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Identification
NameLovastatin
Accession NumberDB00227  (APRD00370)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Lovastatin is a cholesterol-lowering agent that belongs to the class of medications called statins. It was the second agent of this class discovered. It was discovered by Alfred Alberts and his team at Merck 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. Like mevastatin, lovastatin is structurally similar to hydroxymethylglutarate (HMG), a substituent of HMG-Coenzyme A (HMG-CoA), a substrate of the cholesterol biosynthesis pathway via the mevalonic acid pathway. Lovastatin is a competitive inhibitor of HMG-CoA reductase with a binding affinity 20,000 times greater than HMG-CoA. Lovastatin differs structurally from mevastatin by a single methyl group at the 6’ position. Lovastatin is a prodrug that is activated by in vivo hydrolysis of the lactone ring. It, along with mevastatin, has served as one of the lead compounds for the development of the synthetic compounds used today.

Structure
Thumb
Synonyms
SynonymLanguageCode
(1S,3R,7S,8S,8AR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-(2-(2R,4R)-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl)-1-naphthalenyl (S)-2-methyl-butyrateNot AvailableNot Available
2beta,6alpha-Dimethyl-8alpha-(2-methyl-1-oxobutoxy)-mevinic acid lactoneNot AvailableNot Available
6-alpha-methylcompactinNot AvailableNot Available
6alpha-MethylcompactinNot AvailableNot Available
6α-methylcompactinNot AvailableNot Available
LOVASTATINNot AvailableNot Available
LovastatinaSpanishNot Available
LovastatineFrenchNot Available
LovastatinumLatinNot Available
MevacorNot AvailableNot Available
MevinolinNot AvailableNot Available
MK-803Not AvailableNot Available
ML-530bNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mevacortablet20 mgoralMerck Sharp & Dohme Corp.1987-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Mevacortablet40 mgoralMerck Sharp & Dohme Corp.1987-08-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Altoprevtablet, extended release20 mgoralShionogi Inc.2002-06-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Altoprevtablet, extended release40 mgoralShionogi Inc.2002-06-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Altoprevtablet, extended release60 mgoralShionogi Inc.2002-06-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Lovastatintablet20 mgoralTeva Pharmaceuticals USA Inc2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralTeva Pharmaceuticals USA Inc2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralTeva Pharmaceuticals USA Inc2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralKAISER FOUNDATION HOSPITALS2011-07-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralKAISER FOUNDATION HOSPITALS2011-07-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralKAISER FOUNDATION HOSPITALS2011-07-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralEon Labs, Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralEon Labs, Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralEon Labs, Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralMylan Pharmaceuticals Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralMylan Pharmaceuticals Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralMylan Pharmaceuticals Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2011-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralSTAT Rx USA LLC2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralRebel Distributors Corp2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralRebel Distributors Corp2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralRebel Distributors Corp2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralREMEDYREPACK INC.2011-12-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralAidarex Pharmaceuticals LLC2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralAidarex Pharmaceuticals LLC2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralAidarex Pharmaceuticals LLC2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralLake Erie Medical DBA Quality Care Products LLC2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralRebel Distributors Corp2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralRebel Distributors Corp2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralRebel Distributors Corp2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralAv Kare, Inc.2002-06-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralAv Kare, Inc.2002-06-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralAv Kare, Inc.2002-06-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralPd Rx Pharmaceuticals, Inc.2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralPd Rx Pharmaceuticals, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralAphena Pharma Solutions Tennessee, Llc2002-06-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralActavis Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralActavis Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralActavis Inc.2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2010-10-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2013-07-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2011-06-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2011-09-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2011-10-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2011-03-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2011-03-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2011-10-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2011-12-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2013-05-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2013-11-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralREMEDYREPACK INC.2013-04-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2013-02-13Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2013-05-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2013-11-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralREMEDYREPACK INC.2013-02-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2012-09-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralLake Erie Medical DBA Quality Care Products LLC2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralLake Erie Medical DBA Quality Care Products LLC2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralAv Pak2014-04-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralAv Pak2014-04-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralAv Pak2014-04-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralUnit Dose Services2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralUnit Dose Services2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralUnit Dose Services2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralMylan Institutional Inc.2012-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralMylan Institutional Inc.2012-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralMylan Institutional Inc.2012-11-02Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralNorthwind Pharmaceuticals, LLC2014-11-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralREMEDYREPACK INC.2013-05-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralREMEDYREPACK INC.2013-11-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralREMEDYREPACK INC.2013-09-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralREMEDYREPACK