David Gustafsson

Summary

Affiliation: AstraZeneca R and D

Publications

  1. doi request reprint A serendipitously identified novel small molecule procoagulant compound giving rise to a high-throughput screening assay based on human plasma
    David Gustafsson
    Department of Bioscience, AstraZeneca, R and D Mölndal, Sweden Electronic address
    Thromb Res 132:248-55. 2013
  2. pmc The pathophysiology of hyperuricaemia and its possible relationship to cardiovascular disease, morbidity and mortality
    David Gustafsson
    Bioscience, CVMD iMED, AstraZeneca R and D Molndal, Molndal, Sweden
    BMC Nephrol 14:164. 2013
  3. ncbi request reprint A new oral anticoagulant: the 50-year challenge
    David Gustafsson
    AstraZeneca R and D Molndal, S 431 83 Molndal, Sweden
    Nat Rev Drug Discov 3:649-59. 2004
  4. ncbi request reprint The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects
    D Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D Molndal, S 431 83, Molndal, Sweden
    Thromb Res 101:171-81. 2001
  5. ncbi request reprint The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review
    David Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, Molndal, S 431 83 Molndal, Sweden
    Thromb Res 109:S9-15. 2003
  6. ncbi request reprint Oral direct thrombin inhibitors in clinical development
    D Gustafsson
    AstraZeneca R and D, Molndal, Sweden
    J Intern Med 254:322-34. 2003
  7. ncbi request reprint Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young healthy male subjects
    Ulf G Eriksson
    AstraZeneca R and D, 431 83 Mölndal, Sweden
    Eur J Clin Pharmacol 59:35-43. 2003
  8. ncbi request reprint Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor
    Linda C Johansson
    AstraZeneca R and D Molndal, Molndal, Sweden
    Clin Pharmacokinet 42:381-92. 2003
  9. ncbi request reprint 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
    Ulf G Eriksson
    AstraZeneca R and D Molndal, Molndal, Sweden
    Clin Pharmacokinet 42:687-701. 2003
  10. ncbi request reprint 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
    Linda C Johansson
    AstraZeneca R and D, Molndal, Sweden
    Clin Pharmacokinet 42:475-84. 2003

