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度维利塞布:全面剖析。

Duvelisib: A comprehensive profile.

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.

出版信息

Profiles Drug Subst Excip Relat Methodol. 2024;49:19-40. doi: 10.1016/bs.podrm.2023.11.002. Epub 2023 Dec 7.

Abstract

Duvelisib (DUV) is chemically named as (S)-3-(1-((9H-Purin-6-yl)amino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one. It is a novel drug with a small molecular weight and characterized by dual phosphoinositide-3-kinase (PI3K)- and PI3K-inhibitory activity. The Food and Drug Administration (FDA) recently approved DUV for the management of small lymphocytic lymphoma (SLL) and relapsed or refractory chronic lymphocytic leukemia (CLL) in adult patients. DUV is marketed under the brand name of Copiktra® (Verastem, Inc., Needham, MA, USA). This chapter provides a critical extensive review of the literature, the description of DUV in terms of its names, formulae, elemental composition, appearance, and use in the treatment of CLL, SLL, and follicular lymphoma. The chapter also describes the methods for preparation of DUV, its physical-chemical properties, analytical methods for its determination, pharmacological properties, and dosing information.

摘要

度维利塞(DUV)的化学名称为(S)-3-(1-((9H-嘌呤-6-基)氨基)乙基)-8-氯-2-苯基异喹啉-1(2H)-酮。它是一种具有双磷酰肌醇-3-激酶(PI3K)和 PI3K 抑制活性的新型小分子药物。美国食品和药物管理局(FDA)最近批准 DUV 用于治疗成人小淋巴细胞淋巴瘤(SLL)和复发性或难治性慢性淋巴细胞白血病(CLL)。DUV 以 Copiktra®(Verastem,Inc.,马萨诸塞州 Needham)的品牌名称销售。本章对文献进行了批判性的广泛综述,描述了 DUV 的名称、公式、元素组成、外观以及在 CLL、SLL 和滤泡性淋巴瘤治疗中的用途。本章还描述了 DUV 的制备方法、理化性质、测定的分析方法、药理学性质和剂量信息。

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