Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H36O5 |
Molecular Weight | 404.5396 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]12[C@H](C[C@@H](C)C=C1C=C[C@H](C)[C@@H]2CC[C@@H]3C[C@@H](O)CC(=O)O3)OC(=O)[C@@H](C)CC
InChI
InChIKey=PCZOHLXUXFIOCF-BXMDZJJMSA-N
InChI=1S/C24H36O5/c1-5-15(3)24(27)29-21-11-14(2)10-17-7-6-16(4)20(23(17)21)9-8-19-12-18(25)13-22(26)28-19/h6-7,10,14-16,18-21,23,25H,5,8-9,11-13H2,1-4H3/t14-,15-,16-,18+,19+,20-,21-,23-/m0/s1
Molecular Formula | C24H36O5 |
Molecular Weight | 404.5396 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019643s085lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021316s031lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20467214
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019643s085lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021316s031lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20467214
Lovastatin is a cholesterol-lowering agent that belongs to the class of medications called statins. Alfred Alberts and his team at Merck discovered it in 1978 after screening only 18 compounds over 2 weeks. The agent, also known as mevinolin, was isolated from the fungi Aspergillus terreus. Research on this compound was suddenly shut down in 1980 and the drug was not approved until 1987. Interesting, Akira Endo at Sankyo Co. (Japan) patented lovastatin isolated from Monascus ruber four months before Merck. Lovastatin was found to be 2 times more potent than its predecessor, mevastatin, the first discovered statin. The primary uses of lovastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease. Lovastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid, a strong inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate. The conversion of HMG-CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol. Lovastatin, as well as some of its metabolites, are pharmacologically active in humans. The liver is the primary site of action and the principal site of cholesterol synthesis and LDL clearance. The involvement of low-density lipoprotein cholesterol (LDL-C) in atherogenesis has been well documented in clinical and pathological studies, as well as in many animal experiments. Epidemiological and clinical studies have established that high LDL-C and low high-density lipoprotein cholesterol (HDL-C) levels are both associated with coronary heart disease. However, the risk of developing coronary heart disease is continuous and graded over the range of cholesterol levels and many coronary events do occur in patients with total cholesterol (Total-C) and LDL-C levels in the lower end of this range. Lovastatin immediate-release tablets have been shown to reduce elevated LDL-C concentrations. LDL is formed from very low-density lipoprotein (VLDL) and is catabolized predominantly by the high-affinity LDL receptor. The mechanism of the LDL-lowering effect of lovastatin immediate-release may involve both reduction of VLDL-C concentration, and induction of the LDL receptor, leading to reduced production and/or increased catabolism of LDL-C.
CNS Activity
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6933445https://www.ncbi.nlm.nih.gov/pubmed/20467214
Curator's Comment: # Alfred Alberts and his team at Merck in 1978
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL402 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3055919 |
0.64 nM [IC50] | ||
Target ID: CHEMBL402 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12405293 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | ALTOPREV Approved Use1.1 Prevention of Coronary Heart Disease In patients without symptomatic coronary heart disease (CHD), but at high risk, Altoprev® is indicated to reduce the risk of: Myocardial infarction; Unstable angina; Coronary revascularization procedures; Coronary Heart Disease. Altoprev is indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower Total-C and LDL-C to target levels. Hyperlipidemia Altoprev is indicated as an adjunct to diet for the reduction of elevated Total-C, LDL-C, Apo B, and TG, and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrickson types IIa and IIb). Launch Date1.01200318E12 |
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Palliative | ALTOPREV Approved Use1.1 Prevention of Coronary Heart Disease In patients without symptomatic coronary heart disease (CHD), but at high risk, Altoprev® is indicated to reduce the risk of: Myocardial infarction; Unstable angina; Coronary revascularization procedures; Coronary Heart Disease. Altoprev is indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower Total-C and LDL-C to target levels. Hyperlipidemia Altoprev is indicated as an adjunct to diet for the reduction of elevated Total-C, LDL-C, Apo B, and TG, and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrickson types IIa and IIb). Launch Date1.01200318E12 |
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Preventing | MEVACOR Approved UseAfter oral ingestion, lovastatin, which is an inactive lactone, is hydrolyzed to the lovastatin acid. This is a principal metabolite and an inhibitor of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, which is an early and rate limiting step in the biosynthesis of cholesterol. Lovastatin has been shown to reduce both normal and elevated low-density lipoprotein cholesterol (LDL-C). Launch Date5.5728E11 |
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Primary | MEVACOR Approved UseTherapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. MEVACOR is indicated as an adjunct to diet for the reduction of elevated total-C and LDL-C levels in patients with primary hypercholesterolemia (Types IIa and IIb***), when the response to diet restricted in saturated fat and cholesterol and to other nonpharmacological measures alone has been inadequate. Launch Date5.5728E11 |
