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].

Administering Implitapide (3.2 mg/kg/d) significantly inhibits lipid-stained lesions in mice on a Western-type diet (WD), reducing lesion area by 83% compared to the WD group (p<0.01) and substantially lowering plasma lipid levels to near or below those on a chow diet (CD) at both 4 and 8 weeks of treatment (p<0.01). Furthermore, this dosage of Implitapide markedly reduces lipid-stained aortic lesions by 83% in apoE knockout (KO) mice. In addition, apoE KO mice fed a WD supplemented with varying doses of Implitapide (1, 5, and 15 mg/kg/d) for 14 weeks exhibit a significant decrease in both plaque area (66, 78, and 93% reduction, respectively) and lipid content within plaques (to 4.3, 2.6, and 0%, respectively, compared with 9.5% in controls)[1].