High Cholesterol

Also known as: High Blood Cholesterol Level / Hypercholesterolemia / Hypercholesteremia / Hypercholesterolaemia / Congenital xanthoma / Hypercholesteraemia / Elevated cholesterol

DrugDrug NameDrug Description
DB01076AtorvastatinAtorvastatin (Lipitor) is a member of the drug class known as statins. It is used for lowering cholesterol. Atorvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate. Atorvastatin acts primarily in the liver. Decreased hepatic cholesterol levels increases hepatic uptake of cholesterol and reduces plasma cholesterol levels.
DB00227LovastatinLovastatin 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.
DB00641SimvastatinSimvastatin is a lipid-lowering agent that is derived synthetically from the fermentation of Aspergillus terreus. It is a potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (hydroxymethylglutaryl COA reductases), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL receptors, it increases breakdown of LDL cholesterol.
DrugDrug NameTargetType
DB01076Atorvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB01076AtorvastatinCytochrome P450 3A4enzyme
DB01076AtorvastatinDipeptidyl peptidase 4target
DB01076AtorvastatinCytochrome P450 2D6enzyme
DB01076AtorvastatinCytochrome P450 2C9enzyme
DB01076AtorvastatinCytochrome P450 2C19enzyme
DB01076AtorvastatinCytochrome P450 3A5enzyme
DB01076AtorvastatinCytochrome P450 3A7enzyme
DB01076AtorvastatinMultidrug resistance protein 1transporter
DB01076AtorvastatinSolute carrier organic anion transporter family member 1A2transporter
DB01076AtorvastatinSolute carrier organic anion transporter family member 1B1transporter
DB01076AtorvastatinMultidrug resistance-associated protein 4transporter
DB01076AtorvastatinMultidrug resistance-associated protein 5transporter
DB01076AtorvastatinMultidrug resistance-associated protein 1transporter
DB01076AtorvastatinCytochrome P450 2B6enzyme
DB01076AtorvastatinCytochrome P450 2C8enzyme
DB01076AtorvastatinAryl hydrocarbon receptortarget
DB01076AtorvastatinSolute carrier organic anion transporter family member 2B1transporter
DB01076AtorvastatinSolute carrier organic anion transporter family member 1B3transporter
DB01076AtorvastatinUDP-glucuronosyltransferase 1-1enzyme
DB01076AtorvastatinUDP-glucuronosyltransferase 1-3enzyme
DB01076AtorvastatinUDP-glucuronosyltransferase 2B7enzyme
DB01076AtorvastatinCanalicular multispecific organic anion transporter 1transporter
DB01076AtorvastatinBile salt export pumptransporter
DB00227Lovastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB00227LovastatinCytochrome P450 3A4enzyme
DB00227LovastatinCytochrome P450 2C8enzyme
DB00227LovastatinIntegrin alpha-Ltarget
DB00227LovastatinHistone deacetylase 2target
DB00227LovastatinSerum paraoxonase/lactonase 3enzyme
DB00227LovastatinCytochrome P450 2C9enzyme
DB00227LovastatinCytochrome P450 3A5enzyme
DB00227LovastatinCytochrome P450 3A7enzyme
DB00227LovastatinMultidrug resistance protein 1transporter
DB00227LovastatinSolute carrier organic anion transporter family member 1A2transporter
DB00227LovastatinSolute carrier organic anion transporter family member 1B1transporter
