Better Known as: Mevacor
- Marketed By: Merck & Co.
- Major Indication: Hyperlipidemia & High Cholesterol (Hypercholesterolemia)
- Drug Class: HMGR Inhibitor or Statin
- Date of FDA Approval (Patent Expiration): 1991 (2001)
- 2000 Sales: $520 Million
- Importance: Was the first HMG-CoA Inhibitor. Statins are so ubiquitous, doctors have even suggested handing them out with fast food. See: the article
- See Pharmaceutical Drugs for more information about other drugs and disorders
Mechanism of Action
Lovastatin is rapidly hydrolyzed in vivo into its corresponding b-hydroxyacid, which is an inhibitor of HMG-CoA Reductase (HMGR), a highly regulated enzyme responsible for the committed step in cholesterol synthesis. Lovastatin outcompetes HMG-CoA, the substrate of HMGR, in binding to HMGR.
- ↑ Corsini A, Maggi FM, Catapano AL. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharmacol Res. 1995 Jan;31(1):9-27. PMID:7784310