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Extended-release Formulation Attenuates the Impacts of Fluvastatin on Serum PCSK9 Levels in Humans

[ Vol. 14 , Issue. 7 ]

Author(s):

Yuan-Lin Guo, Wei Zhang, Qian Dong, Geng Liu, Cheng-Gang Zhu, Jing Sun, Rui-Xia Xu and Jian-Jun Li*   Pages 837 - 842 ( 6 )

Abstract:


Background: It has been reported that statins therapy can up-regulate PSCK9 expression, which might be associated with the “6% rule” of statins. Additionally, previous data indicated that the extended-release statin could greatly reduce the exposure of statin in circulation. However, whether extended-release statin has less effect on serum PCSK9 level is completely unknown.

Methods: In this randomized, controlled, open-label, prospective study, 61 patients who had not receive any lipid-lowering drugs before were enrolled and assigned to the three groups: immediaterelease fluvastatin 40mg/d, immediate-release fluvastatin 80mg/d and extended-release fluvastatin 80mg/d. Serum PCSK9 levels were measured at baseline and day 3 after treatment.

Results: Serum PCSK9 level was significantly higher on day 3 than that at baseline in all groups (all p=0.0000). Moreover, after 3 days, serum PCSK9 level was significantly higher in immediaterelease fluvastatin 80mg/d group than that in immediate-release fluvastatin 40mg/d group and extended-release fluvastatin 80mg/d group (p=0.011, p=0.007, respectively), while no difference was found between extended-release fluvastatin 80mg/d group and immediate-release fluvastatin 40mg/d group (p=1.000). However, data showed that there was no difference in lipid parameters among groups on day 3.

Conclusion: The data firstly suggested that extended-release fluvastatin had lower impact on serum PCSK9 levels and might be an alternative strategy for attenuating statin-induced elevation on PCSK9.

Keywords:

Proprotein convertase subtilisin/kexin type 9, extended-releasing fluvastatin, immediate-releasing fluvastatin, LDL-C, PCSK9, cardiovascular disease.

Affiliation:

Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, BeiLiShi Road 167, Beijing 100037, Department of Pathology, Beijing Hospital, Beijing 100730, Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, BeiLiShi Road 167, Beijing 100037, Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, BeiLiShi Road 167, Beijing 100037, Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, BeiLiShi Road 167, Beijing 100037, Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, BeiLiShi Road 167, Beijing 100037, Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, BeiLiShi Road 167, Beijing 100037, Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fu Wai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100037

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