Lovastatin

spinqualitylabelsall models Lovastatin, also known as Mevacor Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D 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.

Pharmacokinetics

Statin Hypercholesterolemia at 10mg Dosage Parameter HMGR (Lipitor) Pharmaceutical Drugs (Lescol) Lovastatin (Mevacor) HMG-CoA Reductase (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

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