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多发性骨髓瘤中的 Cereblon E3 连接酶调节剂美法仑和伊班膦酸盐。

Cereblon E3 Ligase Modulators Mezigdomide and Iberdomide in Multiple Myeloma.

机构信息

Department of Hematology and Oncology, Myeloma Center, University of Arkansas for Medical Sciences, Little Rock, AR.

Department of Hematology and Oncology, Myeloma Center, University of Arkansas for Medical Sciences, Little Rock, AR.

出版信息

Clin Lymphoma Myeloma Leuk. 2024 Nov;24(11):762-769. doi: 10.1016/j.clml.2024.06.004. Epub 2024 Jun 24.

DOI:10.1016/j.clml.2024.06.004
PMID:39003099
Abstract

Multiple Myeloma (MM) remains a challenging hematological malignancy despite significant advancements made during the past 2 decades. Outcomes have improved by incorporating immunomodulatory drugs, proteasome inhibitors, and anti-CD38 monoclonal antibodies into treatment algorithms that include high dose chemotherapy and autologous hematopoietic stem cell transplantation. However, many patients may eventually relapse despite these innovations. Newer therapies targeting B-Cell Maturation Antigen (BCMA) offer promise for patients with relapsed or refractory disease. BCMA-targeted therapies carry notable side effects, necessitating vigilant monitoring and proactive infection prevention measures. They can also induce considerable immunosuppression, attributed to lower levels of immunoglobulins and increased susceptibility to infections. There is still a need for alternative treatment options with different mechanisms of action that can be easily administered and have a better safety profile. In addition, pomalidomide only overcomes lenalidomide refractoriness in a subset of patients. This review aims to explore 2 next-generation cereblon E3 ligase modulators (CELMoDs), Mezigdomide (CC92480), and Iberdomide (CC-220). We will discuss the biological aspects of these agents, including their mechanisms of action, efficacy, and toxicity profile, and provide a comprehensive review of current literature. Special attention will be paid to ongoing and future clinical trials that provide insights into the potential of these novel therapies in the management of MM.

摘要

多发性骨髓瘤(MM)尽管在过去 20 年中取得了重大进展,但仍是一种具有挑战性的血液系统恶性肿瘤。通过将免疫调节剂、蛋白酶体抑制剂和抗 CD38 单克隆抗体纳入包括高剂量化疗和自体造血干细胞移植的治疗方案,改善了预后。然而,尽管有这些创新,许多患者最终仍可能复发。针对 B 细胞成熟抗原(BCMA)的新型疗法为复发或难治性疾病患者带来了希望。BCMA 靶向疗法具有显著的副作用,需要进行严密监测和积极的感染预防措施。它们还会引起明显的免疫抑制,导致免疫球蛋白水平降低和感染易感性增加。因此,仍需要具有不同作用机制、易于管理且具有更好安全性特征的替代治疗选择。此外,泊马度胺仅能克服部分患者对来那度胺的耐药性。本综述旨在探讨两种下一代 cereblon E3 连接酶调节剂(CELMoD),美法仑(CC92480)和伊班膦(CC-220)。我们将讨论这些药物的生物学特性,包括它们的作用机制、疗效和毒性特征,并对当前的文献进行全面综述。特别关注正在进行和未来的临床试验,这些试验为这些新型疗法在 MM 管理中的潜在应用提供了深入了解。

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Cereblon E3 Ligase Modulators Mezigdomide and Iberdomide in Multiple Myeloma.多发性骨髓瘤中的 Cereblon E3 连接酶调节剂美法仑和伊班膦酸盐。
Clin Lymphoma Myeloma Leuk. 2024 Nov;24(11):762-769. doi: 10.1016/j.clml.2024.06.004. Epub 2024 Jun 24.
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Iberdomide (CC-220) is a potent cereblon E3 ligase modulator with antitumor and immunostimulatory activities in lenalidomide- and pomalidomide-resistant multiple myeloma cells with dysregulated CRBN.伊布多米德(CC-220)是一种强效的脑啡肽E3连接酶调节剂,在对来那度胺和泊马度胺耐药且CRBN失调的多发性骨髓瘤细胞中具有抗肿瘤和免疫刺激活性。
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引用本文的文献

1
Targeting degradation of IKZF1 and IKZF3 through modulation of the E3 ligase substrates in the context of cellular therapies for multiple myeloma.在多发性骨髓瘤细胞治疗背景下,通过调节E3连接酶底物靶向降解IKZF1和IKZF3
Biomark Res. 2025 Aug 15;13(1):105. doi: 10.1186/s40364-025-00825-8.
2
Regulatory role of E3 ubiquitin ligases in multiple myeloma: from molecular mechanisms to therapeutic strategies.E3泛素连接酶在多发性骨髓瘤中的调控作用:从分子机制到治疗策略
Front Cell Dev Biol. 2025 Jul 30;13:1620097. doi: 10.3389/fcell.2025.1620097. eCollection 2025.
3
Multiple Myeloma Unpacked.
解读多发性骨髓瘤
Hematol Oncol. 2025 Jun;43 Suppl 2(Suppl 2):e70067. doi: 10.1002/hon.70067.