Drug intelligence / Profile preview

simvastatin + extended-release niacin

Development stage
Approved
Lead developer
Abbott
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Simvastatin + extended-release niacin is a fixed-dose oral combination of two lipid-altering agents used to treat dyslipidemia. Simvastatin is an HMG-CoA reductase inhibitor (statin) that lowers cholesterol by inhibiting the enzyme responsible for cholesterol synthesis in the liver. Extended-release niacin (nicotinic acid or vitamin B3) reduces cholesterol and triglyceride levels by decreasing hepatic synthesis of very-low-density lipoprotein (VLDL), which leads to reduced low-density lipoprotein (LDL) and increased high-density lipoprotein (HDL). The combination was developed as an adjunct to diet for patients with primary hypercholesterolemia or mixed dyslipidemia who did not achieve adequate lipid control with statins alone. Clinical studies showed greater improvements in non-HDL-C, HDL-C increase, and triglyceride reduction compared to simvastatin monotherapy. However, it has been discontinued in the United States due to lack of additional benefit over statins alone and increased risk of adverse effects such as myopathy[1][2][3][4][5][6].

Brand names
Simcor
Other names
niacin/simvastatinniacin extended-release/simvastatinsimvastatin and niacinsimcor
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)HCAR2 (Hydroxycarboxylic acid receptor 2)

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