Reversible increase of the apo CII/apo CIII-1 ratio in the very low density lipoproteins after procetofen treatment in hypertriglyceridemic patients.

Procetofen, a new hypolipidemic drug with a powerful cholesterol and triglyceride lowering activity, was administered to hypertriglyceridemic patients, in an effort to determine the major lipoprotein and apoprotein changes, thus providing an insight of the drug's mechanism of action. The twenty-six selected patients (13 type IIB and 13 type IV) were given 100 mg tid of the compound for 9 weeks. Procetofen lowered triglycerides in plasma (-50%) and in all lipoprotein classes (-30-50%) in both patient groups; an 18% reduction of low density lipoprotein cholesterol levels also occurred in type IIB patients. High density lipoprotein cholesterol generally increased significantly, with a maximum of 11% in type IV patients. Plasma apolipoproteins showed a pattern of changes, characteristic of each hyperlipoproteinemia phenotype, reversible after the end of drug treatment. Apoprotein B decreased 16% in type IIB patients, but was not modified in type IV. Conversely, apoprotein CII increased significantly in the very low density lipoproteins of both groups of treated subjects, with a reduction of CIII-1. These findings support the hypothesis that procetofen may act primarily as a stimulator of the catabolism of triglyceride rich lipoproteins. On the other hand, the significant reduction of total and low density lipoprotein cholesterol levels in type IIB, also indicates that other mechanisms, possibly related to changes in the direct liver secretion of apoprotein B or to remnant removal, may be operative with this new drug.