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Secondary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9585793 |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
11.9 ng/mL |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
76.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9585793 |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
83 ng × h/mL |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9585793 |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5% |
40 mg 1 times / day steady-state, oral dose: 40 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
LOVASTATIN ACID plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Disc. AE: Aspartate aminotransferase increased, Alanine aminotransferase increased... AEs leading to discontinuation/dose reduction: Aspartate aminotransferase increased (grade 2-4, 1.3%) Sources: Page: p.1082, 1083Alanine aminotransferase increased (grade 2-4, 1.3%) Gastrointestinal disturbance (0.4%) Rash (0.27%) Myalgia (0.13%) Myopathy (0.27%) Arthralgia (0.13%) Insomnia (0.13%) Weight gain (0.13%) |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
DLT: Creatine phosphokinase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Creatine phosphokinase increased (grade 4, 33.3%) Sources: Page: p.527Aspartate aminotransferase increased (grade 2-3, 33.3%) Alanine aminotransferase increased (grade 2-3, 33.3%) |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
DLT: Creatine phosphokinase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Creatine phosphokinase increased (grade 4, 28.6%) Sources: Page: p.527Aspartate aminotransferase increased (grade 3, 14.3%) Alanine aminotransferase increased (grade 3, 14.3%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Arthralgia | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Insomnia | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Myalgia | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Weight gain | 0.13% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Myopathy | 0.27% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Rash | 0.27% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Gastrointestinal disturbance | 0.4% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Alanine aminotransferase increased | grade 2-4, 1.3% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Aspartate aminotransferase increased | grade 2-4, 1.3% Disc. AE |
80 mg 1 times / day multiple, oral (max) Recommended Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: Page: p.1082, 1083 |
unhealthy, 50 n = 745 Health Status: unhealthy Condition: Hypercholesterolemia Age Group: 50 Sex: M+F Population Size: 745 Sources: Page: p.1082, 1083 |
Alanine aminotransferase increased | grade 2-3, 33.3% DLT |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
Aspartate aminotransferase increased | grade 2-3, 33.3% DLT |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
Creatine phosphokinase increased | grade 4, 33.3% DLT |
10 mg/kg 4 times / day multiple, oral (total daily dose) Highest studied dose Dose: 10 mg/kg, 4 times / day Route: oral Route: multiple Dose: 10 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 6 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 6 Sources: Page: p.527 |
Alanine aminotransferase increased | grade 3, 14.3% DLT |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
Aspartate aminotransferase increased | grade 3, 14.3% DLT |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
Creatine phosphokinase increased | grade 4, 28.6% DLT |
7.5 mg/kg 4 times / day multiple, oral (total daily dose) MTD Dose: 7.5 mg/kg, 4 times / day Route: oral Route: multiple Dose: 7.5 mg/kg, 4 times / day Sources: Page: p.527 |
unhealthy, 56 n = 7 Health Status: unhealthy Condition: Squamous cell carcinoma of the head and neck |Squamous cell carcinoma of the cervix Age Group: 56 Sex: M+F Population Size: 7 Sources: Page: p.527 |
PubMed
Title | Date | PubMed |
---|---|---|
Discovery, biochemistry and biology of lovastatin. | 1988 Nov 11 |
|
Coronary angiographic changes with lovastatin therapy. The Monitored Atherosclerosis Regression Study (MARS). | 1993 Nov 15 |
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Lovastatin augments apoptosis induced by chemotherapeutic agents in colon cancer cells. | 1999 Aug |
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Effect of lipid-lowering strategies on tubular cell biology. | 1999 Jul |
|
Lovastatin-induced apoptosis of human medulloblastoma cell lines in vitro. | 1999 Mar |
|
Lovastatin augments sulindac-induced apoptosis in colon cancer cells and potentiates chemopreventive effects of sulindac. | 1999 Oct |
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Lovastatin inhibits G1/S transition of normal human B-lymphocytes independent of apoptosis. | 1999 Oct 10 |
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Differences in the effects of HMG-CoA reductase inhibitors on proliferation and viability of smooth muscle cells in culture. | 2000 Jun |
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Increased lipid peroxidation in a patient with CK-elevation and muscle pain during statin therapy. | 2000 Nov |
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Rabbit serum paraoxonase 3 (PON3) is a high density lipoprotein-associated lactonase and protects low density lipoprotein against oxidation. | 2000 Oct 27 |
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The cyclin dependent kinase inhibitor p27 and its prognostic role in breast cancer. | 2001 |
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An analysis of nine proprietary Chinese red yeast rice dietary supplements: implications of variability in chemical profile and contents. | 2001 Apr |
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Mevastatin, an HMG-CoA reductase inhibitor, reduces stroke damage and upregulates endothelial nitric oxide synthase in mice. | 2001 Apr |
