Products Rivaroxaban is commercially available in the form of film-coated tablets (Xarelto, Xarelto vascular). It was approved in 2008 as the first agent in the direct factor Xa inhibitor group. Low-dose Xarelto vascular, 2.5 mg, was registered in many countries in 2019. Structure and properties Rivaroxaban (C19H18ClN3O5S, Mr = 435.9 g/mol) is a pure -enantiomer … Rivaroxaban
Products Enoxaparin is commercially available as a solution for injection (Clexane). It has been approved in many countries since 1988. Biosimilars were released in the EU in 2016 and in many countries in 2020 (Inhixa). Structure and properties Enoxaparin is present in the drug as enoxaparin sodium, the sodium salt of a low-molecular-weight heparin (LMWH) … Enoxaparin
Products Nadroparin is commercially available as a solution for injection (Fraxiparine, Fraxiforte). It has been approved in many countries since 1988. Structure and properties Nadroparin is present in the drug as nadroparin calcium. It is the calcium salt of a low-molecular-weight heparin obtained by depolymerization of heparin from the intestinal mucosa of pigs using nitrous … Nadroparin
Products Reteplase was marketed as an injectable (Rapilysin). The drug was approved in many countries in 1996 and withdrawn from the market in 2013. Structure and properties Reteplase is derivative of tissue-specific plasminogen activator (t-PA). It is a serine protease containing 355 of the 527 amino acids of native t-PA. The protein is produced by … Reteplase
Products Edoxaban was approved in many countries and in the United States in 2015 in film-coated tablet form (Lixiana, some countries: Savaysa). In Japan, edoxaban was approved as early as 2011. Structure and properties Edoxaban (C24H30ClN7O4S, Mr = 548.1 g/mol) is present in the drug as edoxabantosilate monohydrate, a white to pale yellow powder that … Edoxaban
Effects Antithrombin III (ATC B01AB02) is anticoagulant: it is an endogenous substance that inhibits blood clotting. Its action is enhanced by heparins, which bind to and activate antithrombin III. Indications Substitution therapy in patients with congenital antithrombin III deficiency.
Products Low-molecular-weight heparins are commercially available as injectable solutions, in the form of prefilled syringes, ampoules, and lancing ampoules. The active ingredients now commonly used in many countries were first approved in the late 1980s. Biosimilars are available in some countries. The active ingredients are abbreviated in English with the acronym LMWH (low molecular weight … Low-Molecular-Weight Heparins
Products Fondaparinux is commercially available as a solution for injection (Arixtra). It has been approved in many countries since 2002. Structure and properties Fondaparinux (C31H43N3Na10O49S8, Mr = 1728 g/mol) is a synthetic pentasaccharide belonging to the class of glycosaminoglycans. It is present in the drug as fondaparinux sodium. Effects Fondaparinux (ATC B01AX05) has antithrombotic properties. … Fondaparinux
Products Defibrotide was approved in many countries in 2020 as a concentrate for the preparation of an infusion solution (Defitelio). Structure and properties Defibrotide is a mixture of single-stranded oligonucleotides derived from porcine intestinal mucosa. Effects Defibrotide (ATC B01AX01) has antithrombotic, fibrinolytic, antiadhesive, and anti-inflammatory properties. Indications For the treatment of severe hepatic veno-occlusive disease … Defibrotide
Products Lepirudin was commercially available as a lyophilizate (Refludan). It was approved in many countries in 1997 and is no longer on the market. Structure and properties Lepirudin is a derivative of hirudin from the leech. Effects Lepirudin (ATC B01AX03) is anticoagulant by direct inhibition of thrombin. Indications Heparin-associated thrombocytopenia (HAT) type II.
Products Dalteparin is commercially available as an injectable (Fragmin). It has been approved in many countries since 1988. Structure and properties Dalteparin is present in drugs as dalteparin sodium, the sodium salt of a low-molecular-weight heparin obtained by depolymerization of heparin from porcine intestinal mucosa using nitrous acid. The average molecular weight is 6000 Da. … Dalteparin
Products Drotrecogin alfa was commercially available as a lyophilizate (Xigris). It has been approved in many countries and in the EU since 2002 and was also available in the United States and Canada. In 2011, Eli Lilly announced it was withdrawing the drug from the market worldwide. The PROWESS-SHOCK study showed insufficient efficacy. Mortality was … Drotrecogin Alfa
