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Effects of MK‐733 on plasma lipid and lipoprotein levels in subjects with hypercholesterolaemia
Author(s) -
Simons Leon A.,
Nestel Paul J.,
Calvert G. Dennis,
Jennings Carry L.
Publication year - 1987
Publication title -
medical journal of australia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.904
H-Index - 131
eISSN - 1326-5377
pISSN - 0025-729X
DOI - 10.5694/j.1326-5377.1987.tb133261.x
Subject(s) - placebo , cholesterol , triglyceride , medicine , endocrinology , lipoprotein , pathology , alternative medicine
MK‐733, which is a competitive inhibitor of the rate‐limiting step in cholesterol biosynthesis, or a matching placebo was administered to 30 subjects with primary hypercholesterolaemia (who were already receving dietary treatment) over a period of four weeks in a double‐blind trial. Twenty‐one subjects manifested heterozygous familial hypercholesterolaemia and nine subjects had polygenic hypercholesterolaemia. Five subjects received placebo, 15 subjects a low dose of MK‐733 (2.5‐10 mg/day) and 10 subjects received a high dose of MK‐733 (20‐80 mg/day). Plasma cholesterol levels in subjects who were receiving MK‐733 declined significantly and in a dose‐dependent fashion (31% reduction in plasma cholesterol levels with a high dose, 19% reduction with a low dose). Eight of 10 subjects who were receiving a high dose of MK‐733 achieved better than a 30% reduction in plasma cholesterol levels after four weeks of treatment. The response was independent of the presence or absence of familial hypercholesterolaemia. High‐density lipoprotein cholesterol levels did not change significantly, but there was a suggestive, dose‐dependent reduction in plasma triglyceride levels after four weeks of treatment. MK‐733 was well‐tolerated, appeared to be safe, and may ultimately become an important drug in the management of more severe grades of hypercholesterolaemia.