DB00227LovastatinCytochrome P450 2D6enzyme
DB00227LovastatinUDP-glucuronosyltransferase 1-1enzyme
DB00227LovastatinUDP-glucuronosyltransferase 1-3enzyme
DB00227LovastatinUDP-glucuronosyltransferase 2B7enzyme
DB00227LovastatinCanalicular multispecific organic anion transporter 1transporter
DB00227LovastatinBile salt export pumptransporter
DB00641Simvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB00641SimvastatinIntegrin beta-2target
DB00641SimvastatinCytochrome P450 3A4enzyme
DB00641SimvastatinCytochrome P450 2C8enzyme
DB00641SimvastatinCytochrome P450 2C9enzyme
DB00641SimvastatinCytochrome P450 2C19enzyme
DB00641SimvastatinCytochrome P450 3A5enzyme
DB00641SimvastatinCytochrome P450 3A7enzyme
DB00641SimvastatinMultidrug resistance protein 1transporter
DB00641SimvastatinSolute carrier organic anion transporter family member 1A2transporter
DB00641SimvastatinSolute carrier organic anion transporter family member 1B1transporter
DB00641SimvastatinCytochrome P450 2B6enzyme
DB00641SimvastatinCytochrome P450 2D6enzyme
DB00641SimvastatinUDP-glucuronosyltransferase 1-1enzyme
DB00641SimvastatinUDP-glucuronosyltransferase 1-3enzyme
DB00641SimvastatinUDP-glucuronosyltransferase 2B7enzyme
DB00641SimvastatinCanalicular multispecific organic anion transporter 1transporter
DB00641SimvastatinIntegrin alpha-Ltarget
DB00641SimvastatinBile salt export pumptransporter
DrugDrug NamePhaseStatusCount
DB00973Ezetimibe0Completed1
DB09302Alirocumab1Completed10
DB06630Anacetrapib1Completed1
DB01076Atorvastatin1Completed6
DB12456Bococizumab1Completed5
DB00973Ezetimibe1Completed7
DB01039Fenofibrate1Completed1
DB05123Gemcabene1Completed3
DB11789Hyodeoxycholic Acid1Unknown Status1
DB11629Laropiprant1Completed1
DB00350Minoxidil1Completed1
DB00627Niacin1Completed2
DB08860Pitavastatin1Completed1
DB06817Raltegravir1Completed1
DB01098Rosuvastatin1Completed2
DB00641Simvastatin1Completed3
DB00877Sirolimus1Completed1
DB09153Sodium Chloride1Completed1
DB09153Sodium Chloride1Terminated2
DB00864Tacrolimus1Completed1
DB126293,5-diiodothyropropionic acid1 / 2Terminated1
DB09302Alirocumab2Active Not Recruiting1
DB09302Alirocumab2Completed5
DB09302Alirocumab2Not Yet Recruiting1
DB09302Alirocumab2Unknown Status1
DB06630Anacetrapib2Terminated1
DB01076Atorvastatin2Completed14
DB01076Atorvastatin2Not Yet Recruiting1
DB01076Atorvastatin2Recruiting2
DB01076Atorvastatin2Terminated1
DB11936Bempedoic acid2Completed7
DB06698Betahistine2Terminated1
DB12456Bococizumab2Completed4
DB01432Cholestyramine2Active Not Recruiting1
DB05035Eprotirome2Completed1
DB00783Estradiol2Completed1
DB09303Evolocumab2Completed2
DB00973Ezetimibe2Active Not Recruiting1
DB00973Ezetimibe2Completed6
DB05449FM-VP42Completed1
DB12469Fasudil2Completed1
DB01039Fenofibrate2Active Not Recruiting1
DB05123Gemcabene2Completed5
DB00125L-Arginine2Completed1
DB00166Lipoic Acid2Completed1
DB08827Lomitapide2Completed3
DB00227Lovastatin2Completed1
DB05192MB078112Withdrawn1
DB00331Metformin2Completed2
DB00959Methylprednisolone2Not Yet Recruiting1
DB05528Mipomersen2Completed5
DB00627Niacin2Active Not Recruiting1
DB11133Omega-3 fatty acids2Active Not Recruiting1
