4-hydroxy Atorvastatin lactone is a metabolite of atorvastatin , an HMG-CoA reductase inhibitor present in formulations that have been used to treat hypercholesterolemia and certain dyslipidemias. Atorvastatin is metabolized by the cytochrome P450 (CYP) isoform CYP3A4 to form 4-hydroxy atorvastatin and 2-hydroxy atorvastatin, which can be interconverted between their acid and lactone forms. Atorvastatin can itself be lactonized to atorvastatin lactone then metabolized by CYP3A4 directly to 4-hydroxy atorvastatin lactone and 2-hydroxy atorvastatin lactone.

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