Ximelagatran (BioDeep_00000033350)

   

human metabolite blood metabolite Chemicals and Drugs


代谢物信息卡片


Glycine, N-((1R)1-cyclohexyl-2-((2S)-((((4-(amino(hydroxyimino)methyl)phenyl)methyl)amino)carbonyl)-1-azetidinyl)2-oxoethyl)-ethyl ester

化学式: C24H35N5O5 (473.26380600000005)
中文名称: 希美加群
谱图信息: 最多检出来源 Homo sapiens(blood) 22.58%

分子结构信息

SMILES: CCOC(=O)CNC(C1CCCCC1)C(=O)N2CCC2C(=O)NCC3=CC=C(C=C3)C(=NO)N
InChI: InChI=1S/C24H35N5O5/c1-2-34-20(30)15-26-21(17-6-4-3-5-7-17)24(32)29-13-12-19(29)23(31)27-14-16-8-10-18(11-9-16)22(25)28-33/h8-11,17,19,21,26,33H,2-7,12-15H2,1H3,(H2,25,28)(H,27,31)/t19-,21+/m0/s1

描述信息

Ximelagatran (Exanta or Exarta, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would not attempt to market ximelagatran after reports of hepatotoxicity (liver damage) during trials, and to discontinue its distribution in countries where the drug had been approved.
B - Blood and blood forming organs > B01 - Antithrombotic agents > B01A - Antithrombotic agents > B01AE - Direct thrombin inhibitors
D004791 - Enzyme Inhibitors > D011480 - Protease Inhibitors > D015842 - Serine Proteinase Inhibitors
D006401 - Hematologic Agents > D000925 - Anticoagulants > D000991 - Antithrombins
C78275 - Agent Affecting Blood or Body Fluid > C263 - Anticoagulant Agent

同义名列表

14 个代谢物同义名

Glycine, N-((1R)1-cyclohexyl-2-((2S)-((((4-(amino(hydroxyimino)methyl)phenyl)methyl)amino)carbonyl)-1-azetidinyl)2-oxoethyl)-ethyl ester; Ethyl 2-[[(1R)-1-cyclohexyl-2- [(2S)-2-[[4-(n-hydroxycarbamimidoyl) phenyl]methylcarbamoyl]azetidin-1-yl]- 2-oxo-ethyl]amino]acetic acid; Glycine, N-((1)1-cyclohexyl-2-((2)-((((4-(amino(hydroxyimino)methyl)phenyl)methyl)amino)carbonyl)-1-azetidinyl)2-oxoethyl)-ethyl ester; ethyl 2-{[(1R)-1-cyclohexyl-2-[(2S)-2-[({4-[(Z)-N-hydroxycarbamimidoyl]phenyl}methyl)carbamoyl]azetidin-1-yl]-2-oxoethyl]amino}acetate; Ethyl 2-[[(1R)-1-cyclohexyl-2- [(2S)-2-[[4-(n-hydroxycarbamimidoyl) phenyl]methylcarbamoyl]azetidin-1-yl]- 2-oxo-ethyl]amino]acetate; Ximelagatran (oxime form); Ximelagatranum; XI-melagatran; ximelagatran; H 376-95; H 376/95; H 37695; Exarta; Exanta



数据库引用编号

9 个数据库交叉引用编号

分类词条

相关代谢途径

Reactome(0)

BioCyc(0)

PlantCyc(0)

代谢反应

0 个相关的代谢反应过程信息。

Reactome(0)

BioCyc(0)

WikiPathways(0)

Plant Reactome(0)

INOH(0)

PlantCyc(0)

COVID-19 Disease Map(0)

PathBank(0)

PharmGKB(0)