INC.2014-02-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralMutual Pharmaceutical Company, Inc.2006-04-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralMutual Pharmaceutical Company, Inc.2006-04-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralMutual Pharmaceutical Company, Inc.2006-04-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralInternational Labs, Inc.2008-03-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralInternational Labs, Inc.2008-03-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralInternational Labs, Inc.2008-03-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralInternational Labs, Inc.2010-04-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralInternational Labs, Inc.2010-04-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralInternational Labs, Inc.2010-03-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralPhysicians Total Care, Inc.2001-12-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralPhysicians Total Care, Inc.2002-01-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralPhysicians Total Care, Inc.2003-04-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralCardinal Health2011-08-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralCardinal Health2010-12-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralPd Rx Pharmaceuticals, Inc.2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralPd Rx Pharmaceuticals, Inc.2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralGolden State Medical Supply, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralGolden State Medical Supply, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralGolden State Medical Supply, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralGolden State Medical Supply, Inc.2014-06-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralGolden State Medical Supply, Inc.2014-06-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralGolden State Medical Supply, Inc.2014-06-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralSt Marys Medical Park Pharmacy2013-07-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralSt Marys Medical Park Pharmacy2014-01-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralSt Marys Medical Park Pharmacy2014-04-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralCarlsbad Technology, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralCarlsbad Technology, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralCarlsbad Technology, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralDIRECT RX2014-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralDIRECT RX2014-01-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralProficient Rx LP2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralbryant ranch prepack2009-06-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralbryant ranch prepack2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2007-09-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2007-08-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralDispensing Solutions, Inc.2002-11-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralAphena Pharma Solutions Tennessee, Llc2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralAphena Pharma Solutions Tennessee, Llc2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralAphena Pharma Solutions Tennessee, Llc2001-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralBlue Point Laboratories2014-02-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralBlue Point Laboratories2014-02-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralBlue Point Laboratories2014-02-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralAmerican Health Packaging2012-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralAmerican Health Packaging2012-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralAmerican Health Packaging2012-01-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralLupin Pharmaceuticals, Inc.2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralLupin Pharmaceuticals, Inc.2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralLupin Pharmaceuticals, Inc.2007-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralPreferred Pharmaceuticals, Inc.2013-03-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralPreferred Pharmaceuticals, Inc.2013-03-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralPreferred Pharmaceuticals, Inc.2013-03-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet10 mgoralPreferred Pharmaceuticals, Inc2005-10-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralPreferred Pharmaceuticals, Inc2005-10-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralPreferred Pharmaceuticals, Inc2005-10-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralPreferred Pharmaceuticals, Inc.2013-07-25Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet40 mgoralPreferred Pharmaceuticals, Inc.2013-07-29Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Lovastatintablet20 mgoralSanis Health IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Lovastatintablet40 mgoralSanis Health IncNot AvailableNot AvailableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Over the Counter ProductsNot Available
International Brands
NameCompany
AltocorNot Available
Brand mixtures
Brand NameIngredients
Advicorniacin + lovastatin
SaltsNot Available
Categories
CAS number75330-75-5
WeightAverage: 404.5396
Monoisotopic: 404.256274262
Chemical FormulaC24H36O5
InChI KeyPCZOHLXUXFIOCF-BXMDZJJMSA-N
InChI
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
IUPAC Name
(1S,3R,7S,8S,8aR)-8-{2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl}-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl (2S)-2-methylbutanoate
SMILES
[H][C@]12[C@H](C[C@@H](C)C=C1C=C[C@H](C)[C@@H]2CC[C@@H]1C[C@@H](O)CC(=O)O1)OC(=O)[C@@H](C)CC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as delta valerolactones. These are cyclic organic compounds containing an oxan-2- one moiety.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassLactones
Sub ClassDelta valerolactones
Direct ParentDelta valerolactones
Alternative Parents
Substituents
  • Delta_valerolactone
  • Fatty acid ester
  • Delta valerolactone
  • Fatty acyl
  • Oxane
  • Dicarboxylic acid or derivatives
  • Saccharide
  • Secondary alcohol
  • Carboxylic acid ester
  • Oxacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor 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.
PharmacodynamicsThe 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 pathway via the mevalonic acid pathway. Decreased hepatic cholesterol levels causes increased uptake of low density lipoprotein (LDL) cholesterol and reduces cholesterol levels in the circulation. At therapeutic doses, lovastatin decreases serum LDL cholesterol by 29-32%, increases high density lipoprotein (HDL) cholesterol by 4.6-7.3%, and decrease triglyceride levels by 2-12%. HDL cholesterol is thought to confer protective effects against CV disease, whereas high LDL and triglyceride levels are associated with higher risk of disease.
Mechanism of actionLovastatin 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 to form the β-hydroxyacid. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind to HMG-CoA reductase with 20,000 times greater affinity than its natural substrate. The bicyclic portion of lovastatin binds to the coenzyme A portion of the active site.
AbsorptionStudies 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.
Volume of distribution

