Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C24H38O6.H3N |
| Molecular Weight | 439.5854 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 8 / 8 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
N.[H][C@]12[C@H](C[C@@H](C)C=C1C=C[C@H](C)[C@@H]2CC[C@@H](O)C[C@@H](O)CC(O)=O)OC(=O)[C@@H](C)CC
InChI
InChIKey=AOIIYQZTRFOGNN-AXHZAXLDSA-N
InChI=1S/C24H38O6.H3N/c1-5-15(3)24(29)30-21-11-14(2)10-17-7-6-16(4)20(23(17)21)9-8-18(25)12-19(26)13-22(27)28;/h6-7,10,14-16,18-21,23,25-26H,5,8-9,11-13H2,1-4H3,(H,27,28);1H3/t14-,15-,16-,18+,19+,20-,21-,23-;/m0./s1
| Molecular Formula | H3N |
| Molecular Weight | 17.0305 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C24H38O6 |
| Molecular Weight | 422.5549 |
| 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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL402 |
0.64 nM [IC50] | ||
Target ID: CHEMBL402 |
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 |
|||
| 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 |
|||
| 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 |
|||
| 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 |
|||
| 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 |
|
| Phase II study of high-dose lovastatin in patients with advanced gastric adenocarcinoma. | 2001 |
|
| The cyclin dependent kinase inhibitor p27 and its prognostic role in breast cancer. | 2001 |
|
| An analysis of nine proprietary Chinese red yeast rice dietary supplements: implications of variability in chemical profile and contents. | 2001 Apr |
|
| The effects of the statins lovastatin and cerivastatin on signalling by the prostanoid IP-receptor. | 2001 Apr |
|
| Mevastatin, an HMG-CoA reductase inhibitor, reduces stroke damage and upregulates endothelial nitric oxide synthase in mice. | 2001 Apr |
|
| A new simvastatin (mevinolin)-resistance marker from Haloarcula hispanica and a new Haloferax volcanii strain cured of plasmid pHV2. | 2001 Apr |
|
| Antiviral activity of lovastatin against respiratory syncytial virus in vivo and in vitro. | 2001 Apr |
|
| Comparative study of HMG-CoA reductase inhibitors on fibrinogen. | 2001 Apr |
|
| Rho GTPases are involved in the regulation of NF-kappaB by genotoxic stress. | 2001 Apr 1 |
|
| Statins are magic when you gotta have heart. | 2001 Apr 16 |
|
| Assessing the results: phase 1 hyperlipidemia outcomes in 27 health plans. | 2001 Apr 16 |
|
| Differential effects of lovastatin treatment on brain cholesterol levels in normal and apoE-deficient mice. | 2001 Apr 17 |
|
| Analysis of 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors using liquid chromatography-electrospray mass spectrometry. | 2001 Apr 25 |
|
| Deterioration of the protein kinase C-K(ATP) channel pathway in regulation of coronary flow in hypercholesterolaemic rabbits. | 2001 Apr 27 |
|
| The widening role of statins: RAS signal transduction and drug-induced cytotoxicity in human leukemia: a commentary to 'interaction of cytosine arabinoside and lovastatin in human leukemia cells'. | 2001 Aug |
|
| Interaction of cytosine arabinoside and lovastatin in human leukemia cells. | 2001 Aug |
|
| Low-dose combination therapy with colesevelam hydrochloride and lovastatin effectively decreases low-density lipoprotein cholesterol in patients with primary hypercholesterolemia. | 2001 Jun |
|
| Effect of lovastatin, an HMG CoA reductase inhibitor, on acute renal allograft rejection. | 2001 Jun |
|
| Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. | 2001 Jun |
|
| Use of statins and the subsequent development of deep vein thrombosis. | 2001 Jun 11 |
|
| Compactin enhances osteogenesis in murine embryonic stem cells. | 2001 Jun 8 |
|
| Recent advances in the biosynthetic studies of lovastatin. | 2001 Mar |
|
| [Statins do not prevent restenosis after coronary angioplasty: where to go from here?]. | 2001 Mar |
|
| [AFCAPS/TexCAPS [The Air Force/Texas Coronary Atherosclerosis Prevention Study]]. | 2001 Mar |
|
| Lovastatin blocks basic fibroblast growth factor-induced mitogen-activated protein kinase signaling in coronary smooth muscle cells via phosphatase inhibition. | 2001 Mar |
|
| [Effect of cholesterol deficiency on the membrane fluidity of Jurkat T lymphocytes]. | 2001 Mar |
|
| Is a statin a statin? | 2001 Mar |
|
| Lovastatin and phenylacetate induce apoptosis, but not differentiation, in human malignant glioma cells. | 2001 Mar |
|
| HMG-CoA reductase inhibitors and P-glycoprotein modulation. | 2001 Mar |
|
| Inhibition of human tumor cell growth in vivo by an orally bioavailable inhibitor of human farnesyltransferase, BIM-46228. | 2001 Mar 1 |
|
| Liver regeneration after hepatectomy. | 2001 Mar-Apr |
|
| New OTC drugs and devices 2000: a selective review. | 2001 Mar-Apr |
|
| The National Service Framework on coronary heart disease: is it sufficiently evidence-based? | 2001 May |
|
| Statin induced myopathy does not show up in MIBI scintigraphy. | 2001 May |
|
| Revised indications for statin therapies. | 2001 May |
|
| What do the statin trials tell us? | 2001 May |
|
| Statins--similarities and differences. | 2001 May |
|
| Should all patients with cardiovascular disease receive statin therapy? | 2001 May |
|
| Long-term administration of the HMG-CoA reductase inhibitor lovastatin in two patients with cholesteryl ester storage disease. | 2001 May |
|
| Plasma concentrations of active lovastatin acid are markedly increased by gemfibrozil but not by bezafibrate. | 2001 May |
|
| The combined effects of novel tocotrienols and lovastatin on lipid metabolism in chickens. | 2001 May |
|
| Can modulation of endothelial nitric oxide synthase explain the vasculoprotective actions of statins? | 2001 May |
|
| Cholesterol ester accumulation: an immediate consequence of acute in vivo ischemic renal injury. | 2001 May |
|
| 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 |
|
| Regulation of sterol regulatory element-binding proteins in hamster intestine by changes in cholesterol flux. | 2001 May 18 |
|
| Lovastatin controls signal transduction in vascular smooth muscle cells by modulating phosphorylation levels of mevalonate-independent pathways. | 2001 May-Jun |
|
| Cost effectiveness of HMG-CoA reductase inhibition in Canada. | 2001 Spring |
Patents
Sample Use Guides
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
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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PARENT -> SALT/SOLVATE |
