Navigating the Challenges of Cyclosporine as an Alternative to Rifampicin as an OATP1B Index Inhibitor.

IF 6.3 2区医学 Q1 PHARMACOLOGY & PHARMACY

Clinical Pharmacology & Therapeutics Pub Date : 2025-01-14 DOI:10.1002/cpt.3564

Manthena V S Varma, Manoli Vourvahis

引用次数: 0

Abstract

Rifampicin is a widely employed index inhibitor to assess the impact of organic anion transporting polypeptide 1B (OATP1B) inhibition on investigational drugs. The observation of nitrosamines in certain drug products, including rifampicin, has impacted the conduct of clinical drug-drug interaction (DDI) studies with rifampicin drug products. Cyclosporine is a recommended alternative to assess in vivo OATP1B activity; however, challenges exist in its use due to pharmacokinetic (PK) variability and non-selective inhibition of other drug disposition mechanisms.

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环孢素替代利福平作为OATP1B指数抑制剂的挑战

利福平是一种广泛使用的指数抑制剂，用于评估有机阴离子转运多肽1B （OATP1B）抑制对研究药物的影响。在包括利福平在内的某些药品中观察到亚硝胺，影响了利福平药品的临床药物相互作用（DDI）研究的进行。环孢素是评估体内OATP1B活性的推荐替代方案；然而，由于药代动力学（PK）的可变性和其他药物处置机制的非选择性抑制，其使用存在挑战。

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

Clinical Pharmacology & Therapeutics 医学-药学

CiteScore

12.70

自引率

7.50%

发文量

290

审稿时长

2 months

期刊介绍： Clinical Pharmacology & Therapeutics (CPT) is the authoritative cross-disciplinary journal in experimental and clinical medicine devoted to publishing advances in the nature, action, efficacy, and evaluation of therapeutics. CPT welcomes original Articles in the emerging areas of translational, predictive and personalized medicine; new therapeutic modalities including gene and cell therapies; pharmacogenomics, proteomics and metabolomics; bioinformation and applied systems biology complementing areas of pharmacokinetics and pharmacodynamics, human investigation and clinical trials, pharmacovigilence, pharmacoepidemiology, pharmacometrics, and population pharmacology.