受体(CAR)T 细胞,将该病的 5 年生存率提高了一倍,在过去几十年中超过了 50%。尽管取得了这些进展,但该疾病仍被认为是无法治愈的,其治疗仍然存在很大的挑战,因为治疗耐药性和患者复发非常常见。本综述重点介绍了当前的治疗方法,以及小分子在 MM 治疗中的现代作用和未来前景。虽然小分子在口服生物利用度、细胞通透性、制备简单性和改善成本效益方面具有潜在优势,但由于脱靶效应,它们也存在毒性问题。讨论中强调了烷基化剂、免疫调节剂、蛋白酶体抑制剂、凋亡诱导剂、驱动蛋白纺锤体蛋白抑制剂、核转运阻滞剂以及影响细胞内信号通路的各种激酶的药物在应用方面的最新进展。描述了每类药物的分子和细胞靶点,以及它们作为 MM 驱动因素的作用。