DB00175Pravastatin2Completed3
DB01098Rosuvastatin2Completed1
DB05317TAK-4752Completed1
DB05317TAK-4752Terminated1
DB12435Tipelukast2Active Not Recruiting1
DB00284Acarbose3Completed1
DB09302Alirocumab3Active Not Recruiting2
DB09302Alirocumab3Completed16
DB09302Alirocumab3Recruiting3
DB00381Amlodipine3Completed2
DB06630Anacetrapib3Completed2
DB01076Atorvastatin3Active Not Recruiting1
DB01076Atorvastatin3Completed39
DB01076Atorvastatin3Not Yet Recruiting1
DB01076Atorvastatin3Recruiting2
DB01076Atorvastatin3Terminated7
DB11936Bempedoic acid3Active Not Recruiting1
DB11936Bempedoic acid3Completed4
DB00542Benazepril3Completed1
DB00796Candesartan cilexetil3Completed1
DB01136Carvedilol3Completed1
DB00310Chlorthalidone3Completed2
DB01432Cholestyramine3Recruiting2
DB00930Colesevelam3Completed1
DB00286Conjugated estrogens3Completed1
DB00343Diltiazem3Completed1
DB00590Doxazosin3Completed1
DB11655Evacetrapib3Terminated2
DB09303Evolocumab3Completed7
DB00973Ezetimibe3Active Not Recruiting1
DB00973Ezetimibe3Completed47
DB00973Ezetimibe3Recruiting2
DB00973Ezetimibe3Terminated4
DB00973Ezetimibe3Unknown Status1
DB01023Felodipine3Completed1
DB01039Fenofibrate3Completed2
DB01039Fenofibrate3Recruiting2
DB01095Fluvastatin3Completed2
DB01095Fluvastatin3Recruiting2
DB01095Fluvastatin3Terminated1
DB00695Furosemide3Completed1
DB00222Glimepiride3Completed1
DB01275Hydralazine3Completed1
DB00999Hydrochlorothiazide3Completed1
DB01306Insulin Aspart3Completed1
DB01307Insulin Detemir3Completed1
DB00030Insulin Human3Completed1
DB00047Insulin glargine3Completed1
DB01029Irbesartan3Completed1
DB11629Laropiprant3Completed1
DB12448Lifibrol3Completed1
DB00722Lisinopril3Completed2
DB00227Lovastatin3Completed2
DB00227Lovastatin3Recruiting2
DB00227Lovastatin3Terminated1
DB00603Medroxyprogesterone acetate3Completed1
DB00331Metformin3Completed2
DB00264Metoprolol3Completed1
DB05528Mipomersen3Completed5
DB00627Niacin3Completed3
DB00627Niacin3Recruiting2
DB11133Omega-3 fatty acids3Recruiting2
DB01132Pioglitazone3Completed1
DB08860Pitavastatin3Completed6
DB00175Pravastatin3Completed4
DB00175Pravastatin3Recruiting2
DB00175Pravastatin3Terminated1
DB00396Progesterone3Completed1
DB00178Ramipril3Completed1
DB00912Repaglinide3Completed1
DB00206Reserpine3Completed1
DB00412Rosiglitazone3Completed1
DB01098Rosuvastatin3Completed33
DB01098Rosuvastatin3Recruiting2
DB01098Rosuvastatin3Terminated3
DB01098Rosuvastatin3Unknown Status1
DB00641Simvastatin3Completed30
DB00641Simvastatin3Recruiting2
DB00641Simvastatin3Terminated4
DB05317TAK-4753Completed6
DB05317TAK-4753Terminated4
DB01162Terazosin3Completed1
DB06281Torcetrapib3Completed1
DB06281Torcetrapib3Terminated1
DB00384Triamterene3Completed1
DB00177Valsartan3Completed4
DB09302Alirocumab4Active Not Recruiting2
DB09302Alirocumab4Completed1
DB00381Amlodipine4Completed2
DB01076Atorvastatin4Active Not Recruiting1
DB01076Atorvastatin4Completed28
DB01076Atorvastatin4Recruiting1
DB01076Atorvastatin4Terminated3
DB01076Atorvastatin4Unknown Status1
DB01393Bezafibrate4Completed1
DB00930Colesevelam4Completed4
DB00375Colestipol4Completed1
DB11874Crocin4Completed1
DB06292Dapagliflozin4Completed1
