Therapeutic Drug Monitoring: A New Hope for Individualised Treatment with Venetoclax.

IF 2.5 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug targets Pub Date : 2025-07-16 DOI:10.2174/0113894501376271250710221018

Yue Tang, Shuojiao Li, Peng Rao, Wenxian Yu, Xuanpeng Jiang, Jiatao Liu

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引用次数: 0

Abstract

B-cell lymphoma-2 (BCL-2) plays a key role in regulating apoptosis. Venetoclax (VEN), a BCL-2 inhibitor, has been approved for the treatment of a variety of haematologic malignancies. VEN is primarily metabolized by CYP3A, and a variety of factors (such as CYP3A inhibitors, as well as food and hepatic functions) have been reported to significantly influence the metabolic process. There is significant interindividual variability in VEN plasma concentrations, and studies have shown that its exposure levels are correlated with efficacy, although the relationship with adverse effects remains controversial. The value of applying of therapeutic drug monitoring (TDM) in individualized VEN therapy has been confirmed by some studies, but the optimal therapeutic window for different malignancies is still unclear. This review summarizes the pharmacokinetic characteristics, along with the factors influencing VEN pharmacokinetics, drug-drug interactions, and advancements in TDM research on VEN, aiming to provide a theoretical basis for TDM-guided individualized therapy.

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治疗药物监测：Venetoclax个体化治疗的新希望。

b细胞淋巴瘤-2 （BCL-2）在调节细胞凋亡中起关键作用。Venetoclax （VEN）是一种BCL-2抑制剂，已被批准用于治疗多种血液恶性肿瘤。VEN主要由CYP3A代谢，多种因素（如CYP3A抑制剂，以及食物和肝功能）已被报道显着影响代谢过程。VEN血浆浓度存在显著的个体间差异，研究表明其暴露水平与疗效相关，尽管与不良反应的关系仍存在争议。治疗药物监测（TDM）在个体化VEN治疗中的应用价值已被一些研究证实，但不同恶性肿瘤的最佳治疗窗口尚不清楚。本文就其药动学特点、影响VEN药动学的因素、药物-药物相互作用以及TDM在VEN方面的研究进展进行综述，旨在为TDM指导下的个体化治疗提供理论依据。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current drug targets 医学-药学

CiteScore

6.20

自引率

0.00%

发文量

127

审稿时长

3-8 weeks

期刊介绍： Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes. Current Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of drug targets. The journal also accepts for publication mini- & full-length review articles and drug clinical trial studies. As the discovery, identification, characterization and validation of novel human drug targets for drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.