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Statin Lactonization by Uridine 5'-Diphospho-glucuronosyltransferases (UGTs).

Author: BilosAlbert, RitschelTina, RusselFrans G M, SchirrisTom J J, SmeitinkJan A M

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

Statins are cholesterol-lowering drugs that have proven to be effective in lowering the risk of major cardiovascular events. This study demonstrates for six clinically relevant statins that only UGT1A1, 1A3, and 2B7 contribute significantly to their lactonization. UGT1A3 appeared to have the highest lactonization capacity with marked differences in statin conversion rates: pitavastatin ≫ atorvastatin > cerivastatin > lovastatin > rosuvastatin (simvastatin not converted). Polymorphisms in these regions of UGT1A1, 1A3, and 2B7 may be a contributing factor in statin-induced myopathies.
Paper Details　
Original Abstract of the Article :
Statins are cholesterol-lowering drugs that have proven to be effective in lowering the risk of major cardiovascular events. Although well tolerated, statin-induced myopathies are the most common side effects. Compared to their pharmacologically active acid form, statin lactones are more potent indu...See full text at original site
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引用元：
https://doi.org/10.1021/acs.molpharmaceut.5b00474

データ提供：米国国立医学図書館（NLM）

Understanding Statin Lactonization

[Statins] are widely used medications for [cholesterol reduction]. However, they can also cause [muscle-related side effects]. This research focuses on the [formation of statin lactones], a potential contributor to statin-induced myopathies. The study investigates the [role of uridine 5'-diphospho-glucuronosyltransferases (UGTs)] in this process. The authors identified specific UGT subtypes responsible for statin lactonization and found that [UGT1A1, 1A3, and 2B7 play a significant role].

UGT Subtypes and Statin Lactonization

The study identified specific UGT subtypes that contribute significantly to statin lactonization, particularly UGT1A1, 1A3, and 2B7. This discovery could help personalize statin therapy, potentially reducing the risk of myopathies by considering individual UGT enzyme activity.

Personalized Statin Therapy

Imagine a camel caravan crossing the desert, each camel requiring different amounts of water to thrive. Similarly, individuals may metabolize statins differently based on their UGT enzyme activity. This research highlights the importance of personalized statin therapy, considering individual genetic variations to optimize treatment outcomes and minimize side effects.

Dr.Camel's Conclusion

Like a camel navigating a vast and diverse desert, statin therapy requires careful consideration of individual differences. This research sheds light on the role of specific enzymes in statin metabolism. By understanding these mechanisms, we can tailor statin treatment to each patient's needs, potentially reducing muscle-related side effects and maximizing their benefits.

Date :
  1. Date Completed 2016-09-15
  2. Date Revised 2015-11-02
Further Info :

Pubmed ID

26412035

DOI: Digital Object Identifier

10.1021/acs.molpharmaceut.5b00474

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Languages

English

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