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LC-ESI-MS/MS reveals the formation of reactive intermediates in brigatinib metabolism: elucidation of bioactivation pathways.

Author: AttwaMohamed W, DarwishHany W, KadiAdnan A

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

Overview

Brigatinib (BGB) is an ALK inhibitor approved for metastatic anaplastic lymphoma kinase-positive non-small cell lung cancer. This study investigated the in vitro phase I metabolism of BGB in rat liver microsomes. Four metabolites were identified, including three iminium reactive metabolites. The bioactivation of BGB was attributed to the piperidine ring, and the presence of these reactive metabolites may contribute to BGB's side effects, which include nausea, fatigue, and elevated liver enzymes. This study provides valuable insights into the metabolism of BGB and its potential for bioactivation.
Paper Details　
Original Abstract of the Article :
Brigatinib (BGB) is a newly approved anaplastic lymphoma kinase (ALK) inhibitor. On April 28, 2017, BGB was approved by the U.S. FDA for the treatment of metastatic anaplastic lymphoma kinase-positive non-small cell lung cancer. The toxicity profile of BGB includes nausea, fatigue, diarrhea, elevate...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9077137/

データ提供：米国国立医学図書館（NLM）

Brigatinib: Exploring Its Metabolic Pathways and Side Effects

This research sheds light on the [pharmacokinetics] of [brigatinib], a [cancer drug], and its potential [side effects]. Using [LC-MS/MS], the researchers investigated the [metabolism] of [brigatinib] in [rat liver microsomes]. They discovered that [brigatinib] can form [reactive intermediates] that may contribute to its [side effects].

The Hidden Side of Brigatinib: Understanding Its Metabolism and Side Effects

This study reveals that brigatinib, a cancer drug, undergoes a complex metabolic process involving the formation of reactive intermediates. These reactive intermediates may play a role in the observed side effects of the drug, highlighting the importance of understanding drug metabolism for optimizing safety and efficacy.

Navigating the Desert of Drug Metabolism

The metabolism of medications can be a complex and intricate process. This study exemplifies how a drug like brigatinib can undergo transformation in the body, leading to the formation of potentially harmful byproducts. It's essential to be aware of these metabolic pathways to understand the potential side effects of medications and make informed decisions about our healthcare.

Dr.Camel's Conclusion

This research provides a peek into the intricate world of drug metabolism and its potential impact on side effects. Understanding these complex processes is crucial for ensuring patient safety and optimizing the effectiveness of medications.
Date :
  1. Date Completed n.d.
  2. Date Revised 2022-05-12
Further Info :

Pubmed ID

35540908

DOI: Digital Object Identifier

PMC9077137

Related Literature

Article Analysis
・Side Effects of brigatinib
SNS
PICO Info
in preparation
Languages

English

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