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High resolution mass spectrometry-based methodologies for identification of Etravirine bioactivation to reactive metabolites: In vitro and in vivo approaches.

Author: AntunesAlexandra M M, CharneiraCatarina, GodinhoAna L A, GriloJorge, JacobCristina C, MarquesM Matilde, MartinsInês L, NunesJoão, OliveiraM Conceição, PereiraSofia A, SilvaDiogo M, SotoKarina

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

Etravirine (ETR), a second-generation NNRTI used to treat HIV infection, can be metabolized into reactive metabolites that form covalent adducts with glutathione and N-acetyl-L-cysteine. These findings suggest that similar reactions may occur with cysteine residues of proteins, supporting a potential role of ETR bioactivation in the onset of its toxic effects.
Paper Details　
Original Abstract of the Article :
Drug bioactivation to reactive metabolites capable of covalent adduct formation with bionucleophiles is a major cause of drug-induced adverse reactions. Therefore, elucidation of reactive metabolites is essential to unravel the toxicity mechanisms induced by drugs and thereby identify patient subgro...See full text at original site
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引用元：
https://doi.org/10.1016/j.ejps.2018.03.026

データ提供：米国国立医学図書館（NLM）

Etravirine: Navigating the Desert of Drug Bioactivation

This research delves into the intricate desert landscape of drug bioactivation, a process where drugs undergo transformations in the body, sometimes leading to unexpected consequences. It's like exploring a vast and complex desert, where the journey of a drug can take unexpected turns. The researchers are particularly interested in etravirine (ETR), a drug used to treat HIV infection. They're trying to identify potentially harmful reactive metabolites that might be formed during ETR's bioactivation process. This is crucial for understanding the drug's safety profile and developing strategies to minimize any potential side effects.

Etravirine: Understanding Its Potential for Toxicity

This research reveals new insights into the bioactivation of etravirine, highlighting the formation of reactive metabolites that could potentially cause adverse effects. This information is valuable for guiding the safe use of this drug and for developing new strategies to minimize potential toxicity. It's like having a roadmap to help us navigate the potential risks and benefits of using this drug effectively.

Living Well with HIV: A Journey of Understanding

This research underscores the importance of understanding the intricate processes that occur when drugs interact with the human body. It's a reminder that even seemingly safe drugs can have unexpected consequences, and ongoing research is crucial for ensuring their safety and effectiveness. It's a journey of continuous learning and adaptation as we navigate the complex desert of drug development and utilization.

Dr. Camel's Conclusion

This research highlights the importance of studying drug bioactivation, a process that can lead to unexpected and potentially harmful outcomes. It's a reminder that the desert of drug development is full of hidden complexities, and ongoing research is essential for ensuring safe and effective therapies.
Date :
  1. Date Completed 2018-09-25
  2. Date Revised 2020-12-09
Further Info :

Pubmed ID

29592839

DOI: Digital Object Identifier

10.1016/j.ejps.2018.03.026

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in preparation
Languages

English

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