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Details on Person Some direct oral anticoagulant (DOAC) drugs are potent, comp...

Class:IdSummation:9603336
_displayNameSome direct oral anticoagulant (DOAC) drugs are potent, comp...
_timestamp2025-01-12 01:59:37
created[InstanceEdit:9603337] Jassal, Bijay, 2018-03-19
literatureReference[LiteratureReference:9015353] The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects
[LiteratureReference:9603313] Novastan (brand of argatroban): a small-molecule, direct thrombin inhibitor
[LiteratureReference:9603314] Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III-independent inhibitors
[LiteratureReference:9603309] Bivalirudin: a direct thrombin inhibitor
[LiteratureReference:9603304] Desirudin: a review of the pharmacology and clinical application for the prevention of deep vein thrombosis
[LiteratureReference:9603680] Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes
[LiteratureReference:9603708] Inhibition of the thrombin-platelet reactions by DuP 714
modified[InstanceEdit:9603338] Jassal, Bijay, 2018-03-19
[InstanceEdit:9603713] Jassal, Bijay, 2018-03-23
[InstanceEdit:9935011] Shamovsky, Veronica, 2025-01-12
textSome direct oral anticoagulant (DOAC) drugs are potent, competitive direct thrombin inhibitors (DTIs). They reversibly and specifically bind both clot-bound and free thrombin (unlike warfarin or heparin), as well as inhibiting thrombin-induced platelet aggregation. These drugs can be synthetic organic compounds (dabigatran, argatroban) or recombinant peptides (lepirudin, bivalirudin, desirudin). Dabigatran (brand name Pradexa) is formulated as a lipophilic prodrug, dabigatran etexilate, to promote gastrointestinal absorption before it is metabolised to the active drug. The kidneys excrete the majority (80%) of unchanged drug (Stangier J et al. 2007). Argatroban is a synthetic inhibitor of thrombin derived from L-arginine, which has a relatively short period of binding only to thrombin’s active site (Hursting MJ et al. 1997). It is given intravenously and is metabolised in the liver. Because of its hepatic metabolism, it may be used in patients with renal dysfunction. Lepirudin (brand name Refludan) is a recombinant hirudin derived from yeast cells (Weitz JI et al. 1990). Hirudin is a naturally occurring anticoagulant produced by the salivary glands of medicinal leeches. Bivalirudin (brand name Angiomax, Angiox) is a synthetic analog of hirudin, with a shorter period of binding to thrombin (Gladwell TD 2002). Desirudin (brand name Iprivask) is another recombinant hirudin derivative that directly inhibits free and fibrin-bound thrombin (Graetz TJ et al. 2011). Melagatran is the active drug formed from the prodrug ximelagatran and is a competitive and rapid inhibitor of thrombin (Gustafsson D et al. 1998). DuP 714 is a potent and specific thrombin inhibitor (Chiu AT et al. 1991).
(summation)[Reaction:140599] factor XIII -> factor XIII cleaved tetramer + 2 factor XIII A activation peptides [Homo sapiens]
[Reaction:140840] fibrinogen -> fibrin monomer + 2 fibrinopeptide A + 2 fibrinopeptide B [Homo sapiens]
[Reaction:158137] factor VIII:von Willibrand factor multimer -> factor VIIIa + factor VIIIa B A3 acidic polypeptide + von Willibrand factor multimer [Homo sapiens]
[Reaction:158419] factor XI:platelet glycoprotein (GP) Ib:IX:V complex -> factor XIa:platelet glycoprotein (GP) Ib:IX:V complex (thrombin catalyst) [Homo sapiens]
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