Serine Proteinase Inhibitors

Exogenous or endogenous compounds which inhibit SERINE ENDOPEPTIDASES.
DrugDrug NameDrug Indication
DB00001LepirudinFor the treatment of heparin-induced thrombocytopenia
DB00006BivalirudinFor treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
DB00058Alpha-1-proteinase inhibitorFor chronic augmentation and maintenance therapy in individuals with alpha1-proteinase inhibitor (A1-PI) deficiency and clinical evidence of emphysema.
DB00278ArgatrobanArgatroban is indicated for prevention and treatment of thrombosis caused by heparin induced thrombocytopenia (HIT). It is also indicated for use in patients with, or at risk for, HIT who are undergoing percutaneous coronary intervention.
DB01683ChymostatinNot Available
DB03127BenzamidineNot Available
DB044593,4-DichloroisocoumarinNot Available
DB04898XimelagatranFor the treatment of acute deep vein thrombosis.
DB06228RivaroxabanRivaroxaban is indicated for the prevention of venous thromboembolic events (VTE) in patients who have undergone total hips replacements and total knee replacement surgery; prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation; treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE); to reduce risk of recurrent DVT and/or PE. Rivaroxaban is also indicated, in combination with aspirin, for reducing the risk of major cardiovascular events in patients with chronic coronary artery disease or peripheral artery disease. Due to a lack of safety studies, it is not recommended for use in those under 18 years old. Its use is also not recommended in those with severe renal impairment (<30mL/min).
DB06406IdraparinuxInvestigated for use/treatment in thrombosis, venous thromboembolism, strokes, heart disease, and atrial fibrillation.
DB06605ApixabanApixaban is indicated for reducing the risk of stroke and systemic embolism in patients who have nonvalvular atrial fibrillation, prophylaxis of deep vein thrombosis(DVT) leading to pulmonary embolism(PE) in patients after a hip or knee replacement surgery, and treatment of DVT and PE to reduce the risk of recurrence[Label,A177565,A6897].
DB06635OtamixabanInvestigated for use/treatment in thrombosis.
DB06692AprotininFor prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion.
DB06695Dabigatran etexilateDabigatran is indicated for the prevention of venous thromboembolic events in patients who have undergone elective hip or knee replacement surgery (based on RE-NOVATE, RE-MODEL, and RE-MOBILIZE trials)[A177463,A6978,A6977]. In 2010, it was approved in the US and Canada for prevention of stroke and systemic embolism in patients with atrial fibrillation (approval based on the RE-LY trial)[Label,A177463].
DB073474-(2-Aminoethyl)Benzenesulfonyl FluorideNot Available
DB09075EdoxabanEdoxaban is indicated for reducing the risk of stroke and systemic embolism (SE) in patients with nonvalvular atrial fibrillation (NVAF). However, it should not be used in patients with creatinine clearance (CrCL) > 95 mL/min because of increased risk of ischemic stroke compared to warfarin at the highest dose studied (60 mg). It is also indicated for the treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE) following 5-10 days of initial therapy with a parenteral anticoagulant.
DB11598Antithrombin III humanAntithrombin III human is a human antithrombin (AT) indicated in patients with hereditary antithrombin deficiency for the treatment and prevention of thromboembolism and prevention of peri-operative and peri-partum thromboembolism
DB11984LetaxabanNot Available
DB12038UlinastatinNot Available
DB12289DarexabanNot Available
DB12598NafamostatUsed as an anticoagulant in patients with disseminative blood vessel coagulation, hemorrhagic lesions, and hemorrhagic tendencies. It prevents blood clot formation during extracorporeal circulation in patients undergoing continuous renal replacement therapy and extra corporeal membrane oxygenation.
DB12831GabexateNo approved indication.
DB12863SivelestatNot Available
DB13616MelagatranNot Available
DB13729CamostatNot Available
DB01990Cholesterol sulfateNot Available
DB14726DabigatranNot Available
DrugDrug NameTargetType
DB00058Alpha-1-proteinase inhibitorNeutrophil elastasetarget
DB00278ArgatrobanCytochrome P450 3A4enzyme
DB00278ArgatrobanCytochrome P450 3A5enzyme
DB01683ChymostatinPeptide amidasetarget
DB03127BenzamidineUrokinase-type plasminogen activatortarget
DB03127BenzamidineCasein kinase II subunit alphatarget
DB03127BenzamidineCopper transport protein ATOX1target
DB03127BenzamidineEnoyl-CoA delta isomerase 1, mitochondrialtarget
DB03127BenzamidineSuppressor of tumorigenicity 14 proteintarget
DB044593,4-DichloroisocoumarinComplement factor Dtarget
DB04898XimelagatranCytochrome P450 2C9enzyme
DB06228RivaroxabanCoagulation factor Xtarget
DB06228RivaroxabanCytochrome P450 3A4enzyme
DB06228RivaroxabanCytochrome P450 2J2enzyme
DB06228RivaroxabanMultidrug resistance protein 1transporter
DB06228RivaroxabanCytochrome P450 3A5enzyme
DB06228RivaroxabanATP-binding cassette sub-family G member 2transporter
DB06406IdraparinuxCoagulation factor Xtarget
DB06605ApixabanCoagulation factor Xtarget
DB06605ApixabanCytochrome P450 3A4enzyme
DB06605ApixabanCytochrome P450 1A2enzyme
DB06605ApixabanCytochrome P450 2C8enzyme
DB06605ApixabanCytochrome P450 2C9enzyme
DB06605ApixabanCytochrome P450 2C19enzyme
DB06605ApixabanCytochrome P450 2J2enzyme
DB06605ApixabanMultidrug resistance protein 1transporter
DB06605ApixabanATP-binding cassette sub-family G member 2transporter
DB06605ApixabanCytochrome P450 3A5enzyme
DB06635OtamixabanCoagulation factor Xtarget
DB06692AprotininChymotrypsinogen Btarget
DB06695Dabigatran etexilateProthrombintarget
DB06695Dabigatran etexilateMultidrug resistance protein 1transporter
DB06695Dabigatran etexilateLiver carboxylesterase 1enzyme
DB06695Dabigatran etexilateCocaine esteraseenzyme
DB06695Dabigatran etexilateUDP-glucuronosyltransferase 1-9enzyme
DB06695Dabigatran etexilateUDP-glucuronosyltransferase 2B7enzyme
DB06695Dabigatran etexilateUDP-glucuronosyltransferase 2B15enzyme
DB06695Dabigatran etexilateRibosyldihydronicotinamide dehydrogenase [quinone]enzyme
DB073474-(2-Aminoethyl)Benzenesulfonyl FluorideGlyceraldehyde-3-phosphate dehydrogenasetarget
DB073474-(2-Aminoethyl)Benzenesulfonyl FluorideV-type proton ATPase subunit B, brain isoformtarget
DB09075EdoxabanCoagulation factor Xtarget
DB09075EdoxabanMultidrug resistance protein 1transporter
DB11598Antithrombin III humanAntithrombin-IIItarget
DB12598NafamostatIntercellular adhesion molecule 1target
DB12598NafamostatCoagulation factor Xtarget
DB12598NafamostatCoagulation factor XIItarget
DB12598NafamostatSolute carrier family 22 member 1transporter
DB12598NafamostatSolute carrier family 22 member 2transporter
DB12831GabexateComplement C1s subcomponentenzyme
DB12831GabexateComplement C1r subcomponentenzyme
DB12831GabexatePlasma kallikreintarget
DB01990Cholesterol sulfateNuclear receptor ROR-alphatarget