Lovastatin is able to cross the blood-brain-barrier and placenta.

Protein bindingLovastatin and its β-hydroxyacid metabolites are highly protein bound (>95%).
Metabolism

Lovastatin is hepatically metabolized in which the major active metabolites are the β-hydroxyacid of lovastatin, the 6’-hydroxy derivative, and two additional metabolites.

Route of eliminationLovastatin 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 life5.3 hours
ClearanceNot Available
ToxicityLD50>1000 mg/kg (orally in mice)
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Lovastatin Action PathwayDrug actionSMP00099
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9452
Blood Brain Barrier+0.9287
Caco-2 permeable-0.5484
P-glycoprotein substrateSubstrate0.7861
P-glycoprotein inhibitor IInhibitor0.7046
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.8299
CYP450 2C9 substrateNon-substrate0.8333
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6868
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 substrateNon-inhibitor0.9291
CYP450 2D6 substrateNon-inhibitor0.923
CYP450 2C19 substrateNon-inhibitor0.9026
CYP450 3A4 substrateInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.8475
CarcinogenicityNon-carcinogens0.9519
BiodegradationNot ready biodegradable0.8819
Rat acute toxicity2.0554 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7272
hERG inhibition (predictor II)Non-inhibitor0.7484
Pharmacoeconomics
Manufacturers
  • Andrx labs llc
  • Actavis elizabeth llc
  • Apotex inc
  • Carlsbad technology inc
  • Lupin ltd
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Merck research laboratories div merck co inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral10 mg
Tabletoral20 mg
Tabletoral40 mg
Tablet, extended releaseoral20 mg
Tablet, extended releaseoral40 mg
Tablet, extended releaseoral60 mg
Prices
Unit descriptionCostUnit
Altoprev 60 mg 24 Hour tablet7.99USD tablet
Altoprev 60 mg tablet7.74USD tablet
Altoprev 20 mg 24 Hour tablet6.88USD tablet
Altoprev 20 mg tablet6.61USD tablet
Mevacor 40 mg tablet4.57USD tablet
Altoprev 40 mg tablet4.41USD tablet
Lovastatin 40 mg tablet4.36USD tablet
Altoprev 10 mg 24 Hour tablet3.07USD tablet
Mevacor 20 mg tablet2.53USD tablet
Lovastatin 20 mg tablet2.42USD tablet
Altocor 20 mg 24 Hour tablet2.36USD tablet
Apo-Lovastatin 40 mg Tablet2.11USD tablet
Co Lovastatin 40 mg Tablet2.11USD tablet
Mylan-Lovastatin 40 mg Tablet2.11USD tablet
Novo-Lovastatin 40 mg Tablet2.11USD tablet
Pms-Lovastatin 40 mg Tablet2.11USD tablet
Ran-Lovastatin 40 mg Tablet2.11USD tablet
Ratio-Lovastatin 40 mg Tablet2.11USD tablet
Sandoz Lovastatin 40 mg Tablet2.11USD tablet
Mevacor 10 mg tablet1.65USD tablet
Lovastatin 10 mg tablet1.37USD tablet
Apo-Lovastatin 20 mg Tablet1.14USD tablet
Co Lovastatin 20 mg Tablet1.14USD tablet
Mylan-Lovastatin 20 mg Tablet1.14USD tablet
Novo-Lovastatin 20 mg Tablet1.14USD tablet
Pms-Lovastatin 20 mg Tablet1.14USD tablet
Ran-Lovastatin 20 mg Tablet1.14USD tablet
Ratio-Lovastatin 20 mg Tablet1.14USD tablet
Sandoz Lovastatin 20 mg Tablet1.14USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States59165951997-12-122017-12-12
United States60807781998-03-232018-03-23
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point174.5 °CNot Available
water solubility0.0004 mg/mLNot Available
logP4.26HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.0243 mg/mLALOGPS
logP4.11ALOGPS
logP3.9ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)14.91ChemAxon
pKa (Strongest Basic)-2.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area72.83 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity113.18 m3·mol-1ChemAxon
Polarizability46.11 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Donald F. Gerson, Xinfa Xiao, “Process for the production of lovastatin using Coniothyrium fuckelii.” U.S. Patent US5409820, issued January, 1984.