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Antiviral activity of lovastatin against respiratory syncytial virus in vivo and in vitro. | 2001 Apr |
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Cell cycle-related changes in regulatory volume decrease and volume-sensitive chloride conductance in mouse fibroblasts. | 2001 Apr |
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Rho GTPases are involved in the regulation of NF-kappaB by genotoxic stress. | 2001 Apr 1 |
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Assessing the results: phase 1 hyperlipidemia outcomes in 27 health plans. | 2001 Apr 16 |
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Differential effects of lovastatin treatment on brain cholesterol levels in normal and apoE-deficient mice. | 2001 Apr 17 |
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[Endocrine disease in adrenoleukodystrophy]. | 2001 Feb |
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[Practical questions for the expert]. | 2001 Feb |
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[Statins: a major therapeutic breakthrough]. | 2001 Feb |
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Do HMG-CoA reductase inhibitors affect fibrinogen? | 2001 Feb |
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Mechanisms for cholesterol homeostasis in rat jejunal mucosa: effects of cholesterol, sitosterol, and lovastatin. | 2001 Feb |
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Bimonthly update. Therapy and clinical trials. | 2001 Feb |
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Nitrogen-bisphosphonates block retinoblastoma phosphorylation and cell growth by inhibiting the cholesterol biosynthetic pathway in a keratinocyte model for esophageal irritation. | 2001 Feb |
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Butyrate-induced differentiation of Caco-2 cells occurs independently from p27. | 2001 Feb 23 |
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Rhabdomyolysis secondary to a drug interaction between simvastatin and clarithromycin. | 2001 Jan |
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Molecular effects of HMG-CoA reductase inhibitors on smooth muscle cell proliferation. | 2001 Jan |
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Reduction of LDL cholesterol in patients with primary hypercholesterolemia by SCH 48461: results of a multicenter dose-ranging study. | 2001 Jan |
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The benefits of niacin in atherosclerosis. | 2001 Jan |
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Statins in children: what do we know and what do we need to do? | 2001 Jan |
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New statins and new doses of older statins. | 2001 Jan |
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Statin trials in progress: unanswered questions. | 2001 Jan |
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Low-dose combination therapy with colesevelam hydrochloride and lovastatin effectively decreases low-density lipoprotein cholesterol in patients with primary hypercholesterolemia. | 2001 Jun |
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[Statins do not prevent restenosis after coronary angioplasty: where to go from here?]. | 2001 Mar |
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[Effect of cholesterol deficiency on the membrane fluidity of Jurkat T lymphocytes]. | 2001 Mar |
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Is a statin a statin? | 2001 Mar |
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A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro. | 2001 Mar |
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3-Hydroxy-3-methylglutaryl coenzyme A synthase-1 of Blattella germanica has structural and functional features of an active retrogene. | 2001 Mar 15 |
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Liver regeneration after hepatectomy. | 2001 Mar-Apr |
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New OTC drugs and devices 2000: a selective review. | 2001 Mar-Apr |
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Statin induced myopathy does not show up in MIBI scintigraphy. | 2001 May |
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Revised indications for statin therapies. | 2001 May |
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Statins--similarities and differences. | 2001 May |
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Should all patients with cardiovascular disease receive statin therapy? | 2001 May |
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Long-term administration of the HMG-CoA reductase inhibitor lovastatin in two patients with cholesteryl ester storage disease. | 2001 May |
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Can modulation of endothelial nitric oxide synthase explain the vasculoprotective actions of statins? | 2001 May |
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Air Force/Texas Coronary Atherosclerosis Prevention Study (AFCAPS/TEXCAPS): additional perspectives on tolerability of long-term treatment with lovastatin. | 2001 May 1 |
|
RhoA is activated during respiratory syncytial virus infection. | 2001 May 10 |
|
Lovastatin controls signal transduction in vascular smooth muscle cells by modulating phosphorylation levels of mevalonate-independent pathways. | 2001 May-Jun |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/monograph/lovastatin.html
Lovastatin is administered orally with the evening meal. Maximal daily dose for adults is 80 mg, maximal dose for children is 40 mg.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6933445