1 个相关的物种来源信息

在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：

  • PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。



文献列表

  • Shohei Takai, Shingo Oda, Koichi Tsuneyama, Tatsuki Fukami, Miki Nakajima, Tsuyoshi Yokoi. Establishment of a mouse model for amiodarone-induced liver injury and analyses of its hepatotoxic mechanism. Journal of applied toxicology : JAT. 2016 Jan; 36(1):35-47. doi: 10.1002/jat.3141. [PMID: 25900201]
  • Christer Tannergren, Anders Borde, Cecilia Boreström, Bertil Abrahamsson, Anders Lindahl. Evaluation of an in vitro faecal degradation method for early assessment of the impact of colonic degradation on colonic absorption in humans. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2014 Jun; 57(?):200-6. doi: 10.1016/j.ejps.2013.10.001. [PMID: 24514453]
  • T Nakabayashi, Y Gotoh, N Kamada, M Fujioka, T Ishihara, A Hirabayashi, H Sato. Characterization of in vitro biotransformation of the new oral anticoagulants, the factor VIIa inhibitors AS1927819-00 and AS1932804-00. Die Pharmazie. 2013 Jun; 68(6):406-13. doi: NULL. [PMID: 23875246]
  • Andreas Clemens, Joanne van Ryn, Regina Sennewald, Norio Yamamura, Joachim Stangier, Martin Feuring, Sebastian Härtter. Switching from enoxaparin to dabigatran etexilate: pharmacokinetics, pharmacodynamics, and safety profile. European journal of clinical pharmacology. 2012 May; 68(5):607-16. doi: 10.1007/s00228-011-1205-2. [PMID: 22252796]
  • Michael Wolzt, Ulf G Eriksson, Ghazaleh Gouya, Nicolai Leuchten, Stylianos Kapiotis, Margareta Elg, Kajs-Marie Schützer, Sofia Zetterstrand, Malin Holmberg, Karin Wåhlander. Effect on perfusion chamber thrombus size in patients with atrial fibrillation during anticoagulant treatment with oral direct thrombin inhibitors, AZD0837 or ximelagatran, or with vitamin K antagonists. Thrombosis research. 2012 Apr; 129(4):e83-91. doi: 10.1016/j.thromres.2011.08.018. [PMID: 21925716]
  • Denisa Margina, Mihaela Ilie, Daniela Gradinaru. Quercetin and epigallocatechin gallate induce in vitro a dose-dependent stiffening and hyperpolarizing effect on the cell membrane of human mononuclear blood cells. International journal of molecular sciences. 2012; 13(4):4839-59. doi: 10.3390/ijms13044839. [PMID: 22606013]
  • Santiago Redondo, Maria-Paz Martínez, Marta Ramajo, Jorge Navarro-Dorado, Abelardo Barez, Teresa Tejerina. Pharmacological basis and clinical evidence of dabigatran therapy. Journal of hematology & oncology. 2011 Dec; 4(?):53. doi: 10.1186/1756-8722-4-53. [PMID: 22189016]
  • Raul Altman, Hector O Vidal. Battle of oral anticoagulants in the field of atrial fibrillation scrutinized from a clinical practice (the real world) perspective. Thrombosis journal. 2011 Jul; 9(?):12. doi: 10.1186/1477-9560-9-12. [PMID: 21794130]
  • Elin M Matsson, Ulf G Eriksson, Lars Knutson, Kurt-Jürgen Hoffmann, Ulrika Logren, Patrik Fridblom, Niclas Petri, Hans Lennernäs. Biliary excretion of ximelagatran and its metabolites and the influence of erythromycin following intraintestinal administration to healthy volunteers. Journal of clinical pharmacology. 2011 May; 51(5):770-83. doi: 10.1177/0091270010370975. [PMID: 20663994]
  • T M O'Connell, P B Watkins. The application of metabonomics to predict drug-induced liver injury. Clinical pharmacology and therapeutics. 2010 Sep; 88(3):394-9. doi: 10.1038/clpt.2010.151. [PMID: 20668441]
  • Noriko Konishi, Katsuhiko Hiroe, Masaki Kawamura. Differential effects of TAK-442, a novel orally active direct factor Xa inhibitor, and ximelagatran, a thrombin inhibitor, on factor V-mediated feedback on coagulation cascade and bleeding. Thrombosis and haemostasis. 2010 Sep; 104(3):504-13. doi: 10.1160/th09-12-0817. [PMID: 20664909]
  • David K Cundiff, Paul S Agutter, P Colm Malone, John C Pezzullo. Diet as prophylaxis and treatment for venous thromboembolism?. Theoretical biology & medical modelling. 2010 Aug; 7(?):31. doi: 10.1186/1742-4682-7-31. [PMID: 20701748]
