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Intracellular pharmacokinetics of gemcitabine, its deaminated metabolite 2',2'-difluorodeoxyuridine and their nucleotides.

Author: BeijnenJos H, DerissenEllen J B, HuitemaAlwin D R, RosingHilde, SchellensJan H M

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study examined the intracellular pharmacokinetics of gemcitabine and its metabolites, including 2',2'-difluoro-2'-deoxyuridine (dFdU) nucleotides. While gemcitabine diphosphate and triphosphate are considered responsible for its antineoplastic effects, dFdU nucleotides may also contribute to the antitumor effects, suggesting that further research on their role is warranted.
Paper Details　
Original Abstract of the Article :
Gemcitabine (2',2'-difluoro-2'-deoxycytidine; dFdC) is a prodrug that has to be phosphorylated within the tumour cell to become active. Intracellularly formed gemcitabine diphosphate (dFdCDP) and triphosphate (dFdCTP) are considered responsible for the antineoplastic effects of gemcitabine. However,...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5980516/

データ提供：米国国立医学図書館（NLM）

Intracellular Pharmacokinetics of Gemcitabine: Unveiling the Mechanisms of Action

The field of [pharmacology] constantly seeks to unravel the complex mechanisms of [drug action] within the body. This research investigates the [intracellular pharmacokinetics] of [gemcitabine], a [chemotherapy drug] used to treat various types of [cancer]. The authors explore the [cellular pathways] involved in the [activation] and [metabolism] of [gemcitabine], specifically focusing on the formation of its [active metabolites] and their potential role in [cancer cell death].

The Molecular Dance of Gemcitabine

The study reveals the intricate [intracellular pharmacokinetics] of [gemcitabine] and its [deaminated metabolite] [2',2'-difluorodeoxyuridine (dFdU)]. The researchers found that both [gemcitabine] and [dFdU] are [phosphorylated] within the cell, resulting in the formation of their respective [nucleotides]. These findings provide a deeper understanding of how [gemcitabine] exerts its [antitumor effects] at the cellular level.

Unraveling the Secrets of Cancer Treatment

This research sheds light on the complex dance of [drug metabolism] within cancer cells. By understanding the [intracellular pharmacokinetics] of [gemcitabine], we may be able to develop [more effective] and [targeted therapies] for [cancer]. Just as a camel navigates the desert by understanding the patterns of water sources, we can learn to target cancer cells by understanding their unique metabolic pathways.

Dr. Camel's Conclusion

This research delves into the molecular dance of gemcitabine within cancer cells. By understanding the intracellular pharmacokinetics of this drug, we can potentially refine treatment strategies and develop more effective cancer therapies.

Date :
  1. Date Completed 2019-06-24
  2. Date Revised 2022-12-07
Further Info :

Pubmed ID

29451684

DOI: Digital Object Identifier

PMC5980516

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Languages

English

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