US5409820
General Reference
  1. Bobek P, Ozdin L, Galbavy S: Dose- and time-dependent hypocholesterolemic effect of oyster mushroom (Pleurotus ostreatus) in rats. Nutrition. 1998 Mar;14(3):282-6. Pubmed
External Links
ATC CodesC10AA02
AHFS Codes
  • 24:06.08
PDB EntriesNot Available
FDA labelDownload (126 KB)
MSDSDownload (99.6 KB)
Interactions
Drug Interactions
Drug
Aluminum hydroxideMay decrease the serum concentration of HMG-CoA Reductase Inhibitors.
AmiodaroneMay decrease the metabolism of HMG-CoA Reductase Inhibitors.
AprepitantMay increase the serum concentration of CYP3A4 Substrates.
AripiprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole.
AtazanavirProtease Inhibitors may increase the serum concentration of Lovastatin.
BatimastatMay increase the serum concentration of Lovastatin.
BezafibrateMay enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors. Bezafibrate may increase the serum concentration of HMG-CoA Reductase Inhibitors. More specifically, bezafibrate may increase the serum concentration of fluvastatin
BoceprevirMay increase the serum concentration of Lovastatin.
BosentanMay increase the metabolism of HMG-CoA Reductase Inhibitors.
Calcium carbonateMay decrease the serum concentration of HMG-CoA Reductase Inhibitors.
ClarithromycinMay increase the serum concentration of Lovastatin.
ColchicineMay enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors. Colchicine may increase the serum concentration of HMG-CoA Reductase Inhibitors.
ConivaptanMay increase the serum concentration of CYP3A4 Substrates.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DanazolMay increase the serum concentration of HMG-CoA Reductase Inhibitors.
DaptomycinHMG-CoA Reductase Inhibitors may enhance the adverse/toxic effect of DAPTOmycin. Specifically, the risk of skeletal muscle toxicity may be increased.
DarunavirProtease Inhibitors may increase the serum concentration of Lovastatin.
DasatinibMay increase the serum concentration of CYP3A4 Substrates.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DelavirdineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
DiltiazemMay increase the serum concentration of Lovastatin. Lovastatin may increase the serum concentration of Diltiazem.
DofetilideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DronedaroneMay increase the serum concentration of Lovastatin.
EfavirenzMay decrease the serum concentration of Lovastatin.
EtravirineMay decrease the serum concentration of HMG-CoA Reductase Inhibitors. This applies to atorvastatin, lovastatin and simvastatin. Conversely, levels of fluvastatin may be increased.
FluconazoleFluconazole may increase the serum concentration of Lovastatin.
FosamprenavirProtease Inhibitors may increase the serum concentration of Lovastatin.
FosaprepitantMay increase the serum concentration of CYP3A4 Substrates.
FosphenytoinMay decrease the serum concentration of HMG-CoA Reductase Inhibitors.
GemfibrozilMay enhance the myopathic (rhabdomyolysis) effect of Lovastatin. Gemfibrozil may increase the serum concentration of Lovastatin. More specifically, gemfibrozil may increase the serum concentrations of lovastatin acid (active form of parent drug).
HydrocodoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Hydrocodone.
IndinavirProtease Inhibitors may increase the serum concentration of Lovastatin.
IsoflurophateMay increase the serum concentration of Lovastatin.
ItraconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
LomitapideMay increase the serum concentration of Lovastatin.
LopinavirProtease Inhibitors may increase the serum concentration of Lovastatin.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
Magnesium oxideMay decrease the serum concentration of HMG-CoA Reductase Inhibitors.
MifepristoneMay increase the serum concentration of Lovastatin.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
NefazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
NelfinavirProtease Inhibitors may increase the serum concentration of Lovastatin.
NiacinMay enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors.
PazopanibHMG-CoA Reductase Inhibitors may enhance the hepatotoxic effect of PAZOPanib. Specifically, the risk for increased serum transaminase concentrations may be increased.
PhenytoinMay decrease the serum concentration of HMG-CoA Reductase Inhibitors.
PimozideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide.
PosaconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
QuinineMay increase the serum concentration of HMG-CoA Reductase Inhibitors.
RaltegravirMay enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors.
RanolazineMay enhance the myopathic (rhabdomyolysis) effect of Lovastatin. Ranolazine may increase the serum concentration of Lovastatin. Ranolazine may also enhance the distribution of lovastatin to specific cells/tissues/organs where P-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.).
RitonavirProtease Inhibitors may increase the serum concentration of Lovastatin.
SaquinavirProtease Inhibitors may increase the serum concentration of Lovastatin.
SildenafilMay decrease the metabolism of HMG-CoA Reductase Inhibitors.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay increase the serum concentration of Lovastatin.
SulfisoxazoleErythromycin (Systemic) may increase the serum concentration of Lovastatin.
TelaprevirMay increase the serum concentration of Lovastatin.
TelithromycinMay increase the serum concentration of Lovastatin.
TicagrelorMay increase the serum concentration of Lovastatin.
TipranavirProtease Inhibitors may increase the serum concentration of Lovastatin.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TrabectedinHMG-CoA Reductase Inhibitors may enhance the myopathic (rhabdomyolysis) effect of Trabectedin.
VerapamilMay increase the serum concentration of Lovastatin.
VoriconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lovastatin.
Food Interactions
  • Avoid alcohol.
  • Avoid drastic changes in dietary habit.
  • Avoid taking with grapefruit juice.
  • Take with food, 50% increase in bioavailability when taken with food.

