Cardiovascular Events

Also known as: Cardiac Event / Cardiovascular events (all) / Cardiovascular Event / Cardiac Events

DrugDrug NameDrug Description
DB00945Acetylsalicylic acidThe prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Acetylsalicylic acid also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)
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.
DB00612BisoprololBisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Bisoprolol is structurally similar to metoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At lower doses (less than 20 mg daily), bisoprolol selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with daily doses of 20 mg or greater. Unlike propranolol and pindolol, bisoprolol does not exhibit membrane-stabilizing or sympathomimetic activity. Bisoprolol possesses a single chiral centre and is administered as a racemic mixture. Only l-bisoprolol exhibits significant β-blocking activity.
DB00758ClopidogrelClopidogrel, an antiplatelet agent structurally and pharmacologically similar to ticlopidine, is used to inhibit blood clots in a variety of conditions such as peripheral vascular disease, coronary artery disease, and cerebrovascular disease. Clopidogrel is sold under the name Plavix by Sanofi and Bristol-Myers Squibb. The drug is an irreversible inhibitor of the P2Y12 adenosine diphosphate receptor found on the membranes of platelet cells. Clopidogrel use is associated with several serious adverse drug reactions such as severe neutropenia, various forms of hemorrhage, and cardiovascular edema.
DB06779DalteparinDalteparin, a low molecular weight heparin (LMWH) prepared by nitrous acid degradation of unfractionated heparin of porcine intestinal mucosa origin, is an anticoagulant. It is composed of strongly acidic sulphated polysaccharide chains with an average molecular weight of 5000 and about 90% of the material within the range of 2000-9000. LMWHs have a more predictable response, a greater bioavailability, and a longer anti-Xa half life than unfractionated heparin. Dalteparin can also be safely used in most pregnant women. Low molecular weight heparins are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.
DB00722LisinoprilLisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Lisinopril may be used to treat hypertension and symptomatic congestive heart failure, to improve survival in certain individuals following myocardial infarction, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy.
DB06209PrasugrelPrasugrel, a thienopyridine derivative, is a platelet activation and aggregation inhibitor structurally and pharmacologically related to clopidogrel and ticlopidine. Similar to clopidogrel, prasugrel is a prodrug that requires enzymatic transformation in the liver to its active metabolite, R-138727. R-138727 irreversibly binds to P2Y12 type ADP receptors on platelets thus preventing activation of the GPIIb/IIIa receptor complex. As a result, inhibition of ADP-mediated platelet activation and aggregation occurs. Prasugrel was developed by Daiichi Sankyo Co. and is currently marketed in the United States and Canada in cooperation with Eli Lilly and Company for acute coronary syndromes planned for percutaneous coronary intervention (PCI). FDA approved in 2009.
DB09292SacubitrilSacubitril is a prodrug neprilysin inhibitor used in combination with valsartan to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015. Sacubitril's active metabolite, LBQ657 inhibits neprilysin, a neutral endopeptidase that would typically cleave natiuretic peptides such as atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP). ANP and BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis. Under normal conditions, neprilysin breaks down other vasodilating peptides and also vasoconstrictors such as angiotensin I and II, endothelin-1 and peptide amyloid beta-protein. Inhibition of neprilysin therefore leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II.
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.
DB00966TelmisartanTelmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects.
DB08816TicagrelorTicagrelor (trade name Brilinta in the US, Brilique and Possia in the EU) is a platelet aggregation inhibitor produced by AstraZeneca. Unlike clopidogrel, ticagrelor is not a prodrug and does not require metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010. The drug was approved by the US Food and Drug Administration on July 20, 2011.
DB00373TimololA beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of migraine disorders and tremor.
DB00775TirofibanTirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation.
DB09030VorapaxarVorapaxar is a tricyclic himbacine-derived selective inhibitor of protease activated receptor (PAR-1) indicated for reducing the incidence of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD). By inhibiting PAR-1, a thrombin receptor expressed on platelets, vorapaxar prevents thrombin-related platelet aggregation.
