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Effects of Upadacitinib Coadministration on the Pharmacokinetics of Sensitive Cytochrome P450 Probe Substrates: A Study With the Modified Cooperstown 5+1 Cocktail.

Author: EnejosaJeffrey V, FengTian, FisnikuOgert, MohamedMohamed-Eslam F, OthmanAhmed A

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
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

This study found that upadacitinib, a Janus kinase 1 inhibitor, has a limited effect on CYP3A activity and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. Therefore, no clinically relevant changes in plasma exposures are expected for drugs that are substrates for these CYP enzymes when coadministered with upadacitinib.
Paper Details　
Original Abstract of the Article :
The aim of this study was to characterize the effects of upadacitinib, a Janus kinase 1 inhibitor, on in vivo activity of different cytochrome P450 (CYP) enzymes using a cocktail approach. Healthy subjects (n = 20) received single oral doses of the modified Cooperstown 5+1 cocktail drugs (midazolam ...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6972567/

データ提供：米国国立医学図書館（NLM）

Upadacitinib and Cytochrome P450: A Cocktail Approach

The world of drug interactions is complex and ever-evolving. This study delves into the pharmacokinetic interactions of upadacitinib, a medication used to treat rheumatoid arthritis, with a cocktail of probe substrates that are metabolized by cytochrome P450 (CYP) enzymes. The researchers used a modified Cooperstown 5+1 cocktail approach, a sophisticated methodology for evaluating drug interactions, to assess the impact of upadacitinib on the activity of various CYP enzymes. The study involved 20 healthy subjects who received both the cocktail and upadacitinib, allowing the researchers to observe and measure the effects of the drug on the metabolism of various probe substrates.

A Balancing Act

The findings reveal a fascinating interplay between upadacitinib and CYP enzymes. The study found that upadacitinib, at a dose twice the optimal dose for rheumatoid arthritis, had a limited effect on CYP3A activity, while no significant effects were observed on other CYP enzymes. This careful examination of drug interactions is crucial for ensuring safe and effective medication use.

Navigating Drug Interactions

This research is like a compass guiding us through the complex terrain of drug interactions. The findings suggest that coadministering upadacitinib with other drugs metabolized by CYP enzymes is generally safe, as long as the appropriate dose is used. This information is essential for healthcare professionals who prescribe medication, helping them make informed decisions about drug combinations and dosages.

Dr.Camel's Conclusion

This study emphasizes the importance of understanding the intricate dance between medications and the body's metabolic machinery. The careful examination of drug interactions, like that conducted in this research, is essential for ensuring patient safety and optimizing treatment outcomes. It reminds us that a thorough understanding of pharmacokinetics is crucial for navigating the complex world of medications and ensuring their effectiveness.

Date :
  1. Date Completed 2021-02-03
  2. Date Revised 2021-02-03
Further Info :

Pubmed ID

31378969

DOI: Digital Object Identifier

PMC6972567

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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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