Drug intelligence / Profile preview

lomitapide + simvastatin

Development stage
Unknown
Lead developer
Chiesi
Modality
Small Molecules
Administration
Oral
01

Overview

**lomitapide + simvastatin** is a combination therapy involving lomitapide, a microsomal triglyceride transfer protein (MTP) inhibitor, and simvastatin, an HMG-CoA reductase inhibitor (statin). Lomitapide acts by inhibiting MTP, thereby reducing the assembly and secretion of apoB-containing lipoproteins (such as VLDL and LDL), primarily indicated for homozygous familial hypercholesterolemia. Simvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, reducing LDL cholesterol and overall cardiovascular risk. Co-administration increases simvastatin exposure via CYP3A4 inhibition by lomitapide, necessitating dose reductions to minimize myopathy and rhabdomyolysis risk[1][2].

Other names
lomitapide + simvastatin
02

Targets

CYP3A4 (Cytochrome P450 3A4)MTTP (Microsomal triglyceride transfer protein large subunit)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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