Apolipoprotein A-I Synthesis Inducer Moderately SuApolipoprotein A-I Synthesis Inducer Moderately Successful
Last Updated: January 21, 2011.
Administration of a novel oral inducer of apolipoprotein A-I(apoA-I) synthesis appears to result in increases of apoA-I levels andhigh-density lipoprotein cholesterol, according to research publishedonline Jan. 19 in the Journal of the American College of Cardiology.
FRIDAY, Jan. 21 (HealthDay News) -- Administration of a noveloral inducer of apolipoprotein A-I (apoA-I) synthesis appears to resultin increases of apoA-I levels and high-density lipoprotein (HDL)cholesterol, according to research published online Jan. 19 in the Journal of the American College of Cardiology.
Stephen J. Nicholls, M.B.B.S., Ph.D., of the Cleveland Clinic, andcolleagues randomized 299 statin-treated coronary artery diseasepatients to RVX-208 or placebo for 12 weeks to investigate the effect ofthe new drug on lipid-related biomarkers as well as its safety andtolerability.
The researchers found that there were no statistically significantdifferences between the two groups in comparisons of apoA-I synthesis,but a dose-dependent increase in apoA-I levels of up to 5.6 percent wasseen in the treatment group, which also experienced significantincreases in HDL cholesterol and large HDL particles. Rapid increases inapoA-I levels were seen in the last four weeks of the trial, suggestingpeak pharmacological effect had not yet been achieved. In 18 patients,there were transient and reversible elevations in liver transaminasesmore than three times the upper limit of normal; these were not relatedto an increase in bilirubin levels.
"Administration of RVX-208 for 12 weeks was associated with increasesin apoA-I, HDL cholesterol, and concentration of large HDL particles,consistent with facilitation of cholesterol mobilization. Maximalincreases in apoA-I may require longer exposure. An increase in liverenzymes was observed with active treatment," the authors write.
Several authors disclosed financial relationships with pharmaceuticalcompanies and/or medical device companies, including ResverlogixCorporation, which focuses on developing novel small molecules thatenhance apoA-I.