  • Federico M Goodsaid, Shashi Amur, Jiri Aubrecht, Michael E Burczynski, Kevin Carl, Jennifer Catalano, Rosane Charlab, Sandra Close, Catherine Cornu-Artis, Laurent Essioux, Albert J Fornace, Lois Hinman, Huixiao Hong, Ian Hunt, David Jacobson-Kram, Ansar Jawaid, David Laurie, Lawrence Lesko, Heng-Hong Li, Klaus Lindpaintner, James Mayne, Peter Morrow, Marisa Papaluca-Amati, Timothy W Robison, John Roth, Ina Schuppe-Koistinen, Leming Shi, Olivia Spleiss, Weida Tong, Sharada L Truter, Jacky Vonderscher, Agnes Westelinck, Li Zhang, Issam Zineh. Voluntary exploratory data submissions to the US FDA and the EMA: experience and impact. Nature reviews. Drug discovery. 2010 06; 9(6):435-45. doi: 10.1038/nrd3116. [PMID: 20514070]
  • Lars Maegdefessel, Joshua M Spin, Junya Azuma, Philip S Tsao. New options with dabigatran etexilate in anticoagulant therapy. Vascular health and risk management. 2010 May; 6(?):339-49. doi: 10.2147/vhrm.s8942. [PMID: 20531953]
  • M Keisu, T B Andersson. Drug-induced liver injury in humans: the case of ximelagatran. Handbook of experimental pharmacology. 2010; ?(196):407-18. doi: 10.1007/978-3-642-00663-0_13. [PMID: 20020269]
  • Ulf Andersson, Johan Lindberg, Shunghuang Wang, Raji Balasubramanian, Maritha Marcusson-Ståhl, Mira Hannula, Chenhui Zeng, Peter J Juhasz, Johan Kolmert, Jonas Bäckström, Lars Nord, Kerstin Nilsson, Steve Martin, Björn Glinghammar, Karin Cederbrant, Ina Schuppe-Koistinen. A systems biology approach to understanding elevated serum alanine transaminase levels in a clinical trial with ximelagatran. Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals. 2009 Dec; 14(8):572-86. doi: 10.3109/13547500903261354. [PMID: 19780643]
  • Odile Sergent, Kim Ekroos, Luz Lefeuvre-Orfila, Mary Rissel, Gun-Britt Forsberg, Jan Oscarsson, Tommy B Andersson, Dominique Lagadic-Gossmann. Ximelagatran increases membrane fluidity and changes membrane lipid composition in primary human hepatocytes. Toxicology in vitro : an international journal published in association with BIBRA. 2009 Oct; 23(7):1305-10. doi: 10.1016/j.tiv.2009.07.019. [PMID: 19616086]
  • Andreas Goette, Alicja Bukowska, Dobromir Dobrev, Jan Pfeiffenberger, Henning Morawietz, Denis Strugala, Ingrid Wiswedel, Friedrich-Wilhelm Röhl, Carmen Wolke, Sybille Bergmann, Peter Bramlage, Ursula Ravens, Uwe Lendeckel. Acute atrial tachyarrhythmia induces angiotensin II type 1 receptor-mediated oxidative stress and microvascular flow abnormalities in the ventricles. European heart journal. 2009 Jun; 30(11):1411-20. doi: 10.1093/eurheartj/ehp046. [PMID: 19269986]
  • Elin Sjödin, Holger Fritsch, Ulf G Eriksson, Ulrika Logren, Anders Nordgren, Patrik Forsell, Lars Knutson, Hans Lennernäs. Intestinal and hepatobiliary transport of ximelagatran and its metabolites in pigs. Drug metabolism and disposition: the biological fate of chemicals. 2008 Aug; 36(8):1519-28. doi: 10.1124/dmd.108.020412. [PMID: 18458048]
  • Edward K Ainscow, James E Pilling, Nick M Brown, Alexandra T Orme, Michael Sullivan, Andy C Hargreaves, Emma-Louise Cooke, Elaine Sullivan, Stefan Carlsson, Tommy B Andersson. Investigations into the liver effects of ximelagatran using high content screening of primary human hepatocyte cultures. Expert opinion on drug safety. 2008 Jul; 7(4):351-65. doi: 10.1517/14740338.7.4.351. [PMID: 18613800]
  • Kerstin Kenne, Inger Skanberg, Bjorn Glinghammar, Alain Berson, Dominique Pessayre, Jean-Pierre Flinois, Philippe Beaune, Irene Edebert, Cecilia Diaz Pohl, Stefan Carlsson, Tommy B Andersson. Prediction of drug-induced liver injury in humans by using in vitro methods: the case of ximelagatran. Toxicology in vitro : an international journal published in association with BIBRA. 2008 Apr; 22(3):730-46. doi: 10.1016/j.tiv.2007.11.014. [PMID: 18191936]
  • K Gjesdal, J Feyzi, S B Olsson. Digitalis: a dangerous drug in atrial fibrillation? An analysis of the SPORTIF III and V data. Heart (British Cardiac Society). 2008 Feb; 94(2):191-6. doi: 10.1136/hrt.2006.108399. [PMID: 17483128]
  • Alexey Poyarkov, Xavier Rocabayera, Svetlana Poyarkova, Valery Kukhar. Influence of aromatic and aliphatic moieties on thrombin inhibitors potency. The open biochemistry journal. 2008; 2(?):143-9. doi: 10.2174/1874091x00802010143. [PMID: 19238188]