DrugDrug NameTargetType
DB00945Acetylsalicylic acidProstaglandin G/H synthase 1target
DB00945Acetylsalicylic acidProstaglandin G/H synthase 2target
DB00945Acetylsalicylic acidSerum albumincarrier
DB00945Acetylsalicylic acidAldo-keto reductase family 1 member C1target
DB00945Acetylsalicylic acidSolute carrier family 22 member 6transporter
DB00945Acetylsalicylic acidMultidrug resistance protein 1transporter
DB00945Acetylsalicylic acidSolute carrier family 22 member 7transporter
DB00945Acetylsalicylic acidCytochrome P450 2C19enzyme
DB00945Acetylsalicylic acidCytochrome P450 2C8enzyme
DB00945Acetylsalicylic acidCytochrome P450 2C9enzyme
DB00945Acetylsalicylic acid5'-AMP-activated protein kinasetarget
DB00945Acetylsalicylic acidEndothelin-1 receptortarget
DB00945Acetylsalicylic acidInhibitor of nuclear factor kappa-B kinase subunit betatarget
DB00945Acetylsalicylic acidCellular tumor antigen p53target
DB00945Acetylsalicylic acid78 kDa glucose-regulated proteintarget
DB00945Acetylsalicylic acidRibosomal protein S6 kinase alpha-3target
DB00945Acetylsalicylic acidNF-kappa-B inhibitor alphatarget
DB00945Acetylsalicylic acidNuclear factor NF-kappa-Btarget
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
DB00612BisoprololBeta-1 adrenergic receptortarget
DB00612BisoprololBeta-2 adrenergic receptortarget
DB00612BisoprololCytochrome P450 2D6enzyme
DB00612BisoprololCytochrome P450 3A4enzyme
DB00758ClopidogrelP2Y purinoceptor 12target
DB00758ClopidogrelCytochrome P450 3A4enzyme
DB00758ClopidogrelCytochrome P450 2B6enzyme
DB00758ClopidogrelCytochrome P450 3A5enzyme
DB00758ClopidogrelCytochrome P450 2C19enzyme
DB00758ClopidogrelCytochrome P450 2C9enzyme
DB00758ClopidogrelCytochrome P450 1A2enzyme
DB00758ClopidogrelCytochrome P450 2C8enzyme
DB00758ClopidogrelLiver carboxylesterase 1enzyme
DB00758ClopidogrelMultidrug resistance protein 1transporter
DB00758ClopidogrelSolute carrier family 22 member 1transporter
DB00758ClopidogrelSolute carrier family 22 member 2transporter
DB06779DalteparinVascular endothelial growth factor Atarget
DB06779DalteparinTissue factor pathway inhibitortarget
DB00722LisinoprilAngiotensin-converting enzymetarget
DB06209PrasugrelP2Y purinoceptor 12target
DB06209PrasugrelCocaine esteraseenzyme
DB06209PrasugrelCytochrome P450 3A4enzyme
DB06209PrasugrelCytochrome P450 2B6enzyme
DB06209PrasugrelCytochrome P450 2C9enzyme
DB06209PrasugrelCytochrome P450 2C19enzyme
DB06209PrasugrelSerum albumincarrier
DB09292SacubitrilSolute carrier organic anion transporter family member 1B1transporter
DB09292SacubitrilSolute carrier organic anion transporter family member 1B3transporter
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
DB00966TelmisartanType-1 angiotensin II receptortarget
DB00966TelmisartanPeroxisome proliferator-activated receptor gammatarget
DB00966TelmisartanMultidrug resistance protein 1transporter
DB00966TelmisartanCanalicular multispecific organic anion transporter 1transporter
DB00966TelmisartanATP-binding cassette sub-family G member 2transporter
DB00966TelmisartanCytochrome P450 2C19enzyme
DB00966TelmisartanBile salt export pumptransporter
DB00966TelmisartanUDP-glucuronosyltransferase 1-3enzyme
DB08816TicagrelorCytochrome P450 3A4enzyme
DB08816TicagrelorP2Y purinoceptor 12target
DB08816TicagrelorMultidrug resistance protein 1transporter
DB08816TicagrelorCytochrome P450 2D6enzyme
DB08816TicagrelorCytochrome P450 2C9enzyme
DB00373TimololBeta-1 adrenergic receptortarget
DB00373TimololBeta-2 adrenergic receptortarget
DB00373TimololCytochrome P450 2D6enzyme
DB00373TimololMultidrug resistance protein 1transporter
DB00373TimololCytochrome P450 2C19enzyme
DB00775TirofibanIntegrin alpha-IIbtarget
DB00775TirofibanIntegrin beta-3target
DB09030VorapaxarProteinase-activated receptor 1target
DB09030VorapaxarCytochrome P450 3A4enzyme
DB09030VorapaxarCytochrome P450 2J2enzyme
DrugDrug NamePhaseStatusCount
DB06724Calcium Carbonate4Completed1
DB00258Calcium acetate4Completed1
DB01184Domperidone4Not Yet Recruiting1
DB00448Lansoprazole4Not Yet Recruiting1
DB01112CefuroximeNot AvailableWithdrawn1
DB01235LevodopaNot AvailableCompleted1