CAS 163217-74-1: O-HYDROXY ATORVASTATIN LACTONE

2-Hydroxy atorvastatin lactone, a metabolite of Atorvastatin, is an orally active HMG-CoA reductase inhibitor that efficiently reduces blood lipids [1][2].

2-Hydroxyatorvastatin lactone is a prodrug of atorvastatin, which is an HMG-CoA reductase inhibitor. It is used to lower cholesterol and triglycerides in the blood. The drug is administered as a tablet, capsule, or liquid and can be taken with or without food. 2-Hydroxyatorvastatin lactone is metabolized by cytochrome P450 enzymes in the liver to produce active atorvastatin. This metabolism may be inhibited by other drugs that are also metabolized by cytochrome P450 enzymes, such as erythromycin and ketoconazole. 2-Hydroxyatorvastatin lactone has been shown to have an inhibition constant (Ki) of 0.5 μM for human liver microsomes and plasma concentrations of 1 μM or higher are required for therapeutic effect.