Targets

1. 3-hydroxy-3-methylglutaryl-coenzyme A reductase

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
3-hydroxy-3-methylglutaryl-coenzyme A reductase P04035 Details

References:

  1. Abe Y, Suzuki T, Ono C, Iwamoto K, Hosobuchi M, Yoshikawa H: Molecular cloning and characterization of an ML-236B (compactin) biosynthetic gene cluster in Penicillium citrinum. Mol Genet Genomics. 2002 Jul;267(5):636-46. Epub 2002 Jun 28. Pubmed
  2. Miyazaki A, Koieyama T, Shimada Y, Kikuchi T, Nezu H, Ito K, Kasanuki N, Koga T: Effects of pravastatin sodium on mevalonate metabolism in common marmosets. J Biochem (Tokyo). 2002 Sep;132(3):395-400. Pubmed
  3. Buxbaum JD, Geoghagen NS, Friedhoff LT: Cholesterol depletion with physiological concentrations of a statin decreases the formation of the Alzheimer amyloid Abeta peptide. J Alzheimers Dis. 2001 Apr;3(2):221-229. Pubmed
  4. Baranova NA, Kreier VG, Egorov NS: [Concentration on Diapak C 16 capsules of lovastatin, mevinolinic acid and other inhibitors of biosynthesis of sterins produced by Penicillium citrinum 89] Antibiot Khimioter. 2002;47(4):3-6. Pubmed
  5. Farina HG, Bublik DR, Alonso DF, Gomez DE: Lovastatin alters cytoskeleton organization and inhibits experimental metastasis of mammary carcinoma cells. Clin Exp Metastasis. 2002;19(6):551-9. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Podar K, Tai YT, Hideshima T, Vallet S, Richardson PG, Anderson KC: Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. Pubmed
  8. Dimitroulakos J, Marhin WH, Tokunaga J, Irish J, Gullane P, Penn LZ, Kamel-Reid S: Microarray and biochemical analysis of lovastatin-induced apoptosis of squamous cell carcinomas. Neoplasia. 2002 Jul-Aug;4(4):337-46. Pubmed