  • Jess L Thompson, Chad E Hamner, D Dean Potter, Matthew Lewin, Thoralf M Sundt, Hartzell V Schaff. Melagatran for thromboprophylaxis after mechanical valve implantation: results in a heterotopic porcine model. The Journal of thoracic and cardiovascular surgery. 2007 Aug; 134(2):359-65. doi: 10.1016/j.jtcvs.2007.01.093. [PMID: 17662773]
  • Kristina Dunér, Jonas Bäckström, Niklas Magnell, Henrik Svennberg, Martin Ahnoff, Ulrika Logren. Determination of ximelagatran, melagatran and two intermediary metabolites in plasma by mixed-mode solid phase extraction and LC-MS/MS. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2007 Jun; 852(1-2):317-24. doi: 10.1016/j.jchromb.2007.01.035. [PMID: 17296338]
  • Hassan Dorani, Kajs-Marie Schützer, Troy C Sarich, Ulrika Wall, Ulrika Logren, Lis Ohlsson, Ulf G Eriksson. Pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor ximelagatran co-administered with different classes of antibiotics in healthy volunteers. European journal of clinical pharmacology. 2007 Jun; 63(6):571-81. doi: 10.1007/s00228-007-0292-6. [PMID: 17387462]
  • M-M Samama, G Gerotziafas. [New antitoagulants]. Annales pharmaceutiques francaises. 2007 Mar; 65(2):85-94. doi: 10.1016/s0003-4509(07)90021-8. [PMID: 17404541]
  • A Schwienhorst. Direct thrombin inhibitors - a survey of recent developments. Cellular and molecular life sciences : CMLS. 2006 Dec; 63(23):2773-91. doi: 10.1007/s00018-006-6219-z. [PMID: 17103113]
  • Martin Koestenberger, Siegfried Gallistl, Leschnik Bettina, Christina Cimenti, Joerg Kutschera, Gerhard Cvirn. Effects of melagatran on activated partial thromboplastin time and on ecarin clotting time in cord versus adult plasma. Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis. 2006 Nov; 17(8):677-80. doi: 10.1097/01.mbc.0000252604.63142.e0. [PMID: 17102656]
  • Ulf G Eriksson, Hassan Dorani, Johan Karlsson, Holger Fritsch, Kurt-Jürgen Hoffmann, Lis Olsson, Troy C Sarich, Ulrika Wall, Kajs-Marie Schützer. Influence of erythromycin on the pharmacokinetics of ximelagatran may involve inhibition of P-glycoprotein-mediated excretion. Drug metabolism and disposition: the biological fate of chemicals. 2006 May; 34(5):775-82. doi: 10.1124/dmd.105.008607. [PMID: 16455803]
  • Rodger A Liddle, Philip P Toskes, Jay Horrow, Jalal Ghali, Abraham Dachman, David Stong. Lack of trophic pancreatic effects in humans with long-term administration of ximelagatran. Pancreas. 2006 Mar; 32(2):205-10. doi: 10.1097/01.mpa.0000202949.64870.87. [PMID: 16552342]
  • Linda C Wernevik, Per Nyström, Gillis Johnsson, Takashi Nakanishi, Ulf G Eriksson. Pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor ximelagatran in young healthy Japanese men. Clinical pharmacokinetics. 2006; 45(1):77-84. doi: 10.2165/00003088-200645010-00005. [PMID: 16430312]
  • Linda C Wernevik, Per Nyström, Magnus Andersson, Gillis Johnsson, Anders Bylock, Takashi Nakanishi, Ulf G Eriksson. Comparable pharmacokinetics and pharmacodynamics of melagatran in Japanese and caucasian volunteers after oral administration of the direct thrombin inhibitor ximelagatran. Clinical pharmacokinetics. 2006; 45(1):85-94. doi: 10.2165/00003088-200645010-00006. [PMID: 16430313]
  • Sofie Bååthe, Bengt Hamrén, Mats O Karlsson, Maria Wollbratt, Margaretha Grind, Ulf G Eriksson. Population pharmacokinetics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in atrial fibrillation patients receiving long-term anticoagulation therapy. Clinical pharmacokinetics. 2006; 45(8):803-19. doi: 10.2165/00003088-200645080-00004. [PMID: 16884319]
  • Shir-Jing Ho, Tim A Brighton. Ximelagatran: direct thrombin inhibitor. Vascular health and risk management. 2006; 2(1):49-58. doi: 10.2147/vhrm.2006.2.1.49. [PMID: 17319469]
  • Grigoris T Gerotziafas, François Depasse, Joël Busson, Lena Leflem, Ismail Elalamy, Meyer M Samama. Towards a standardization of thrombin generation assessment: the influence of tissue factor, platelets and phospholipids concentration on the normal values of Thrombogram-Thrombinoscope assay. Thrombosis journal. 2005 Oct; 3(?):16. doi: 10.1186/1477-9560-3-16. [PMID: 16250908]
