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QuickView for Lovastatin (compound)
PubChem
| Name: | Lovastatin |
|---|---|
| PubChem Compound ID: | 10574285 |
| Description: | A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver. |
| Molecular formula: | C24H36O5 |
| Molecular weight: | 423.458 g/mol |
DrugBank
Identification
| Name: | Lovastatin |
|---|---|
| Name (isomeric): | DB00227 |
| Drug Type: | small molecule |
| Description: | A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver. |
| Synonyms: |
Lovastatinum [Latin]; Lovastatina [Spanish]; 6 alpha-Methylcompactin; Lovastatine [French]
|
| Brand: | Paschol, Closterol, Mevlor, Lozutin, Monacolin K, Mevinacor, Taucor, Rodatin, Tecnolip, Sivlor, Lipivas, Lipdip, Altocor, Lovastin, Hipolip, Nergadan, Lovasterol, Lovalip, Lipofren, Lestatin, Mevacor, Belvas, Hipovastin, Colevix, Teroltrat, Altoprev, Cholestra, Lovalord, Rovacor, Artein |
| Category: | Antineoplastic Agents, HMG-CoA Reductase Inhibitors, Anticholesteremic Agents, Hydroxymethylglutaryl-CoA Reductase Inhibitors |
| CAS number: | 75330-75-5 |
Pharmacology
| Indication: | 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. |
|---|---|
| Pharmacology: |
The primary cause of cardiovascular disease is atherosclerotic plaque formation. Sustained elevations of cholesterol in the blood increase the risk of cardiovascular disease. Lovastatin lowers hepatic cholesterol synthesis by competitively inhibiting HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step in the cholesterol biosynthesis...
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| Mechanism of Action: |
Lovastatin is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Lovastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind with 20,000 times greater aff...
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| Absorption: | < 5%. Time to peak serum concentration is 2-4 hours. |
| Protein binding: | > 95% |
| Biotransformation: | Undergoes first pass hydrolysis to active metabolites β-hydroxyacid and 6'-hydroxy dervative. |
| 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 |
| Toxicity: | LD50>1000 mg/kg (orally in mice) |
| Affected organisms: | Humans and other mammals |
Interactions
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