Atorvastatin Calcium (Lipitor®)

Jie Jack Li, Douglas S. Johnson, Drago Robert Sliskovic, Bruce David Roth · 2004

Drugs that inhibit the enzyme HMG-CoA reductase (HMGR), the rate-limiting enzyme in cholesterol biosynthesis have become the standard of care for treatment of hypercholesterolemia due to the efficacy, safety and long-term benefits demonstrated in clinical trials employing these agents. Atorvastatin calcium was the first totally synthetic HMGR inhibitor to be developed and marketed as a single enantiomer for lowering cholesterol. Synthesis of racemic atorvastatin and enantioselective syntheses of atorvastatin calcium are discussed.

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