  • C Christersson, J Oldgren, A Bylock, L Wallentin, A Siegbahn. Long-term treatment with ximelagatran, an oral direct thrombin inhibitor, persistently reduces the coagulation activity after a myocardial infarction. Journal of thrombosis and haemostasis : JTH. 2005 Oct; 3(10):2245-53. doi: 10.1111/j.1538-7836.2005.01557.x. [PMID: 16194202]
  • Thomas M Hyers. Heparin and other rapidly acting anticoagulants. Seminars in vascular surgery. 2005 Sep; 18(3):130-3. doi: 10.1053/j.semvascsurg.2005.05.002. [PMID: 16168887]
  • S Bertil Olsson, Jonathan L Halperin. Prevention of stroke in patients with atrial fibrillation. Seminars in vascular medicine. 2005 Aug; 5(3):285-92. doi: 10.1055/s-2005-916168. [PMID: 16123916]
  • NULL. Melagatran and ximelagatran: new drug. No real simplification of anticoagulant therapy. Prescrire international. 2005 Aug; 14(78):127-32. doi: NULL. [PMID: 16106594]
  • Michael Wolzt, Troy S Sarich, Ulf G Eriksson. Low potential for interactions between melagatran/ximelagatran and other drugs, food, or alcohol. Seminars in vascular medicine. 2005 Aug; 5(3):254-8. doi: 10.1055/s-2005-916164. [PMID: 16123912]
  • Lars Wallentin. Prevention of cardiovascular events after acute coronary syndrome. Seminars in vascular medicine. 2005 Aug; 5(3):293-300. doi: 10.1055/s-2005-916169. [PMID: 16123917]
  • Menno V Huisman, Henri Bounameaux. Treating patients with venous thromboembolism: initial strategies and long-term secondary prevention. Seminars in vascular medicine. 2005 Aug; 5(3):276-84. doi: 10.1055/s-2005-916167. [PMID: 16123915]
  • Stefan C Carlsson, Sam Schulman. A step change in oral anticoagulation: lack of coagulation monitoring with ximelagatran. Seminars in vascular medicine. 2005 Aug; 5(3):259-65. doi: 10.1055/s-2005-916165. [PMID: 16123913]
  • Michael Wolzt, Troy S Sarich, Ulf G Eriksson. Pharmacokinetics and pharmacodynamics of ximelagatran. Seminars in vascular medicine. 2005 Aug; 5(3):245-53. doi: 10.1055/s-2005-916163. [PMID: 16123911]
  • Stefan Carlsson, Margareta Elg. The effects of ximelagatran and warfarin on the prophylaxis of a caval vein thrombosis and bleeding in the anaesthetized rat. Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis. 2005 Jun; 16(4):245-9. doi: 10.1097/01.mbc.0000169216.70184.8d. [PMID: 15870543]
  • M Hellgren, S Johansson, U G Eriksson, K Wåhlander. The oral direct thrombin inhibitor, ximelagatran, an alternative for anticoagulant treatment during the puerperium and lactation. BJOG : an international journal of obstetrics and gynaecology. 2005 May; 112(5):579-83. doi: 10.1111/j.1471-0528.2004.00494.x. [PMID: 15842280]
  • Marie Cullberg, Ulf G Eriksson, Karin Wåhlander, Henry Eriksson, Sam Schulman, Mats O Karlsson. Pharmacokinetics of ximelagatran and relationship to clinical response in acute deep vein thrombosis. Clinical pharmacology and therapeutics. 2005 Apr; 77(4):279-90. doi: 10.1016/j.clpt.2004.11.001. [PMID: 15903126]
  • Susanne Johansson, Lis Ohlsson, Helene Stenhoff, Karin Wåhlander, Marie Cullberg. No effect of encapsulation on the pharmacokinetics of warfarin. Biopharmaceutics & drug disposition. 2005 Apr; 26(3):121-7. doi: 10.1002/bdd.441. [PMID: 15751004]
  • Gregory W Albers, Hans-Christoph Diener, Lars Frison, Margaretha Grind, Mark Nevinson, Stephen Partridge, Jonathan L Halperin, Jay Horrow, S Bertil Olsson, Palle Petersen, Alec Vahanian. Ximelagatran vs warfarin for stroke prevention in patients with nonvalvular atrial fibrillation: a randomized trial. JAMA. 2005 Feb; 293(6):690-8. doi: 10.1001/jama.293.6.690. [PMID: 15701910]
  • Jonathan L Halperin. Ximelagatran: oral direct thrombin inhibition as anticoagulant therapy in atrial fibrillation. Journal of the American College of Cardiology. 2005 Jan; 45(1):1-9. doi: 10.1016/j.jacc.2004.09.049. [PMID: 15629364]
  • Eva Ersdal, Kajs-Marie Schützer, Carina Lönnerstedt, Lis Ohlsson, Ulrika Wall, Ulf G Eriksson. No influence of food on the pharmacokinetics, pharmacodynamics or tolerability of the 24mg and 36mg oral tablet formulations of ximelagatran. Clinical drug investigation. 2005; 25(7):425-33. doi: 10.2165/00044011-200525070-00001. [PMID: 17532684]
