Lovastatin (洛伐他汀) 是高效HMG-CoA还原酶抑制剂,IC50为3.4 nM,有降血脂作用。
Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM, used for lowering cholesterol (hypolipidemic agent). Decreases CDK2, 4, 6 and cyclin E levels and induces G1 arrest and apoptosis in tumor cell lines in vitro. Inactive lactam prodrug of lovastatin hydroxy acid, naturally bioactivated in vivo.
30% PEG400+0.5% Tween80+5% propylene glycol
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Pahan K, et al. J Clin Invest, 1997, 100(11), 2671-2679.
[2] Mendola, C.E. and Backer, J.M. 1990. Cell Growth Differ. 1: 499-502.
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[4] Rubins, J.B., et al. 1998. Am. J. Respir. Crit. Care Med. 157: 1616-1622.
[5] Bobek, P., et al. 1998. Nutrition. 14: 282-286.
[6] Kim, W.S., et al. 2001. Invest New Drugs. 19: 81-83.
分子式 C24H36O5 |
分子量 404.54 |
CAS号 75330-75-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mg/mL |
Water <1 mg/mL |
Ethanol 10 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00285857 | Breast Cancer | Drug: Lovastatin | Stanford University | Phase 2 | 2005-11-01 | 2017-01-19 |
NCT00580970 | Prostate Cancer | Drug: lovastatin | Virginia Commonwealth University|Hunter Holmes Mcguire Veteran Affairs Medical Center | Phase 2 | 2007-04-01 | 2016-09-28 |
NCT00585052 | Ovarian Cancer | Drug: Lovastatin and Paclitaxel | University of Iowa | Phase 2 | 2003-08-01 | 2010-12-20 |
NCT01527669 | Healthy Subjects | Drug: LipoCol Forte capsules|Drug: Lovastatin Tablet | National Taiwan University Hospital|National Science Council, Taiwan | Phase 4 | 2012-02-01 | 2012-07-09 |
NCT01478828 | Prostate Cancer | Drug: Lovastatin | Sidney Kimmel Comprehensive Cancer Center | 2012-03-01 | 2015-10-13 | |
NCT01346670 | Healthy Volunteer | Drug: LipoCol and Mevacor | Taipei Medical University WanFang Hospital | Phase 4 | 2006-10-01 | 2011-05-01 |
NCT00963664 | Melanoma|Malignant Melanoma | Drug: lovastatin|Drug: interferon alfa-2b | NeoPlas Innovation | Phase 2 | 2009-12-01 | 2009-09-04 |
NCT00700921 | Chronic Obstructive Pulmonary Disease (COPD) | Drug: Lovastatin|Drug: Placebo | National Jewish Health|National Heart, Lung, and Blood Institute (NHLBI) | Phase 2 | 2008-04-01 | 2012-11-26 |
NCT00302952 | Rheumatoid Arthritis | Drug: Lovastatin|Drug: Placebo | National Institute of Allergy and Infectious Diseases (NIAID)|Autoimmunity Centers of Excellence | Phase 2 | 2006-08-01 | 2016-09-13 |
NCT02642653 | Fragile X Syndrome|Genetic Diseases | Drug: Lovastatin|Drug: Placebo | Randi J. Hagerman, MD|University of California, Davis | Phase 4 | 2016-01-01 | 2016-10-24 |
NCT00352599 | Neurofibromatosis 1 | Drug: Lovastatin|Drug: Lovastatin|Drug: placebo pill | University of California, Los Angeles | Phase 1 | 2009-09-01 | 2016-11-18 |
NCT00584012 | Any Cancer|Breast Cancer | Drug: Lovastatin and Docetaxel | University of Iowa | Phase 1|Phase 2 | 2004-04-01 | 2009-06-18 |
NCT02603770 | Lipid Metabolism Disorder | Drug: XueZhiKang|Drug: Lovastatin | Luye Pharma Group Ltd. | Phase 1 | 2015-11-01 | 2016-12-02 |
NCT00583102 | Acute Myeloid Leukemia | Drug: Lovastatin and Cytarabine | University of Iowa | Phase 1|Phase 2 | 2001-06-01 | 2010-12-20 |
NCT01110642 | Syndromic Ichthyoses|CHILD Syndrome|Smith Lemli Opitz Syndrome|Conradi Syndrome | Drug: Lovastatin | Northwestern University | Phase 2 | 2011-07-01 | 2015-05-15 |
NCT00243880 | Stroke | Drug: lovastatin | Columbia University | Phase 1 | 2005-09-01 | 2016-05-05 |
NCT00689806 | Severe Persistent Asthma | Drug: Lovastatin|Drug: Placebo | University of Chicago | Phase 1|Phase 2 | null | 2013-06-20 |
NCT00462280 | Precancerous Condition|Stage 0 Melanoma|Stage I Melanoma|Stage II Melanoma | Drug: lovastatin|Other: placebo|Procedure: biopsy|Procedure: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2007-05-01 | 2014-10-24 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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