DB00973Ezetimibe4Completed28
DB00973Ezetimibe4Recruiting2
DB00973Ezetimibe4Terminated2
DB00973Ezetimibe4Unknown Status2
DB01039Fenofibrate4Completed2
DB01095Fluvastatin4Completed2
DB01095Fluvastatin4Unknown Status1
DB11629Laropiprant4Completed1
DB00238Nevirapine4Completed1
DB00627Niacin4Completed2
DB11133Omega-3 fatty acids4Completed1
DB09539Omega-3-acid ethyl esters4Completed1
DB09539Omega-3-acid ethyl esters4Unknown Status1
DB08860Pitavastatin4Completed6
DB00175Pravastatin4Completed3
DB00175Pravastatin4Unknown Status1
DB01098Rosuvastatin4Completed9
DB01098Rosuvastatin4Recruiting1
DB01098Rosuvastatin4Terminated2
DB01098Rosuvastatin4Unknown Status2
DB00641Simvastatin4Completed20
DB00641Simvastatin4Recruiting1
DB00641Simvastatin4Unknown Status1
DB00945Acetylsalicylic acidNot AvailableCompleted2
DB00802AlfentanilNot AvailableRecruiting1
DB09302AlirocumabNot AvailableRecruiting1
DB00381AmlodipineNot AvailableCompleted1
DB01060AmoxicillinNot AvailableCompleted1
DB01238AripiprazoleNot AvailableRecruiting1
DB01076AtorvastatinNot AvailableCompleted6
DB01076AtorvastatinNot AvailableUnknown Status1
DB13015CardarineNot AvailableCompleted1
DB00438CeftazidimeNot AvailableRecruiting1
DB00369CidofovirNot AvailableRecruiting1
DB00537CiprofloxacinNot AvailableRecruiting1
DB00758ClopidogrelNot AvailableUnknown Status1
DB00363ClozapineNot AvailableRecruiting1
DB01234DexamethasoneNot AvailableRecruiting1
DB00829DiazepamNot AvailableRecruiting1
DB00973EzetimibeNot AvailableCompleted9
DB01095FluvastatinNot AvailableCompleted1
DB01320FosphenytoinNot AvailableRecruiting1
DB00502HaloperidolNot AvailableRecruiting1
DB01109HeparinNot AvailableRecruiting1
DB00327HydromorphoneNot AvailableRecruiting1
DB01202LevetiracetamNot AvailableRecruiting1
DB00227LovastatinNot AvailableCompleted1
DB08815LurasidoneNot AvailableRecruiting1
DB00760MeropenemNot AvailableRecruiting1
DB00331MetforminNot AvailableWithdrawn1
DB00959MethylprednisoloneNot AvailableRecruiting1
DB00683MidazolamNot AvailableRecruiting1
DB01618MolindoneNot AvailableRecruiting1
DB00295MorphineNot AvailableRecruiting1
DB00627NiacinNot AvailableCompleted1
DB00622NicardipineNot AvailableRecruiting1
DB00334OlanzapineNot AvailableRecruiting1
DB00198OseltamivirNot AvailableRecruiting1
DB00312PentobarbitalNot AvailableRecruiting1
DB08860PitavastatinNot AvailableTerminated1
DB00175PravastatinNot AvailableCompleted3
DB00175PravastatinNot AvailableTerminated1
DB00818PropofolNot AvailableRecruiting1
DB01224QuetiapineNot AvailableRecruiting1
DB00734RisperidoneNot AvailableRecruiting1
DB01098RosuvastatinNot AvailableCompleted4
DB01098RosuvastatinNot AvailableTerminated1
DB01098RosuvastatinNot AvailableUnknown Status1
DB00133SerineNot AvailableCompleted2
DB00641SimvastatinNot AvailableCompleted5
DB00641SimvastatinNot AvailableUnknown Status1
DB00300Tenofovir disoproxilNot AvailableCompleted1
DB00373TimololNot AvailableRecruiting1
DB00684TobramycinNot AvailableRecruiting1
DB00273TopiramateNot AvailableRecruiting1
DB00313Valproic AcidNot AvailableRecruiting1
DB00682WarfarinNot AvailableRecruiting1
DB00246ZiprasidoneNot AvailableRecruiting1