  • Giancarlo Agnelli, Francesco Sonaglia, Cecilia Becattini. Direct thrombin inhibitors for the prevention of venous thromboembolism after major orthopaedic surgery. Current pharmaceutical design. 2005; 11(30):3885-91. doi: 10.2174/138161205774580615. [PMID: 16305519]
  • Martin Koestenberger, Siegfried Gallistl, Gerhard Cvirn, Katrin Baier, Bettina Leschnik, Wolfgang Muntean. Anticoagulant action of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, in umbilical cord and adult plasma: an in vitro examination. Thrombosis research. 2005; 115(1-2):135-42. doi: 10.1016/j.thromres.2004.07.003. [PMID: 15567465]
  • Palle Petersen. Ximelagatran--a promising new drug in thromboembolic disorders. Current pharmaceutical design. 2005; 11(4):527-38. doi: 10.2174/1381612053382016. [PMID: 15725069]
  • Anne Grand'Maison, Andre F Charest, William H Geerts. Anticoagulant use in patients with chronic renal impairment. American journal of cardiovascular drugs : drugs, devices, and other interventions. 2005; 5(5):291-305. doi: 10.2165/00129784-200505050-00002. [PMID: 16156685]
  • Mike Ufer. Comparative pharmacokinetics of vitamin K antagonists: warfarin, phenprocoumon and acenocoumarol. Clinical pharmacokinetics. 2005; 44(12):1227-46. doi: 10.2165/00003088-200544120-00003. [PMID: 16372822]
  • Timothy A Brighton. The direct thrombin inhibitor melagatran/ximelagatran. The Medical journal of Australia. 2004 Oct; 181(8):432-7. doi: 10.5694/j.1326-5377.2004.tb06367.x. [PMID: 15487959]
  • Giuseppe Leone, Elena Rossi, Antonio Maria Leone, Valerio De Stefano. Novel antithrombotic agents: indirect synthetic inhibitors of factor Xa and direct thrombin inhibitors. Evidences from clinical studies. Current medicinal chemistry. Cardiovascular and hematological agents. 2004 Oct; 2(4):311-26. doi: 10.2174/1568016043356183. [PMID: 15320782]
  • Mark A Crowther. Acute reversal of anticoagulant-induced bleeding complications. Clinical advances in hematology & oncology : H&O. 2004 Sep; 2(9):578-82. doi: NULL. [PMID: 16163240]
  • Palle Petersen. New approaches to anticoagulation in atrial fibrillation. Current cardiology reports. 2004 Sep; 6(5):354-64. doi: 10.1007/s11886-004-0038-3. [PMID: 15306092]
  • Troy C Sarich, Kajs-Marie Schützer, Hassan Dorani, Ulrika Wall, Inge Kalies, Lis Ohlsson, Ulf G Eriksson. No pharmacokinetic or pharmacodynamic interaction between atorvastatin and the oral direct thrombin inhibitor ximelagatran. Journal of clinical pharmacology. 2004 Aug; 44(8):928-34. doi: 10.1177/0091270004268047. [PMID: 15286097]
  • Troy C Sarich, Kajs-Marie Schützer, Maria Wollbratt, Ulrika Wall, Eva Kessler, Ulf G Eriksson. No pharmacokinetic or pharmacodynamic interaction between digoxin and the oral direct thrombin inhibitor ximelagatran in healthy volunteers. Journal of clinical pharmacology. 2004 Aug; 44(8):935-41. doi: 10.1177/0091270004268048. [PMID: 15286098]
  • Michael Wolzt, Marcel Levi, Troy C Sarich, Stig L Boström, Ulf G Eriksson, Maria Eriksson-Lepkowska, Mia Svensson, Jeffrey I Weitz, Margareta Elg, Karin Wåhlander. Effect of recombinant factor VIIa on melagatran-induced inhibition of thrombin generation and platelet activation in healthy volunteers. Thrombosis and haemostasis. 2004 Jun; 91(6):1090-6. doi: 10.1160/th03-09-0605. [PMID: 15175794]
  • Bernhard R Winkelmann. American Heart Association scientific sessions. Expert opinion on investigational drugs. 2004 Apr; 13(4):435-45. doi: 10.1517/13543784.13.4.435. [PMID: 15102593]
  • Charles W Francis. Ximelagatran: a new oral anticoagulant. Best practice & research. Clinical haematology. 2004 Mar; 17(1):139-52. doi: 10.1016/j.beha.2004.03.005. [PMID: 15171963]
  • Kajs-Marie Schützer, Ulrika Wall, Carina Lönnerstedt, Lis Ohlsson, Renli Teng, Troy C Sarich, Ulf G Eriksson. Bioequivalence of ximelagatran, an oral direct thrombin inhibitor, as whole or crushed tablets or dissolved formulation. Current medical research and opinion. 2004 Mar; 20(3):325-31. doi: 10.1185/030079903125003035. [PMID: 15025841]
