Implitapide

Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor. IC50 & Target:MTP^[1] In Vitro: Implitapide suppresses MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC₅₀=10 nM) and inhibit secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) with an IC₅₀ value of 1.1 nM^[1]. In Vivo: Implitapide (3.2 mg/kg/d) significantly reduces the plasma lipid levels to nearly or below the chow diet (CD) level at 4 and 8 weeks of treatment (p<0.01). Implitapide (3.2 mg/kg/d) markedly suppresses 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). 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). Implitapide at a dosage of approximately 3.2 mg/kg/d significantly reduces the lipid-stained aortic lesions by 83% in apoE KO mice^[1].