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Briefing Therapeutic Approaches in Anticoagulant, Thrombolytic, and Antiplatelet Therapy
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Idraparinux and idrabiotaparinux (Figure 7.4) are polymethylated derivatives of fondaparinux. Their elimination half-life increases from 7 days after single administration up to 60 days after a 6–12 month treatment period. However, the development of idraparinux and idrabiotaparinux is halted. Biotinylated idraparinux, named idrabiotaparinux, is structurally similar to idraparinux, with the addition of a biotin segment. It has the same anticoagulant activity as idraparinux. Avidin exposes a strong affinity to biotin and can be given intravenously to rapidly bind, neutralize and eliminate idrabiotaparinux [43, 44].
Fibrinolytic Enzymes for Thrombolytic Therapy
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Swaroop S. Kumar, Sabu Abdulhameed
Factor Xa is a serine protease and since it is part of prothrombinase complex, it carries crucial role in blood coagulation. Factor Xa inhibitors are another class of anticoagulant drugs reducing thrombin formation. These small molecules bind with active site of factor X (Xa), which in turn inhibits the formation of thrombin. They demonstrate varying structural and functional diversity and can be either naturally occurring or synthetic molecule and chemically it can be peptide, protein, or heparin saccharidic sequences (Fareed et al., 1999; Leone et al., 2004; Bauer, 2006; Samama et al., 1999). Their mode of action could be either direct by binding to factor Xa or indirect through binding with antithrombin III (AT), leading to Factor Xa inactivation. The interaction of Xa inhibitors could be reversible or irreversible (Harenberg and Fenyvesi, 2004; Walenga et al., 2002). Fondaparinux is a heparin pentasaccharide, the FDA approved this for its use after surgery and also for initial management of thrombotic disorders such as pulmonary embolism and deep vein thrombosis trials (Hoppensteadt et al., 2008). Another indirect-acting FXa inhibitor is Idraparinux (SANORG-34006), which is a hyper methylated variant of fondaparinux and showed more affinity towards antithrombin III (AT) (PERSIST investigators, 2004). Rivaroxaban was an orally active, direct thrombin inhibitor and extensively studied for its use in preventing venous thromboembolism during knee and hip replacement (Turpie et al., 2005; Eriksson et al., 2006). A few other direct Factor Xa inhibitors include otamixaban, apixaban, edoxaban, etc. Although most of the Factor Xa inhibitors are either under clinical trial or in different developmental stages, still they are considered safer than thrombin inhibitors (Hoppensteadt et al., 2008).
Antithrombotic therapy for secondary prevention of unprovoked venous thromboembolism: a systematic review and network meta-analysis of randomized controlled trials
Published in Annals of Medicine, 2022
Dandan Li, Yi Liu, Yao Song, Aiping Wen
Many meta-analyses have compared the efficacy and safety of different antithrombotic strategies for secondary prevention of VTE patients including the provoked and unprovoked: Kakkos [11] assessed the DOACs versus placebo, and found that DOACs can reduced recurrent VTE and all-cause mortality at the expense of higher risk of clinically relevant non-major bleeding. Alotaibi [12] compared different DOACs, and found no significant differences in risk for recurrent VTE, major bleeding, or all-cause mortality. Using network meta-analysis method, Sobieraj [13] found that oral anticoagulants (including apixaban, dabigatran, rivaroxaban, and warfarin) and idraparinux were superior to placebo on recurrent VTE, while Rollins [14] found that no differences among oral anticoagulants and placebo on the composite end point of VTE or death, nonfatal PE, or DVT. However, apixaban demonstrated a more favourable safety profile compared to other therapies in both studies [13,14].