Hydroxymethylglutaryl-CoA Reductase Inhibitors

Compounds that inhibit HMG-CoA reductases. They have been shown to directly lower cholesterol synthesis.
DrugDrug NameDrug Indication
DB00175PravastatinPravastatin is indicated for primary prevention of coronary events hypercholesterolemic patients without clinical evidence of coronary heart disease. Its use includes the reduction of risk on myocardial infarction, undergoing myocardial revascularization procedures and cardiovascular mortality.[T274] As well, pravastatin can be used as a secondary prevention agent for cardiovascular events in patients with clinically evident coronary heart disease. This indication includes the reduction of risk of total mortality by reducing coronary death, myocardial infarction, undergoing myocardial revascularization procedures, stroke, and stroke/transient ischemic attack as well as to slow the progression of coronary atherosclerosis.[T274] The term cardiovascular events correspond to all the incidents that can produce damage to the heart muscle including the interruption of blood flow.[L6028] As adjunctive therapy to diet, pravastatin is used in: - Patients with primary hypercholesterolemia and mixed dyslipidemias including hyperlipidemia type IIa and IIb. - Patients with elevated serum triglycerides including type IV hyperlipidemia. - Patients with heterozygous familial hypercholesterolemia in patients over 8 years of age with low-density lipoprotein (LDL) cholesterol higher than 190 mg/dl after diet modifications or LDL levels higher than 160 mg/dl and familial history of premature cardiovascular diseases or at least two cardiovascular risk factors.[T274] In patients that do not respond adequately to diet, pravastatin is used to treat patients with primary dysbetalipoproteinemia (type III hyperlipidemia).[T274] Dyslipidemia is defined as an elevation of plasma cholesterol, triglycerides or both as well as to the presence of low levels of high-density lipoprotein. This condition represents an increased risk for the development of atherosclerosis.[L6025]
DB00227LovastatinLovastatin is indicated to reduce the risk of myocardial infarction, unstable angina, and the need for coronary revascularization procedures in individuals without symptomatic cardiovascular disease, average to moderately elevated total-C and LDL-C, and below average HDL-C. It is indicated as an intervention alternative in individuals presenting dyslipidemia at risk of developing atherosclerotic vascular disease. The administration of this agent should be accompanied by the implementation of a fat and cholesterol-restricted diet.[F4661] Therapy 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. Lovastatin 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 IIb2), when the response to diet restricted in saturated fat and cholesterol and to other nonpharmacological measures alone has been inadequate.[F4661,F4664] Lovastatin is also 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.[F4661] Lovastatin is indicated as an adjunct to diet to reduce total-C, LDL-C and apolipoprotein B levels in adolescent boys and girls with Heterozygous Familial Hypercholesterolemia (HeFH) who are at least one year post-menarche, 10 to 17 years of age, with HeFH if after an adequate trial of diet therapy the following findings are present: LDL-C remains greater than 189 mg/dL or LDL-C remains greater than 160 mg/dL and there is a positive family history of premature cardiovascular disease or two or more other CVD risk factors are present in the adolescent patient. Before administering lovastatin, it is important to rule out the presence of secondary causes of hypercholesterolemia and a lipid profile should be performed. Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.[A181087, A181406]
DB00439CerivastatinUsed as an adjunct to diet for the reduction of elevated total and LDL cholesterol levels in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Types IIa and IIb) when the response to dietary restriction of saturated fat and cholesterol and other non-pharmacological measures alone has been inadequate.
DB00641SimvastatinSimvastatin is indicated for the treatment of hyperlipidemia to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL‑C), apolipoprotein B (Apo B), and triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C).[F4655, F4658] This includes the treatment of primary hyperlipidemia (Fredrickson type IIa, heterozygous familial and nonfamilial), mixed dyslipidemia (Fredrickson type IIb), hypertriglyceridemia (Fredrickson type IV hyperlipidemia), primary dysbetalipoproteinemia (Fredrickson type III hyperlipidemia), homozygous familial hypercholesterolemia (HoFH) as an adjunct to other lipid-lowering treatments, as well as adolescent patients with Heterozygous Familial Hypercholesterolemia (HeFH).[F4655, F4658] Simvastatin is also indicated to reduce the risk of cardiovascular morbidity and mortality including myocardial infarction, stroke, and the need for revascularization procedures. It is primarily used in patients at high risk of coronary events because of existing coronary heart disease, diabetes, peripheral vessel disease, history of stroke or other cerebrovascular disease.[F4655, F4658] Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.[A181087, A181406]
DB01076AtorvastatinAtorvastatin is approved for the treatment of several types of dyslipidemias including: - Primary hyperlipidemia and mixed dyslipidemia in adults. - Hypertriglyceridemia. - Primary dysbetalipoproteinemia. - Homozygous familial hypercholesterolemia. - Heterozygous familial hypercholesterolemia in adolescent patients with failed dietary modifications.[A177397] Dyslipidemia is defined as an elevation of plasma cholesterol, triglycerides or both as well as to the presence of low levels of high-density lipoprotein. This condition represents an increased risk for the development of atherosclerosis.[L6025] Atorvastatin is indicated, in combination with dietary modifications, to prevent cardiovascular events in patients with cardiac risk factors and/or abnormal lipid profiles.[A177397] Atorvastatin can be used as a preventive agent for myocardial infarction, stroke, revascularization, and angina, in patients without coronary heart disease but with multiple risk factors, and in patients with type 2 diabetes without coronary heart disease but multiple risk factors.[A177397] Atorvastatin can also be used as a preventive agent for non-fatal myocardial infarction, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure and angina in patients with coronary heart disease.[A177397] Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.[A181087, A181406]
DB01095FluvastatinTo be used as an adjunct to dietary therapy to prevent cardiovascular events. May be used as secondary prevention in patients with coronary heart disease (CHD) to reduce the risk of requiring coronary revascularization procedures, for reducing progression of coronary atherosclerosis in hypercholesterolemic patients with CHD, and for the treatment of primary hypercholesterolemia and mixed dyslidipidemia.