  • Stig L Boström, Göran F H Hansson, Troy C Sarich, Michael Wolzt. The inhibitory effect of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, compared with enoxaparin and r-hirudin on ex vivo thrombin generation in human plasma. Thrombosis research. 2004; 113(1):85-91. doi: 10.1016/j.thromres.2004.02.009. [PMID: 15081569]
  • David Bergqvist, Jan-Helge Solhaug, Lena Holmdahl, Ulf G Eriksson, Magnus Andersson, Barbro Boberg, Mats Ogren. Pharmacokinetics, preliminary efficacy and safety of subcutaneous melagatran and oral ximelagatran : a multicentre study of thromboprophylaxis in elective abdominal surgery. Clinical drug investigation. 2004; 24(3):127-36. doi: 10.2165/00044011-200424030-00001. [PMID: 17516699]
  • G Pindur, S Ziegeler, S Kleinschmidt. [Melagatran and ximelagatran. Pharmacologic characteristics and anesthesiological aspects]. Der Anaesthesist. 2003 Dec; 52(12):1171-5. doi: 10.1007/s00101-003-0602-z. [PMID: 14691631]
  • S Bertil Olsson. Stroke prevention with the oral direct thrombin inhibitor ximelagatran compared with warfarin in patients with non-valvular atrial fibrillation (SPORTIF III): randomised controlled trial. Lancet (London, England). 2003 Nov; 362(9397):1691-8. doi: 10.1016/s0140-6736(03)14841-6. [PMID: 14643116]
  • D Gustafsson. Oral direct thrombin inhibitors in clinical development. Journal of internal medicine. 2003 Oct; 254(4):322-34. doi: 10.1046/j.1365-2796.2003.01225.x. [PMID: 12974871]
  • Michael Wolzt, Maria Wollbratt, Mia Svensson, Karin Wåhlander, Margaretha Grind, Ulf G Eriksson. Consistent pharmacokinetics of the oral direct thrombin inhibitor ximelagatran in patients with nonvalvular atrial fibrillation and in healthy subjects. European journal of clinical pharmacology. 2003 Oct; 59(7):537-43. doi: 10.1007/s00228-003-0667-2. [PMID: 12955372]
  • P Prandoni, P Simioni, A Pagnan. [Therapeutic indications for acute venous thromboembolism. Current status and future perspectives]. Minerva cardioangiologica. 2003 Aug; 51(4):361-71. doi: NULL. [PMID: 12900718]
  • Gunnar Fager, Marie Cullberg, Maria Eriksson-Lepkowska, Lars Frison, Ulf G Eriksson. Pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, are not influenced by acetylsalicylic acid. European journal of clinical pharmacology. 2003 Aug; 59(4):283-9. doi: 10.1007/s00228-003-0619-x. [PMID: 12845508]
  • Jack Hirsh. Current anticoagulant therapy--unmet clinical needs. Thrombosis research. 2003 Jul; 109 Suppl 1(?):S1-8. doi: 10.1016/s0049-3848(03)00250-0. [PMID: 12818628]
  • Stig L Boström, Göran F Hansson, Magnus Kjaer, Troy C Sarich. Effects of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran, and dalteparin on the endogenous thrombin potential in venous blood from healthy male subjects. Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis. 2003 Jul; 14(5):457-62. doi: 10.1097/00001721-200307000-00005. [PMID: 12851531]
  • Bernd Clement, Katrin Lopian. Characterization of in vitro biotransformation of new, orally active, direct thrombin inhibitor ximelagatran, an amidoxime and ester prodrug. Drug metabolism and disposition: the biological fate of chemicals. 2003 May; 31(5):645-51. doi: 10.1124/dmd.31.5.645. [PMID: 12695354]
  • Ulf G Eriksson, Ulf Bredberg, Kristina Gislén, Linda C Johansson, Lars Frison, Martin Ahnoff, David Gustafsson. Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young healthy male subjects. European journal of clinical pharmacology. 2003 May; 59(1):35-43. doi: 10.1007/s00228-003-0565-7. [PMID: 12743672]
  • Ulf G Eriksson, Ulf Bredberg, Kurt-Jürgen Hoffmann, Anneli Thuresson, Margareth Gabrielsson, Hans Ericsson, Martin Ahnoff, Kristina Gislén, Gunnar Fager, David Gustafsson. Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs, and humans. Drug metabolism and disposition: the biological fate of chemicals. 2003 Mar; 31(3):294-305. doi: 10.1124/dmd.31.3.294. [PMID: 12584156]
  • Marita Larsson, Martin Ahnoff, Anna Abrahamsson, Ulrika Logren, Christina Fakt, Irene Ohrman, Bengt Arne Persson. Determination of ximelagatran, an oral direct thrombin inhibitor, its active metabolite melagatran, and the intermediate metabolites, in biological samples by liquid chromatography-mass spectrometry. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2003 Jan; 783(2):335-47. doi: 10.1016/s1570-0232(02)00768-7. [PMID: 12482476]
