Abstract
Purpose: To investigate the frequency of gene CYP2C9 *3 in Chinese populations, and to analyze the impact of CYP2C9 *3 genetic polymorphism on the cholesterol-lowering effect of fluvastatin in a Chinese hyperlipidemic population. Methods: CYP2C 9 genotype was determined by polymerase chain reaction - restriction fragment length polymorphism (PCR - RFLP) in 270 unrelated hyperlipidemic patients who were treated with 80mg fluvastatin monotherapy daily for 4 weeks and 250 healthy controls. Clinical data were collected prior to treatment with fluvastatin and 4 weeks after. Results: In 270 hyperlipidemic patients, the frequency of CYP2C9 *3 was 3.70 % which is significantly higher than in 250 healthy controls (2.60 %) ( p < 0.01). After oral intake of fluvastatin 80 mg daily for 4 weeks, CYP2C9 *1/*3 genotype was associated with a decrease in LDL-C levels (by 33.9 % in CYP2C9 *1/*3 versus 24.5 % for CYP2C9 *1/*1, p < 0.05) and with reduction of TC (by 36.4 % in CYP2C9 *1/*3 versus 19.4 % in CYP2C9 *1/*1, p < 0.05). Conclusion: The frequency of CYP2C9 *3 is 3.17 % in Chinese populations, and those who carry CYP2C9 *3 mutation have a high risk of hyperlipidemia. CYP2C9 *3 seems to increase the lipid-lowering effects of fluvastatin. Keywords: Hyperlipidemia, Gene, CYP2C9 , Polymorphism, Polymerase chain reaction, Restriction fragment length polymorphism, Fluvastatin
Highlights
Hypercholesterolemia plays a key role in the development of atherosclerotic disease
Genetic polymorphisms of CYP enzymes are an important source of interindividual variation in drug metabolism [4]
Fluvastatinis metabolized primarily by CYP2C9 [7], there may be an association between CYP2C9 polymorphisms and the lipid-lowering efficacy of fluvastatin
Summary
Hypercholesterolemia plays a key role in the development of atherosclerotic disease. Statins are known to reduce cardiovascular morbidity and mortality. There is a wide interindividual variation in response to statin therapy. Genetic polymorphisms of CYP enzymes are an important source of interindividual variation in drug metabolism [4]. CYP2C9 is an important enzyme, and several drugs are metabolized by it, e.g., fluvastatin, simvastatin, losartan and warfarin [4,5]. The polymorphisms of CYP2C9 may be have an effect on the above drugs’ therapeutic efficacy. Any predictions of biological response of individuals to statins would be very valuable for more efficacious, personalized treatments. Individuals who carry CYP2C9*3 gene may have reduced enzyme activity [6]. Fluvastatinis metabolized primarily by CYP2C9 [7], there may be an association between CYP2C9 polymorphisms and the lipid-lowering efficacy of fluvastatin
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