LDL-C Lowering Of Pitavastatin Equivalent To Other Statins But Effect On HDL-C And Triglycerides Superior

Date: Jun-14-2012Two papers published in the European Journal of Preventive Cardiology (1,2) complete
the publication of data from the pitavastatin development programme by
Japanese-headquartered company, Kowa.

Kowa now has clinical study data from nearly 25,000 patients for its novel and potent statin, pitavastatin, showing its efficacy and pharmacokinetics are consistent across the
world. The last tranche of primary data show pitavastatin is as effective as other
commonly used statins at lowering low density lipoprotein cholesterol (LDL-C), with
excellent tolerability. (3,4,5,6,7)

Pitavastatin is also effective at elevating high density lipoprotein (HDL-C) levels,
reducing triglyceride (TG) levels, (8,5) and appears to have less effect on glycaemic
control, (3) than some other statins.

Comparisons to simvastatin in patients with dyslipidemia at high risk of coronary
heart disease showed the two statins to be equivalent. In one study, 355 patients were
randomised between pitavastatin and simvastatin: both drugs were equally effective at
reducing LDL-C but pitavastatin increased HDL-C by 6.8%, compared to 4.5% in the
simvastatin arm, and was better than simvastatin at reducing triglycerides (TG). (5) This
may make pitavastatin a good choice for the management of dyslipidemic patients at high
cardiovascular risk.

An extension of this study over 44 weeks showed that pitavastatin's effects were
sustained and while both treatments were generally well tolerated, fewer pitavastatin
patients stopped treatment because of adverse events, although this was not statistically
significant. (4)

Another head to head comparison, in 857 patients with either primary
hypercholesterolaemia or combined dyslipidemia, showed that pitavastatin was superior to
simvastatin in terms of percentage reduction of LDL-C, at lower doses (pitavastatin 2
mg/day v. simvastatin 20 mg/day) and proved to be equivalent to simvastatin in percentage
reduction of LDL-C at higher-doses (pitavastatin 4 mg/day v. simvastatin 40 mg/day). (6)
Comparisons to atorvastatin showed reductions in LDL-C were not significantly
different between the two treatments and attainment of National Cholesterol Education
Program (NCEP) and European Atherosclerosis Society targets for LDL-C was similarly high
for both treatment groups.(3,7) Both treatments were well tolerated, including in patients
with diabetes, but atorvastatin increased fasting blood glucose in patients with diabetes
from baseline (+7.2%; p(3)

A comparison of the full range of doses of pitavastatin (1, 2, 4 mg) against the
lowest doses of the best tolerated statin, pravastatin (10, 20, 40 mg) in elderly patients
showed pitavastatin was as well tolerated as pravastatin. Differing clinical outcomes were
observed: pitavastatin was statistically, significantly better than pravastatin for all
comparisons in total cholesterol and Apo-B reduction, in the medium- and high-dose group
for HDL-C elevation, and in the low- and high-dose groups for TG reduction. (1)

This study was extended for 60 weeks to assess the safety and tolerability of
pitavastatin 2 mg once daily or 4 mg if required. The majority of patients attained NCEP
treatment targets on the 2 mg dose and only 17% required up titration to 4 mg daily.(2)
Only 15.6% subjects discontinued treatment during this time, but only half of them because
of adverse events.(2) There were no cases of severe myalgia, myopathy, myositis or
rhabdomyolysis, and no significant findings on urinalysis, vital signs or 12-lead ECG.(2)

Other safety and tolerability studies of pitavastatin at its highest dose, 4 mg, show
that efficacious LDL-C lowering is not associated with treatment- limiting side
effects.(8) In a study of 1,353 patients the reduction in LDL-C levels seen during
double-blind studies was sustained, while HDL-C levels rose continually during follow up,
ultimately increasing by 14.3% over the initial baseline at 52 weeks. (8) Changes in other
lipid parameters (TG, total cholesterol, non-HDL-C, Apo-A1 and Apo-B, high sensitivity
C-reactive protein, oxidised LDL) and ratios (total cholesterol: HDL-C, non-HDL-C:HDL-C
and Apo-B:Apo-A1) were sustained during 52-weeks treatment.(8)

Pitavastatin was well tolerated: only 4.1% of patients withdrew from the study because
of side effects and none of the serious adverse events were considered treatment-related.(8)

About LIVAZO

LIVAZO (pitavastatin) is a HMG-CoA reductase inhibitor indicated for patients with
primary hyperlipidemia and mixed dyslipidemia as an adjunctive therapy to diet to reduce
elevated TC, LDL-C, Apo B, TG, and to increase HDL-C. LIVAZO is predominantly metabolized
via glucuronidation and is only minimally metabolized by CYP system, which may help reduce
its potential for CYP-mediated drug-drug interactions.

LIVAZO, also known as LIVALO and ALIPZA in some markets, has been available in Japan
since 2003 and is available in South Korea, Thailand, China, Taiwan, the US, Portugal,
Spain, Lebanon, Mexico, and Indonesia. It is approved in Australia and an application for
licence has been filed in Central and South America.

View drug information on Livalo.
Courtesy: Medical News Today Note: Any medical information available in this news section is not intended as a substitute for informed medical advice and you should not take any action before consulting with a health care professional.