  • Linda C Johansson, Magnus Andersson, Gunnar Fager, David Gustafsson, Ulf G Eriksson. No influence of ethnic origin on the pharmacokinetics and pharmacodynamics of melagatran following oral administration of ximelagatran, a novel oral direct thrombin inhibitor, to healthy male volunteers. Clinical pharmacokinetics. 2003; 42(5):475-84. doi: 10.2165/00003088-200342050-00005. [PMID: 12739985]
  • Eva Bredberg, Tommy B Andersson, Lars Frison, Annelie Thuresson, Susanne Johansson, Maria Eriksson-Lepkowska, Marita Larsson, Ulf G Eriksson. Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions. Clinical pharmacokinetics. 2003; 42(8):765-77. doi: 10.2165/00003088-200342080-00005. [PMID: 12846597]
  • Linda C Johansson, Lars Frison, Ulrika Logren, Gunnar Fager, David Gustafsson, Ulf G Eriksson. Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. Clinical pharmacokinetics. 2003; 42(4):381-92. doi: 10.2165/00003088-200342040-00006. [PMID: 12648028]
  • Troy C Sarich, Renli Teng, Gary R Peters, Maria Wollbratt, Robert Homolka, Mia Svensson, Ulf G Eriksson. No influence of obesity on the pharmacokinetics and pharmacodynamics of melagatran, the active form of the oral direct thrombin inhibitor ximelagatran. Clinical pharmacokinetics. 2003; 42(5):485-92. doi: 10.2165/00003088-200342050-00006. [PMID: 12739986]
  • Ulf G Eriksson, Jaap W Mandema, Mats O Karlsson, Lars Frison, Per Olsson Gisleskog, Ulrika Wählby, Bengt Hamrén, David Gustafsson, Bengt I Eriksson. Pharmacokinetics of melagatran and the effect on ex vivo coagulation time in orthopaedic surgery patients receiving subcutaneous melagatran and oral ximelagatran: a population model analysis. Clinical pharmacokinetics. 2003; 42(7):687-701. doi: 10.2165/00003088-200342070-00006. [PMID: 12844328]
  • Ulf G Eriksson, Susanne Johansson, Per-Ola Attman, Henrik Mulec, Lars Frison, Gunnar Fager, Ola Samuelsson. Influence of severe renal impairment on the pharmacokinetics and pharmacodynamics of oral ximelagatran and subcutaneous melagatran. Clinical pharmacokinetics. 2003; 42(8):743-53. doi: 10.2165/00003088-200342080-00003. [PMID: 12846595]
  • Karin Wåhlander, Maria Eriksson-Lepkowska, Lars Frison, Gunnar Fager, Ulf G Eriksson. No influence of mild-to-moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor. Clinical pharmacokinetics. 2003; 42(8):755-64. doi: 10.2165/00003088-200342080-00004. [PMID: 12846596]
  • Meyer Michel Samama, Grigoris T Gerotziafas, Ismail Elalamy, Marie Hélène Horellou, Jacqueline Conard. Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiology of haemostasis and thrombosis. 2002 Sep; 32(5-6):218-24. doi: 10.1159/000073570. [PMID: 13679646]
  • Karin Wåhlander, Leif Lapidus, Carl-Gustav Olsson, Anneli Thuresson, Ulf G Eriksson, Göran Larson, Henry Eriksson. Pharmacokinetics, pharmacodynamics and clinical effects of the oral direct thrombin inhibitor ximelagatran in acute treatment of patients with pulmonary embolism and deep vein thrombosis. Thrombosis research. 2002 Aug; 107(3-4):93-9. doi: 10.1016/s0049-3848(02)00259-1. [PMID: 12431473]
  • Bengt I Eriksson, Ann-Christin Arfwidsson, Lars Frison, Ulf G Eriksson, Anders Bylock, Peter Kälebo, Gunnar Fager, David Gustafsson. A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. MElagatran for THRombin inhibition in Orthopaedic surgery. Thrombosis and haemostasis. 2002 Feb; 87(2):231-7. doi: NULL. [PMID: 11858482]
  • J Hauptmann. Pharmacokinetics of an emerging new class of anticoagulant/antithrombotic drugs. A review of small-molecule thrombin inhibitors. European journal of clinical pharmacology. 2002 Jan; 57(11):751-8. doi: 10.1007/s00228-001-0392-7. [PMID: 11868795]
  • D Gustafsson, J Nyström, S Carlsson, U Bredberg, U Eriksson, E Gyzander, M Elg, T Antonsson, K Hoffmann, A Ungell, H Sörensen, S Någård, A Abrahamsson, R Bylund. The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. Thrombosis research. 2001 Feb; 101(3):171-81. doi: 10.1016/s0049-3848(00)00399-6. [PMID: 11228340]