Chemical Name: N-(2,2,2-Trifluoroethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide methanesulfonate
Biological ActivityLomitapide mesylate is a potent inhibitor of microsomal triglyceride transfer protein (IC50 = 8 nM). Lomitapide inhibits or normalizes lipoprotein production in rodents and in a rabbit model of hypercholesterolemia. Lomitapide is antimalarial; it inhibits hemozoin formation and growth of CQ-sensitive (PfNF54) and multidrug-resistant (PfK1) strains of P. falciparum (IC50 values are 0.56 µM and 0.69 µM respectively). Orally bioavailable.
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