Paper Details

  1. Home
  2. Paper Details

Inhibition of human UDP-glucuronosyltransferase (UGT) enzymes by kinase inhibitors: Effects of dabrafenib, ibrutinib, nintedanib, trametinib and BIBF 1202.

Author: ChauNuy, KorprasertthawornPorntipa, MinersJohn O, NairPramod C, RowlandAndrew

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

Four kinase inhibitors (KIs), dabrafenib, ibrutinib, nintedanib, and trametinib, were potent inhibitors of human liver microsomal UGT1A1. However, in vitro - in vivo extrapolation excluded the likelihood that these KIs would precipitate drug-drug interactions (DDIs) due to their low unbound plasma concentrations. This suggests that while these KIs are potent inhibitors of UGT1A1, they are unlikely to cause significant DDI issues.
Paper Details　
Original Abstract of the Article :
We have demonstrated previously that the kinase inhibitors (KIs) lapatinib, pazopanib, regorafenib and sorafenib are potent inhibitors of UGT1A1 and UGTs 1A7-1A10. The present study characterised the effects of four additional drugs in this class, dabrafenib, ibrutinib, nintedanib and trametinib, on...See full text at original site
Dr.Camel IconDr.Camel's Paper Summary Blogラクダ博士について

ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。

* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。


引用元：
https://doi.org/10.1016/j.bcp.2019.08.018

データ提供：米国国立医学図書館（NLM）

Kinase Inhibitors and UDP-Glucuronosyltransferase (UGT) Enzymes: A Complex Dance

The study of drug interactions is crucial for ensuring safe and effective medication use. This paper explores the potential for drug-drug interactions between kinase inhibitors (KIs), a class of drugs commonly used in cancer treatment, and UDP-glucuronosyltransferase (UGT) enzymes, which play a key role in drug metabolism. The research investigates the inhibitory effects of several KIs on UGT enzyme activity, providing valuable information for clinicians and pharmacists.

Kinase Inhibitors: A Potential Hitch in the Metabolism Highway

The study reveals that several KIs, including dabrafenib, ibrutinib, nintedanib, and trametinib, are potent inhibitors of UGT1A1, a key enzyme involved in drug metabolism. This finding suggests that there is a potential for drug-drug interactions when KIs are used in combination with other medications that are metabolized by UGT1A1. Think of it like a traffic jam on a desert highway - one stalled vehicle can create a domino effect, disrupting the flow of traffic.

Navigating the Desert of Drug Metabolism with Caution

The study emphasizes the importance of careful consideration regarding the potential for drug-drug interactions when using KIs. The researchers recommend further investigation into the potential for interactions between KIs and UGTs, particularly for newly developed agents in this class. It's like a desert traveler navigating a complex maze, carefully considering each step and potential obstacle to ensure a safe journey.

Dr.Camel's Conclusion

This study highlights the importance of understanding drug interactions, particularly when using KIs. The research underscores the need for caution and careful monitoring when using these medications, ensuring safe and effective treatment for patients.

Date :
  1. Date Completed 2020-07-13
  2. Date Revised 2021-12-04
Further Info :

Pubmed ID

31445021

DOI: Digital Object Identifier

10.1016/j.bcp.2019.08.018

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.

This site uses cookies. Visit our privacy policy page or click the link in any footer for more information and to change your preferences.