Drug intelligence / Profile preview

fluvastatin

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Fluvastatin is a fully synthetic small molecule statin (HMG-CoA reductase inhibitor) used to lower cholesterol and prevent cardiovascular disease. It works by competitively inhibiting the enzyme HMG-CoA reductase in the liver, which is the rate-limiting step in cholesterol biosynthesis. This leads to reduced total cholesterol and LDL ("bad") cholesterol levels and modestly increases HDL ("good") cholesterol. Fluvastatin is indicated for hypercholesterolemia and for reducing cardiovascular risk in patients with or at high risk of coronary artery disease, cerebrovascular disease, or peripheral arterial disease. It can also be used in children aged 10–17 years with familial heterozygous hypercholesterolemia[1][2][3]. The drug was patented in 1982 and approved for medical use in 1994[3]. Common side effects include muscle pain (myalgia), headache, joint pain, nausea, indigestion, insomnia; serious adverse events like rhabdomyolysis are rare[1][3]. Compared to other statins it has a lower potential for drug-drug interactions due to its metabolism mainly via CYP2C9 rather than CYP3A4[3].

Brand names
LescolLescol XLLipaxanPrimexin
Other names
氟伐他汀Fluvastatin sodiumFluvastatin-D7Fluvastatin-D-7Fluvastatin-D 7
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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