The results of animal studies with ciprofibrate, a new orally effective hypolipidemic drug.
Findings are given to show that ciprofibrate, a new orally active phenoxyisobutyrate, is significantly more hypolipidemic than is the reference clofibrate. In hyperlipidemic rats ciprofibrate suppresses the increase in blood lipids 33% at a daily dosage of 0.6--3 mg/kg. The corresponding dosage for clofibrate is 125--460 mg/kg. Based on studies with cholesterol pools pre-labeled with [14C]mevalonate or with cholesterol-labeled pools in ciprofibrate-treated normolipidemic rats, ciprofibrate was shown to inhibit cholesterol biosynthesis. No evidence of the presence of 7- or 24-dehydrocholesterol was obtained in the sera of ciprofibrate-treated rats as shown by gas chromatography examination. The order of hypolipidemic effectiveness of ciprofibrate in hyperlipidemic rats provides a basis for anticipating that ciprofibrate will be hypolipidemic in hyperlipoproteinemic subjects who are considered at high risk of acquiring coronary artery disease.
D000284:Administration, Oral; D000818:Animals; D000924:Anticholesteremic Agents / Q000627:therapeutic use; D002784:Cholesterol / Q000096:biosynthesis / Q000097:blood; D002994:Clofibrate / Q000031:analogs & derivatives* / Q000627:therapeutic use; D003521:Cyclopropanes / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D058607:Fibric Acids; D006949:Hyperlipidemias / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D008297:Male; D051381:Rats; D014280:Triglycerides / Q000037:antagonists & inhibitors / Q000097:blood
D000924:Anticholesteremic Agents; D003521:Cyclopropanes; D058607:Fibric Acids; D000960:Hypolipidemic Agents; D014280:Triglycerides; D002784:Cholesterol; C019304:ciprofibrate; D002994:Clofibrate