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Inhibition of human UDP-glucuronosyltransferase enzyme by ripretinib: Implications for drug-drug interactions.

Author: JiangLili, LiuYong, LvXin, WangZhe, WangZhen, XiaYangliu, YinHang

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

Ripretinib, a tyrosine kinase inhibitor (TKI) for advanced gastrointestinal stromal tumor (GIST), was found to potently inhibit several UDP-glucosyltransferase (UGT) isoforms, including UGT1A1, UGT1A3, UGT1A4, UGT1A7, and UGT1A8. In vitro-in vivo extrapolation (IVIVE) predicts a potential risk of drug-drug interactions (DDIs) when ripretinib is combined with drugs metabolized by these UGT isoforms. Clinicians should be aware of this potential risk and consider adjusting dosages or avoiding concomitant use when necessary.
Paper Details　
Original Abstract of the Article :
Ripretinib, a tyrosine kinase inhibitor (TKI), is the first FDA approved fourth-line therapy for adults with advanced gastrointestinal stromal tumor (GIST). Studies have shown that several TKIs for treating GIST were potent inhibitors of human UDP-glucosyltransferase (UGTs) enzymes. However, whether...See full text at original site
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引用元：
https://doi.org/10.1016/j.taap.2023.116490

データ提供：米国国立医学図書館（NLM）

Navigating the Interplay of Drugs: Ripretinib and UGT Enzymes

The world of drug interactions is like a vast desert, where different compounds can interact in complex and unpredictable ways. This study, conducted by [著者名] et al., explores the potential interactions between ripretinib, a tyrosine kinase inhibitor (TKI) used to treat gastrointestinal stromal tumors (GIST), and human UDP-glucuronosyltransferase (UGTs) enzymes. The researchers investigated the inhibitory effects of ripretinib on major UGT isoforms, aiming to understand the potential for drug-drug interactions (DDIs) when ripretinib is combined with other drugs metabolized by UGTs. This is like exploring the intricate ecosystem of the desert, where different species interact with each other, potentially affecting the survival and well-being of the whole system.

Ripretinib: A Powerful Drug with Potential Interactions

The study found that ripretinib exhibited potent inhibition against several UGT isoforms, suggesting that it could potentially interfere with the metabolism of other drugs. This is like discovering a new plant in the desert that, while offering potential benefits, may also have unexpected effects on the surrounding ecosystem.

Minimizing Drug-Drug Interactions

This research highlights the importance of considering potential drug interactions when prescribing ripretinib. Clinicians should carefully evaluate the potential for DDIs and adjust drug regimens accordingly to minimize the risk of adverse effects. This is like carefully managing the water resources in the desert, ensuring a balanced and sustainable supply for all species.

Dr.Camel's Conclusion

This research provides valuable insights into the complex world of drug-drug interactions, emphasizing the importance of understanding the potential effects of ripretinib on UGT enzyme activity. This is like uncovering a hidden oasis in the desert of drug interactions, reminding us that even the most promising treatments may have unexpected consequences, necessitating careful monitoring and management.

Date :
  1. Date Completed 2023-04-07
  2. Date Revised 2023-05-08
Further Info :

Pubmed ID

36963523

DOI: Digital Object Identifier

10.1016/j.taap.2023.116490

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SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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