Mixed hypercholesterolemia

Also known as: Mixed Hyperlipidemia / Mixed Dyslipidemia / Mixed dyslipidemias / Mixed Hyperlipidaemia / Broad- or floating-betalipoproteinemia / Type V hyperlipidaemia / Type V hyperlipidemia / Type V lipidaemia / Type V lipidemia / Hyperlipoproteinemia Type V / Type V hyperlipoproteinemia / Fredrickson Type V lipidemia / Fredrickson Type V lipidaemia / Type V hyperlipoproteinaemia

DrugDrug NameDrug Description
DB01076AtorvastatinAtorvastatin is a member of the statins firstly synthesized in 1985 by Dr. Bruce Roth and FDA approved in 1996.[T568] It is a pentasubstituted pyrrole[A177415] formed by two contrasting moieties with an achiral heterocyclic core unit and a 3,5-dihydroxypentanoyl side chain identical to its parent compound.[T571] Unlike other members of the statin group, atorvastatin is an active compound and hence, it does not require activation.[A177436] It is the most widely used and potent member of the statin group.[T568]
DB00973EzetimibeEzetimibe is a lipid-lowering compound that inhibits intestinal cholesterol and related phytosterol absorption. The discovery and research of this drug began in the early 1990's, where intravenous administration of radio-labelled compound in rats resulting in subsequent localization of the drug within enterocytes at the intestinal villus, leading to studies of investigating the effect of ezetimibe on intestinal cholesterol absorption [A15202]. Ezetimibe is used as an adjunctive therapy to diet to lower cholesterol levels in primary hyperlipidemia, mixed hyperlipidemia, homozygous familial hypercholesterolemia (HoFH), and homozygous sitosterolemia (phytosterolemia) [FDA Label]. Unlike other classes of cholesterol-reducing compounds including statins and bile acid sequestrants, ezetimibe has a distinct mechanism of action involving the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), and is the first drug that does not affect absorption of fat-soluble nutrients such as fat-soluble vitamins, triglycerides, or bile acids [A33313]. In genetically NPC1L1-deficient mice, a 70% reduction in intestinal cholesterol absorption was seen and the mice were insensitive to ezetimibe treatment [A15202]. Based on these findings, it is indicated that NPC1L1 plays an essential role in promoting intestinal cholesterol uptake via an ezetimibe-sensitive pathway [A15202]. By interfering with the intestinal uptake of cholesterol and phytosterols, ezetimibe reduces the delivery of intestinal cholesterol to the liver [FDA Label].
DB01039FenofibrateFenofibrate is a prodrug of fenofibric acid, an antilipemic agent which reduces both cholesterol and triglycerides in the blood.
DB01095FluvastatinFluvastatin is an antilipemic agent that competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Fluvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. It is also the first entirely synthetic HMG-CoA reductase inhibitor and is structurally distinct from the fungal derivatives of this therapeutic class. Fluvastatin is a racemate comprising equimolar amounts of (3R,5S)- and (3S,5R)-fluvastatin.
DB00627NiacinA water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has pellagra-curative, vasodilating, and antilipemic properties.
DB08860PitavastatinPitavastatin a lipid-lowering agent that belongs to the statin class of medications for treatment of dyslipidemia. It is also used for primary and secondary prevention of cardiovascular disease. FDA approved in Aug 3, 2009.
