PMID- 24647152 OWN - NLM STAT- MEDLINE DCOM- 20140814 LR - 20191112 IS - 1881-7831 (Print) IS - 1881-7831 (Linking) VI - 8 IP - 1 DP - 2014 Feb TI - Pharmacological effects and clinical applications of ultra low molecular weight heparins. PG - 1-10 AB - Heparin, one of the common anticoagulants, is clinically used to prevent and treat venous thromboembolism (VTE). Though it has been the drug of choice for many advanced medical and surgical procedures with a long history, the adverse events, such as bleeding, heparin-induced thrombocytopenia (HIT), allergic reactions, follow. Therefore, low molecular weight heparins (LMWHs) and ultra low molecular weight heparins (ULMWHs), with lower molecular weights, higher anti-FXa activity, longer half-life times and lower incidence of adverse events than unfractionated heparin (UFH), were researched and developed. Fondaparinux, a chemically synthesized ULMWH of pentasaccharide, has the same antithrombin III (AT-III)-binding sequence as found in UFH and LMWH. In addition, AVE5026 and RO-14, another two ULMWHs, are obtained by selective chemical depolymerization. In this paper, we review the preparation process, pharmacological effects and clinical applications of fondaparinux, AVE5026 and RO-14. FAU - Liu, Zhang AU - Liu Z AD - Key Laboratory of Chemical Biology of Natural Products (Ministry of Education), Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Sciences, Shandong University. FAU - Ji, Shengli AU - Ji S FAU - Sheng, Juzheng AU - Sheng J FAU - Wang, Fengshan AU - Wang F LA - eng PT - Journal Article PT - Review PL - Japan TA - Drug Discov Ther JT - Drug discoveries & therapeutics JID - 101493809 RN - 0 (AVE 5026) RN - 0 (Anticoagulants) RN - 0 (Factor Xa Inhibitors) RN - 0 (Heparin, Low-Molecular-Weight) RN - 0 (Polysaccharides) RN - 9005-49-6 (Heparin) RN - EC 3.4.21.6 (Factor Xa) RN - J177FOW5JL (Fondaparinux) SB - IM MH - Animals MH - Anticoagulants/adverse effects/chemical synthesis/pharmacokinetics/*therapeutic use MH - Blood Coagulation/drug effects MH - *Drug Design MH - Factor Xa/metabolism MH - Factor Xa Inhibitors MH - Fondaparinux MH - Half-Life MH - Hemorrhage/chemically induced MH - Heparin/analogs & derivatives/therapeutic use MH - Heparin, Low-Molecular-Weight/adverse effects/chemical synthesis/pharmacokinetics/*therapeutic use MH - Humans MH - Molecular Structure MH - Molecular Weight MH - Polysaccharides/therapeutic use MH - Structure-Activity Relationship MH - Venous Thromboembolism/*drug therapy EDAT- 2014/03/22 06:00 MHDA- 2014/08/15 06:00 CRDT- 2014/03/21 06:00 PHST- 2014/03/21 06:00 [entrez] PHST- 2014/03/22 06:00 [pubmed] PHST- 2014/08/15 06:00 [medline] AID - DN/JST.JSTAGE/ddt/8.1 [pii] AID - 10.5582/ddt.8.1 [doi] PST - ppublish SO - Drug Discov Ther. 2014 Feb;8(1):1-10. doi: 10.5582/ddt.8.1.