Top Gene Interactions
- Metabolism: Lovastatin is hepatically metabolized in which the major active metabolites are the beta-hydroxyacid of lovastatin, the 6'-hydroxy derivative, and two additional metabolites. Route of Elimination: Lovastatin undergoes extensive first-pass extraction in the liver, its primary site of action, with subsequent excretion of drug equivalents in the bile. 83% of the orally administered dose is excreted in bile and 10% is excreted in urine. Half Life: 5.3 hours
- Uses/Sources: For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia. For primary prevention of coronary heart disease and to slow progression of coronary atherosclerosis in patients with coronary heart disease.
- Route of Exposure: Studies suggest that <5% of the oral dose reaches the general circulation as active inhibitors. Time to peak serum concentration is 2-4 hours. Lovastatin undergoes extensive first-pass metabolism so the availability of the drug in the system is low and variable.
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD<sub>50</sub>>1000 mg/kg (orally in mice)
Mechanism of Action
|Target Name||Mechanism of Action||References|
Cellular tumor antigen p53
Cytochrome P450 19A1
Vitamin D3 receptor
Nuclear receptor subfamily 1 group I member 2
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Oxysterols receptor LXR-alpha
Histone deacetylase 2