Lovastatin

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.

spinqualitylabelsall models Lovastatin, also known as Mevacor Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Pharmacokinetics

Statin Pharmacokinetics at 10mg Dosage Parameter Atorvastatin (Lipitor) Fluvastatin (Lescol) Lovastatin (Mevacor) Simvastatin (Zocor) Rosuvastatin (Crestor) Cerivastatin (Baycol) Tmax (hr) 2.5 1 3 1.5 4 1.5 Cmax (ng/ml) 27-66 448 10-20 7.3 4.34 3.43 Bioavailability (%) 12 19-29 5 5 20 60 Protein Binding (%) 80-90 99 95 95 88 99 T1/2 (hr) 15-30 2 3 2.7 19 2.2 AUC (ng/ml/hr) 104 ~150 33 125 48 14.5 IC50 (nM) 154 198 800 66 320 50-90 Equivalent LDL Reduction Dosage (mg) 10 -- 80 20 5 -- Metabolism Hepatic (CYP3A4) Hepatic (CYP2C9) Hepatic (CYP3A4) Hepatic (CYP3A4) None Hepatic (CYP2C8) For References, See References