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度维利塞:一种2018年获美国食品药品监督管理局批准的新型小分子磷酸肌醇3激酶抑制剂。

Duvelisib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Phosphoinositide 3-Kinases.

作者信息

Rodrigues Daniel A, Sagrillo Fernanda S, Fraga Carlos A M

机构信息

Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, PO Box 68023, Rio de Janeiro, RJ 21941-902, Brazil.

Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ 21941-909, Brazil.

出版信息

Pharmaceuticals (Basel). 2019 May 6;12(2):69. doi: 10.3390/ph12020069.

DOI:10.3390/ph12020069
PMID:31064155
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6631818/
Abstract

Duvelisib (Copiktra) is a dual inhibitor of phosphoinositide 3-kinases (PI3Kδ and PI3Kγ). In 2018, duvelisib was first approved by the Food and Drug Administration (FDA) for the treatment of adult patients with relapsed or refractory chronic lymphocytic leukaemia (CLL)/ small lymphocytic lymphoma (SLL) after at least two prior therapies. Duvelisib has also been approved under accelerated track for relapsed or refractory follicular lymphoma (FL) after at least two prior systemic therapies. In this review, we provide a series of information about duvelisib, such as the development of clinical trials for LLC/SLL and FL and the steps used for its synthesis.

摘要

度维利塞(Copiktra)是一种磷酸肌醇3-激酶(PI3Kδ和PI3Kγ)双重抑制剂。2018年,度维利塞首次获得美国食品药品监督管理局(FDA)批准,用于治疗至少接受过两种先前疗法的复发或难治性成人慢性淋巴细胞白血病(CLL)/小淋巴细胞淋巴瘤(SLL)。度维利塞也已在加速审批通道下获批,用于治疗至少接受过两种先前全身疗法的复发或难治性滤泡性淋巴瘤(FL)。在本综述中,我们提供了一系列关于度维利塞的信息,例如LLC/SLL和FL的临床试验进展及其合成步骤。

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Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.PI3Kγ 和 δ 抑制剂在炎症和自身免疫性疾病中的研究进展。
J Med Chem. 2019 May 23;62(10):4783-4814. doi: 10.1021/acs.jmedchem.8b01298. Epub 2018 Dec 24.
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Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.1 类 PI3K 临床候选药物和近期抑制剂设计策略:药物化学视角。
急性髓系白血病中的大鼠肉瘤病毒科基因:发病机制及临床意义
Biomedicines. 2025 Jan 15;13(1):202. doi: 10.3390/biomedicines13010202.
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Duvelisib is a novel NFAT inhibitor that mitigates adalimumab-induced immunogenicity.度维利塞是一种新型的NFAT抑制剂,可减轻阿达木单抗诱导的免疫原性。
Front Pharmacol. 2025 Jan 9;15:1397995. doi: 10.3389/fphar.2024.1397995. eCollection 2024.
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Insights into genetic aberrations and signalling pathway interactions in chronic lymphocytic leukemia: from pathogenesis to treatment strategies.慢性淋巴细胞白血病中基因畸变与信号通路相互作用的见解:从发病机制到治疗策略
Biomark Res. 2024 Dec 28;12(1):162. doi: 10.1186/s40364-024-00710-w.
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