DB00175PravastatinPravastatin is the 6-alpha-hydroxy acid form of [mevastatin].[T303] Pravastatin was firstly approved in 1991 becoming the second available statin in the United States. It was the first statin administered as the active form and not as a prodrug.[T274] This drug was developed by Sankyo Co. Ltd.; however, the first approved pravastatin product was developed by Bristol Myers Squibb and FDA approved in 1991.[L6142] Pravastatin is made through a fermentation process in which [mevastatin] is first obtained. The manufacturing process is followed by the hydrolysis of the lactone group and the biological hydroxylation with _Streptomyces carbophilus_ to introduce the allylic 6-alcohol group.[T239]
DB01098RosuvastatinRosuvastatin is an antilipemic agent that competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reducuase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
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
DB01076AtorvastatinCanalicular multispecific organic anion transporter 1transporter
DB01076AtorvastatinBile salt export pumptransporter
DB01076AtorvastatinSerum albumincarrier
DB00973EzetimibeNiemann-Pick C1-like protein 1target
DB00973EzetimibeAminopeptidase Ntarget
DB00973EzetimibeSterol O-acyltransferase 1target
DB00973EzetimibeUDP-glucuronosyltransferase 1-1enzyme
DB00973EzetimibeUDP-glucuronosyltransferase 1-3enzyme
DB00973EzetimibeMultidrug resistance protein 1transporter
DB00973EzetimibeCanalicular multispecific organic anion transporter 1transporter
DB00973EzetimibeSolute carrier organic anion transporter family member 1B1transporter
DB00973EzetimibeUDP-glucuronosyltransferase 2B15enzyme
DB00973EzetimibeUDP-glucuronosyltransferase 2B7enzyme
DB00973EzetimibeCytochrome P450 3A4enzyme
DB00973EzetimibeATP-binding cassette sub-family G member 5transporter
DB00973EzetimibeCanalicular multispecific organic anion transporter 2transporter
DB00973EzetimibeATP-binding cassette sub-family G member 2transporter
DB00973EzetimibeATP-binding cassette sub-family G member 8transporter
DB00973EzetimibeCytochrome P450 2C8enzyme
DB00973EzetimibeBile salt export pumptransporter
DB01039FenofibratePeroxisome proliferator-activated receptor alphatarget
DB01039FenofibrateMetalloproteinasetarget
DB01039FenofibrateCytochrome P450 2C8enzyme
DB01039FenofibrateCytochrome P450 2C9enzyme
DB01039FenofibrateCytochrome P450 3A4enzyme
DB01039FenofibratePeroxisome proliferator-activated receptor gammatarget
DB01039FenofibratePeroxisome proliferator-activated receptor deltatarget
DB01039FenofibrateNuclear receptor subfamily 1 group I member 2target
DB01039FenofibrateUDP-glucuronosyltransferase 1-1enzyme
DB01039FenofibrateBile salt export pumptransporter
DB01095Fluvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB01095FluvastatinCytochrome P450 2C9enzyme
DB01095FluvastatinCytochrome P450 3A4enzyme
DB01095FluvastatinCytochrome P450 2C8enzyme
DB01095FluvastatinCytochrome P450 2D6enzyme
DB01095FluvastatinCytochrome P450 2C19enzyme
DB01095FluvastatinCytochrome P450 1A1enzyme
DB01095FluvastatinSolute carrier organic anion transporter family member 1B1transporter
DB01095FluvastatinSolute carrier organic anion transporter family member 1B3transporter
DB01095FluvastatinSolute carrier organic anion transporter family member 2B1transporter
DB01095FluvastatinSolute carrier family 15 member 1transporter
DB01095FluvastatinCytochrome P450 3A5enzyme
DB01095FluvastatinUDP-glucuronosyltransferase 1-1enzyme
DB01095FluvastatinUDP-glucuronosyltransferase 1-3enzyme
DB01095FluvastatinUDP-glucuronosyltransferase 2B7enzyme
DB01095FluvastatinCanalicular multispecific organic anion transporter 1transporter
DB01095FluvastatinCytochrome P450 2B6enzyme
DB00627NiacinHydroxycarboxylic acid receptor 2target
DB00627NiacinNicotinamide N-methyltransferasetarget
DB00627NiacinNicotinate-nucleotide pyrophosphorylase [carboxylating]target
DB00627NiacinHydroxycarboxylic acid receptor 3target
DB00627NiacinSolute carrier family 22 member 5transporter
DB00627NiacinSolute carrier organic anion transporter family member 2B1transporter
DB00627NiacinMonocarboxylate transporter 1transporter
DB00627NiacinCytochrome P450 2D6enzyme
DB00627NiacinSodium-coupled monocarboxylate transporter 1transporter
DB00627NiacinMonocarboxylate transporter 4transporter
