Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).

Implitapide inhibits MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC50=10 nM). Implitapide also inhibits the secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) (IC50: 1.1 nM)[1].

Implitapide (3.2 mg/kg/d) markedly inhibits lipid-stained lesions in the mice fed the western-type diet (WD). Implitapide (3.2 mg/kg/d) significantly decreases lesion area by 83% compared with that of the WD group (p<0.01). Implitapide (3.2 mg/kg/d) significantly decreases the plasma lipid levels to nearly or below the chow diet (CD) level at 4 and 8 weeks of treatment (p<0.01). Implitapide at a dosage of approximately 3.2 mg/kg/d significantly reduces the lipid-stained aortic lesions by 83% in apoE KO mice. ApoE KO mice fed a WD containing Implitapide (1, 5, and 15 mg/kg/d) for 14 weeks have been shown to reduce significantly both plaque area (by 66, 78, and 93%, respectively) and lipid moieties within plaque (4.3, 2.6, and 0%, respectively, versus 9.5% in controls)[1].