DB01098RosuvastatinThe FDA monograph states that rosuvastatin is indicated as an adjunct to diet in the treatment of triglyceridemia, Primary Dysbetalipoproteinemia (Type III Hyperlipoproteinemia), and Homozygous Familial Hypercholesterolemia.[F4649] The Health Canada monograph for rosuvastatin further specifies that rosuvastatin is indicated for the reduction of elevated total cholesterol (Total-C), LDL-C, ApoB, the Total-C/HDL-C ratio and triglycerides (TG) and for increasing HDL-C in hyperlipidemic and dyslipidemic conditions when response to diet and exercise alone has been inadequate. It is also indicated for the prevention of major cardiovascular events (including risk of myocardial infarction, nonfatal stroke, and coronary artery revascularization) in adult patients without documented history of cardiovascular or cerebrovascular events, but with at least two conventional risk factors for cardiovascular disease.[F4652] Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.[A181087, A181406]
DB08860PitavastatinPitavastatin is indicated for the treatment of adult patients with primary hyperlipidemia or mixed dyslipidemia to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C). It is also indicated for the treatment of pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia (HeFH) to reduce elevated TC, LDL-C, and Apo B.[F4667] Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.[A181087, A181406]
DB06693MevastatinNot used therapeutically due to its many side effects.
DrugDrug NameTargetType
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
DB00175PravastatinHistone deacetylase 2target
DB00227Lovastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB00227LovastatinCytochrome P450 3A4enzyme
DB00227LovastatinCytochrome P450 2C8enzyme
DB00227LovastatinIntegrin alpha-Ltarget
DB00227LovastatinHistone deacetylase 2target
DB00227LovastatinSerum paraoxonase/lactonase 3enzyme
DB00227LovastatinMultidrug resistance protein 1transporter
DB00227LovastatinSolute carrier organic anion transporter family member 1A2transporter
DB00227LovastatinSolute carrier organic anion transporter family member 1B1transporter
DB00227LovastatinUDP-glucuronosyltransferase 1-1enzyme
DB00227LovastatinUDP-glucuronosyltransferase 1-3enzyme
DB00227LovastatinUDP-glucuronosyltransferase 2B7enzyme
DB00227LovastatinCanalicular multispecific organic anion transporter 1transporter
DB00227LovastatinBile salt export pumptransporter
DB00227LovastatinSerum albumincarrier
DB00227LovastatinCytochrome P450 2C19enzyme
DB00227LovastatinSolute carrier organic anion transporter family member 2B1transporter
DB00227LovastatinSolute carrier organic anion transporter family member 1B3transporter
DB00439Cerivastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB00439CerivastatinCytochrome P450 2C8enzyme
DB00439CerivastatinCytochrome P450 3A4enzyme
DB00439CerivastatinCytochrome P450 2D6enzyme
DB00439CerivastatinCytochrome P450 2C9enzyme
DB00439CerivastatinCytochrome P450 3A5enzyme
DB00439CerivastatinCytochrome P450 3A7enzyme
DB00439CerivastatinMultidrug resistance protein 1transporter
DB00439CerivastatinCanalicular multispecific organic anion transporter 1transporter
DB00439CerivastatinATP-binding cassette sub-family G member 2transporter
DB00439CerivastatinSolute carrier organic anion transporter family member 1B1transporter
DB00439CerivastatinCytochrome P450 2B6enzyme
DB00439CerivastatinUDP-glucuronosyltransferase 1-1enzyme
DB00439CerivastatinBile salt export pumptransporter
DB00641Simvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB00641SimvastatinCytochrome P450 3A4enzyme
DB00641SimvastatinCytochrome P450 2C8enzyme
DB00641SimvastatinCytochrome P450 2C9enzyme
DB00641SimvastatinCytochrome P450 3A5enzyme
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
DB00641SimvastatinCytochrome P450 2C19enzyme
DB00641SimvastatinSolute carrier organic anion transporter family member 2B1transporter
DB00641SimvastatinSolute carrier organic anion transporter family member 1B3transporter
DB00641SimvastatinHistone deacetylase 2target
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
DB01076AtorvastatinHistone deacetylase 2target
DB01076AtorvastatinNuclear receptor subfamily 1 group I member 3target
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
DB01095FluvastatinHistone deacetylase 2target
DB01098Rosuvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB01098RosuvastatinCytochrome P450 2C9enzyme
DB01098RosuvastatinMultidrug resistance-associated protein 4transporter
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
DB01098RosuvastatinSodium/bile acid cotransportertransporter
DB01098RosuvastatinIntegrin alpha-Ltarget
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
DB08860PitavastatinIntegrin alpha-Ltarget
DB06693Mevastatin3-hydroxy-3-methylglutaryl-coenzyme A reductasetarget
DB06693MevastatinLiver carboxylesterase 1enzyme