HMG-CoA reductase from rat liver microsomes was solubilizes and purified through the second ammonium sulfate precipitation. Prior to use, the enzyme was activated at 37C for 30 min. The reaction mix contained, in 100 uL: 0.14 M potassium phosphate buffer, pH 6.8; 0.18 M KCI; 3.5 mM EDTA, pH 7.0; 10 mM dithiothreitol; bovine serum albumin at 0.1 mg/ml; 0.02 uCi of [14C]HMG-CoA and 0.3 pg of partially purified enzyme (specific activity 100-150 nmol min-1 mg-1) with or without inhibitor. After 5-min incubation at 37C, the reaction was initiated with 0.2 mM NADPH. The reaction was terminated with 20 Al of 5 M HCL. After an additional incubation for 15 min at 370C to allow for complete lactonization of the product, mevalonate, the mixture was passed over a 0.5 X 5 cm column containing 100-200 mesh Bio-Rex, chloride form (Bio-Rad), which was equilibrated with distilled water. With this resin the unreacted [14C]HMG-CoA was adsorbed and the product, [14C]mevalonolactone, was eluted with 3 ml of distilled water directly into scintillation vials. After the addition of 10 ml of Aquasol II, radioactivities of the samples were measured in a scintillation counter. Lovastatin acid inhibited HMG-CoA reductase with Ki of 0.64 nM.
Substance Class |
Chemical
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9LHU78OQFD
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WHO-ATC |
C10AA02
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LIVERTOX |
NBK548670
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WHO-ATC |
C10BA01
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NCI_THESAURUS |
C54679
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WHO-VATC |
QC10BA01
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WHO-VATC |
QC10AA02
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NDF-RT |
N0000000121
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NCI_THESAURUS |
C1655
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NDF-RT |
N0000175589
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6074
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admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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M6914
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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PRIMARY | Merck Index | ||
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CHEMBL503
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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1370600
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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100000092165
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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DTXSID5020784
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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Lovastatin
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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D008148
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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DB00227
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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6472
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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PRIMARY | RxNorm | ||
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C620
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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53232
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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40303
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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9LHU78OQFD
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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758662
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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SUB08604MIG
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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1612
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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75330-75-5
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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2739
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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LOVASTATIN
Created by
admin on Wed Jul 05 22:37:10 UTC 2023 , Edited by admin on Wed Jul 05 22:37:10 UTC 2023
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
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TRANSPORTER -> INHIBITOR | |||
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OFF TARGET->ACTIVATOR |
Kd
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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Related Record | Type | Details | ||
---|---|---|---|---|
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METABOLITE -> PARENT |
CYP3A
PLASMA
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METABOLITE ACTIVE -> PRODRUG |
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METABOLITE -> PARENT |
In Vitro metabolite; CYP3A
IN-VITRO
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Related Record | Type | Details | ||
---|---|---|---|---|
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IMPURITY -> PARENT |
correction factor: for the calculation of content, multiply the peak area of impurity E by 1.6
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
|
PARENT -> IMPURITY |
sum of impurities E and F: not more than twice the area of the principal peak in the chromatogram obtained with reference solution (b) (1.0 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Tmax | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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MAXIMUM TOLERATED DOSE | TOXICITY |
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ORAL BIOAVAILABILITY | PHARMACOKINETIC |
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