DB00627NiacinThyroxine-binding globulincarrier
DB08860PitavastatinSolute carrier organic anion transporter family member 1B1transporter
DB08860PitavastatinSolute carrier organic anion transporter family member 1B3transporter
DB08860PitavastatinUDP-glucuronosyltransferase 2B7enzyme
DB08860PitavastatinUDP-glucuronosyltransferase 1-3enzyme
DB08860PitavastatinCytochrome P450 2C9enzyme
DB08860PitavastatinCytochrome P450 2C8enzyme
DB08860Pitavastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB08860PitavastatinSolute carrier organic anion transporter family member 2B1transporter
DB08860PitavastatinSodium/bile acid cotransportertransporter
DB08860PitavastatinATP-binding cassette sub-family G member 2transporter
DB08860PitavastatinMultidrug resistance protein 1transporter
DB08860PitavastatinCanalicular multispecific organic anion transporter 1transporter
DB08860PitavastatinSerum albumincarrier
DB08860PitavastatinAlpha-1-acid glycoprotein 1carrier
DB08860PitavastatinBile salt export pumptransporter
DB00175Pravastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB00175PravastatinSolute carrier organic anion transporter family member 2B1transporter
DB00175PravastatinMultidrug resistance protein 1transporter
DB00175PravastatinSolute carrier organic anion transporter family member 1A2transporter
DB00175PravastatinSolute carrier family 22 member 6transporter
DB00175PravastatinSolute carrier family 22 member 8transporter
DB00175PravastatinCanalicular multispecific organic anion transporter 1transporter
DB00175PravastatinSolute carrier family 22 member 11transporter
DB00175PravastatinATP-binding cassette sub-family G member 2transporter
DB00175PravastatinSolute carrier family 22 member 7transporter
DB00175PravastatinSolute carrier organic anion transporter family member 1B1transporter
DB00175PravastatinMonocarboxylate transporter 1transporter
DB00175PravastatinBile salt export pumptransporter
DB00175PravastatinSolute carrier organic anion transporter family member 1B3transporter
DB01098Rosuvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB01098RosuvastatinCytochrome P450 2C9enzyme
DB01098RosuvastatinMultidrug resistance-associated protein 4transporter
DB01098RosuvastatinMultidrug resistance-associated protein 1transporter
DB01098RosuvastatinCytochrome P450 2C19enzyme
DB01098RosuvastatinCytochrome P450 3A4enzyme
DB01098RosuvastatinCytochrome P450 3A5enzyme
DB01098RosuvastatinSolute carrier organic anion transporter family member 1A2transporter
DB01098RosuvastatinSolute carrier organic anion transporter family member 1B3transporter
DB01098RosuvastatinSolute carrier organic anion transporter family member 2B1transporter
DB01098RosuvastatinCystine/glutamate transportertransporter
DB01098RosuvastatinSolute carrier organic anion transporter family member 1B1transporter
DB01098RosuvastatinBile salt export pumptransporter
DB01098RosuvastatinATP-binding cassette sub-family G member 2transporter
DB01098RosuvastatinSerum albumincarrier
DB01098RosuvastatinCanalicular multispecific organic anion transporter 1transporter
DB01098RosuvastatinSolute carrier family 22 member 8transporter
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
DB00945Acetylsalicylic acid1Completed1
DB00758Clopidogrel1Completed1
DB09303Evolocumab1Completed1
DB11629Laropiprant1Completed1
DB04115Berberine2Recruiting1
DB01393Bezafibrate2Recruiting1
DB05123Gemcabene2Active Not Recruiting1
DB01377Magnesium oxide2Recruiting1
DB12433SCH-9002712Completed1
DB01076Atorvastatin3Completed7
DB01076Atorvastatin3Terminated1
DB01076Atorvastatin3Unknown Status1
DB09303Evolocumab3Completed3
DB00973Ezetimibe3Completed1
DB01039Fenofibrate3Completed7
DB01039Fenofibrate3Unknown Status1
DB01095Fluvastatin3Completed2
DB00627Niacin3Completed1
DB01098Rosuvastatin3Completed4
DB00641Simvastatin3Completed8
DB00641Simvastatin3Terminated1
DB06281Torcetrapib3Terminated1
DB00227Lovastatin4Completed1
DB00627Niacin4Completed1
DB09539Omega-3-acid ethyl esters4Completed1
DB09539Omega-3-acid ethyl esters4Unknown Status1
DB08860Pitavastatin4Completed1
DB00175Pravastatin4Completed1
DB00641Simvastatin4Unknown Status1
DB01076AtorvastatinNot AvailableUnknown Status1
DB01039FenofibrateNot AvailableCompleted1
DB00641SimvastatinNot AvailableCompleted1