2. Integrin alpha-L

Kind: protein

Organism: Human

Pharmacological action: no

Actions: other/unknown

Components

Name UniProt ID Details
Integrin alpha-L P20701 Details

References:

  1. Kallen J, Welzenbach K, Ramage P, Geyl D, Kriwacki R, Legge G, Cottens S, Weitz-Schmidt G, Hommel U: Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain. J Mol Biol. 1999 Sep 10;292(1):1-9. Pubmed

3. Histone deacetylase 2

Kind: protein

Organism: Human

Pharmacological action: no

Actions: other

Components

Name UniProt ID Details
Histone deacetylase 2 Q92769 Details

References:

  1. Lin YC, Lin JH, Chou CW, Chang YF, Yeh SH, Chen CC: Statins increase p21 through inhibition of histone deacetylase activity and release of promoter-associated HDAC1/2. Cancer Res. 2008 Apr 1;68(7):2375-83. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Neuvonen PJ, Niemi M, Backman JT: Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81. Pubmed
  2. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. Pubmed
  3. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  4. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  6. Lexicomp

2. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

3. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

4. Serum paraoxonase/lactonase 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Serum paraoxonase/lactonase 3 Q15166 Details

References:

  1. Draganov DI, Stetson PL, Watson CE, Billecke SS, La Du BN: Rabbit serum paraoxonase 3 (PON3) is a high density lipoprotein-associated lactonase and protects low density lipoprotein against oxidation. J Biol Chem. 2000 Oct 27;275(43):33435-42. Pubmed

5. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Tornio A, Pasanen MK, Laitila J, Neuvonen PJ, Backman JT: Comparison of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) as inhibitors of cytochrome P450 2C8. Basic Clin Pharmacol Toxicol. 2005 Aug;97(2):104-8. Pubmed
  2. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. Pubmed
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

6. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor inducer

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. Pubmed
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  4. Lexicomp

7. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. Pubmed

8. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

9. UDP-glucuronosyltransferase 1-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-1 P22309 Details

References:

  1. http://www.pharmacologyweekly.com/content/pages/ugt-enzymes-medications-herbs-substrate-inhibitor-inducer

10. UDP-glucuronosyltransferase 1-3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-3 P35503 Details

References:

  1. http://www.pharmacologyweekly.com/content/pages/ugt-enzymes-medications-herbs-substrate-inhibitor-inducer

11. UDP-glucuronosyltransferase 2B7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 2B7 P16662 Details

References:

  1. Prueksaritanont T, Subramanian R, Fang X, Ma B, Qiu Y, Lin JH, Pearson PG, Baillie TA: Glucuronidation of statins in animals and humans: a novel mechanism of statin lactonization. Drug Metab Dispos. 2002 May;30(5):505-12. Pubmed

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Wang E, Casciano CN, Clement RP, Johnson WW: HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein. Pharm Res. 2001 Jun;18(6):800-6. Pubmed
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. Pubmed
  3. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. Pubmed

2. Solute carrier organic anion transporter family member 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1A2 P46721 Details

References:

  1. Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, Kim RB: OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos. 1999 Aug;27(8):866-71. Pubmed
  2. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. Pubmed

3. Solute carrier organic anion transporter family member 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B1 Q9Y6L6 Details

References:

  1. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. Pubmed
  2. Sandhu P, Lee W, Xu X, Leake BF, Yamazaki M, Stone JA, Lin JH, Pearson PG, Kim RB: Hepatic uptake of the novel antifungal agent caspofungin. Drug Metab Dispos. 2005 May;33(5):676-82. Epub 2005 Feb 16. Pubmed

4. Canalicular multispecific organic anion transporter 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Canalicular multispecific organic anion transporter 1 Q92887 Details

References:

  1. Ellis LC, Hawksworth GM, Weaver RJ: ATP-dependent transport of statins by human and rat MRP2/Mrp2. Toxicol Appl Pharmacol. 2013 Jun 1;269(2):187-94. doi: 10.1016/j.taap.2013.03.019. Epub 2013 Apr 2. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:08