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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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

Author(s): Yuan-Lin Guo, Wei Zhang, Qian Dong, Geng Liu, Cheng-Gang Zhu, Jing Sun, Rui-Xia Xu and Jian-Jun Li*

Volume 14 , Issue 7 , 2017

Page: [837 - 842] Pages: 6

DOI: 10.2174/1570180814666161216121558

Price: $65


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.

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