Drug intelligence / Profile preview

2-hydroxy atorvastatin

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
01

Overview

**2-hydroxy atorvastatin** is a primary active metabolite of atorvastatin, a member of the statin class (HMG-CoA reductase inhibitors) used principally for lowering lipid levels and reducing cardiovascular risk. Like atorvastatin, this metabolite acts by competitively inhibiting the HMG-CoA reductase enzyme, thus reducing cholesterol biosynthesis in hepatocytes—including lower LDL-C and total cholesterol—as well as pleiotropic effects related to vascular protection. 2-hydroxy atorvastatin is formed in vivo by CYP3A metabolism of atorvastatin and is pharmacologically active, contributing significantly to the lipid-lowering effect seen with atorvastatin therapy. It has been investigated in vitro for neuroprotective effects and continues to be used primarily as a research compound rather than an approved drug for medical use[2][5][6].

Other names
2-hydroxy atorvastatino-hydroxyatorvastatin2-hydroxyatorvastatin calciumo-hydroxyatorvastatin dihydrate monosodium salt(3R,5R)-7-[3-(2-hydroxyphenylcarbamoyl)-5-(4-fluorophenyl)-2-isopropyl-4-phenyl-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid calciumAKOS025394527AKOS-025394527AKOS 0253945272-hydroxy atorvastatin calcium salt214217-86-4265989-46-62-hydroxyatorvastatin dihydrate monosodium salt
02

Targets

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

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