Detail Information

Publications26

  1. doi request reprint A serendipitously identified novel small molecule procoagulant compound giving rise to a high-throughput screening assay based on human plasma
    David Gustafsson
    Department of Bioscience, AstraZeneca, R and D Mölndal, Sweden Electronic address
    Thromb Res 132:248-55. 2013
    ..This publication describes some characteristics of AZ10047130 and a systematic search for novel hits using a, human plasma-based, high-throughput screening (HTS) assay...
  2. pmc The pathophysiology of hyperuricaemia and its possible relationship to cardiovascular disease, morbidity and mortality
    David Gustafsson
    Bioscience, CVMD iMED, AstraZeneca R and D Molndal, Molndal, Sweden
    BMC Nephrol 14:164. 2013
    ..This article briefly reviews uric acid metabolism and summarizes the current literature on hyperuricaemia in cardiovascular disease and related co-morbidities, and emerging treatment options. ..
  3. ncbi request reprint A new oral anticoagulant: the 50-year challenge
    David Gustafsson
    AstraZeneca R and D Molndal, S 431 83 Molndal, Sweden
    Nat Rev Drug Discov 3:649-59. 2004
  4. ncbi request reprint The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects
    D Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D Molndal, S 431 83, Molndal, Sweden
    Thromb Res 101:171-81. 2001
    ....
  5. ncbi request reprint The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review
    David Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, Molndal, S 431 83 Molndal, Sweden
    Thromb Res 109:S9-15. 2003
    ..As a consequence of its favourable pharmacokinetic and pharmacodynamic properties, ximelagatran is currently undergoing full-scale clinical development for the prophylaxis and treatment of thromboembolic disorders...
  6. ncbi request reprint Oral direct thrombin inhibitors in clinical development
    D Gustafsson
    AstraZeneca R and D, Molndal, Sweden
    J Intern Med 254:322-34. 2003
    ..It is anticipated that with a favourable outcome of the Phase III clinical studies new oral DTIs, with the oral fixed-dose regimen without routine coagulation monitoring, will ease the use of today's anticoagulant therapy...
  7. ncbi request reprint Pharmacokinetics and pharmacodynamics of ximelagatran, a novel oral direct thrombin inhibitor, in young healthy male subjects
    Ulf G Eriksson
    AstraZeneca R and D, 431 83 Mölndal, Sweden
    Eur J Clin Pharmacol 59:35-43. 2003
    ..The primary objectives were to determine the dose linearity and reproducibility of melagatran exposure and the influence of food intake...
  8. ncbi request reprint Influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran, an oral direct thrombin inhibitor
    Linda C Johansson
    AstraZeneca R and D Molndal, Molndal, Sweden
    Clin Pharmacokinet 42:381-92. 2003
    ..To investigate the influence of age on the pharmacokinetics and pharmacodynamics of ximelagatran...
  9. ncbi request reprint 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
    Ulf G Eriksson
    AstraZeneca R and D Molndal, Molndal, Sweden
    Clin Pharmacokinet 42:687-701. 2003
    ..To support the design of a pivotal dose-finding study, the impact of individualised dosage based on bodyweight and calculated creatinine clearance was examined...
  10. ncbi request reprint 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
    Linda C Johansson
    AstraZeneca R and D, Molndal, Sweden
    Clin Pharmacokinet 42:475-84. 2003
    ..To determine the influence of ethnic origin on the pharmacokinetic and pharmacodynamic properties of melagatran after oral administration of ximelagatran, a novel oral direct thrombin inhibitor...
  11. ncbi request reprint Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs, and humans
    Ulf G Eriksson
    AstraZeneca R and D Molndal, Sweden
    Drug Metab Dispos 31:294-305. 2003
    ..The fraction of ximelagatran absorbed was at least 40 to 70% in all species. First-pass metabolism of ximelagatran with subsequent biliary excretion of the formed metabolites account for the lower bioavailability of melagatran...
  12. ncbi request reprint A combination of a thrombin inhibitor and dexamethasone prevents the development of experimental disseminated intravascular coagulation in rats
    Margareta Elg
    Department of Integrative Pharmacology, AstraZeneca R and D Molndal, Molndal, Sweden
    Thromb Res 117:429-37. 2006
    ....
  13. ncbi request reprint Discovery of ximelagatran in an historical perspective
    David Gustafsson
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, Molndal, Sweden
    Semin Vasc Med 5:227-34. 2005
    ..A comparison of the discovery and early clinical development of the two classes of oral anticoagulants reveals some similarities but also several differences that illustrate the change in drug discovery over the last half century...
  14. ncbi request reprint Antithrombotic effects and bleeding time of thrombin inhibitors and warfarin in the rat
    M Elg
    Department of Cardiovascular Pharmacology, ASTRA Hässle, Molndal, Sweden
    Thromb Res 94:187-97. 1999
    ....
  15. ncbi request reprint Inhibition of thrombin generation by the oral direct thrombin inhibitor ximelagatran in shed blood from healthy male subjects
    Troy C Sarich
    AstraZeneca R and D Molndal, Sweden
    Thromb Haemost 87:300-5. 2002
    ..Using a shed blood model, we demonstrate that the reversible thrombin inhibitor melagatran and, therefore, oral administration of ximelagatran, inhibits thrombin generation in humans after acute activation of coagulation...
  16. ncbi request reprint Effects of ximelagatran, an oral direct thrombin inhibitor, r-hirudin and enoxaparin on thrombin generation and platelet activation in healthy male subjects
    Troy C Sarich
    AstraZeneca LP, DCC2 W1 345, 1800 Concord Pike, Wilmington, DE 19850, USA
    J Am Coll Cardiol 41:557-64. 2003
    ..The effects of ximelagatran, an oral direct thrombin inhibitor (DTI), recombinant hirudin (r-hirudin) and enoxaparin on thrombin generation and platelet activation were studied in humans...
  17. ncbi request reprint Effect of activated prothrombin complex concentrate or recombinant factor VIIa on the bleeding time and thrombus formation during anticoagulation with a direct thrombin inhibitor
    M Elg
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, S 431 83 Molndal, Sweden
    Thromb Res 101:145-57. 2001
    ..NovoSeven (r-F VIIa) at high doses had less pronounced effects on blood loss and bleeding times compared with Feiba...
  18. ncbi request reprint Effects of agents, used to treat bleeding disorders, on bleeding time prolonged by a very high dose of a direct thrombin inhibitor in anesthesized rats and rabbits
    M Elg
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, Molndal, Sweden
    Thromb Res 101:159-70. 2001
    ..Thus, stimulating thrombin generation with the use of APCC may counteract the anticoagulant effect observed with a very high dose of a thrombin inhibitor...
  19. ncbi request reprint The effects of oral and intravenous direct thrombin inhibitors on the size of photochemically induced cortical infarction in rats
    A Mikulski
    Department of Cardiovascular Pharmacology, AstraZeneca R and D, Molndal, Sweden
    Thromb Res 101:477-82. 2001
    ..This study showed that experimental focal ischaemic infarction, elicited by photochemically induced endothelial cell damage, can be significantly reduced with melagatran and inogatran, direct thrombin inhibitors...
  20. ncbi request reprint Factor V Leiden (G1691A) and prothrombin gene G20210A mutations as potential risk factors for venous thromboembolism after total hip or total knee replacement surgery
    K Wahlander
    Department of Clinical Chemistry and Transfusion Medicine, Sahlgrenska University Hospital, Goteborg, Sweden
    Thromb Haemost 87:580-5. 2002
    ..03 and p = 0.05, respectively). However, since 90% of the patients with these genetic risk factors will not suffer a VTE event, a general pre-operative genotyping is, in our opinion, of questionable value...
  21. ncbi request reprint Acute antithrombotic effects of ximelagatran, an oral direct thrombin inhibitor, and r-hirudin in a human ex vivo model of arterial thrombosis
    T C Sarich
    Experimental Medicine, AstraZeneca LP, Wilmington, DE 19850, USA
    J Thromb Haemost 1:999-1004. 2003
    ..The antithrombotic effect of 40-80 mg ximelagatran appeared comparable to that of parenterally administered r-hirudin, which has been previously demonstrated to be clinically effective in acute coronary syndromes...
  22. pmc Characterization of a small molecule inhibitor of plasminogen activator inhibitor type 1 that accelerates the transition into the latent conformation
    Ola Fjellström
    Department of Medicinal Chemistry, AstraZeneca R and D Molndal, S 431 83 Molndal, Sweden
    J Biol Chem 288:873-85. 2013
    ....
  23. doi request reprint Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia
    Peter Bach
    Department of Medicinal Chemistry, AstraZeneca R and D, CVMD iMED, Molndal, Pepparedsleden 1, SE 431 83 Molndal, Sweden Electronic address
    Bioorg Med Chem Lett 24:821-7. 2014
    ..The data indicate that at least a 100-fold selectivity over other serine proteases in the coagulation cascade will be required for an effective APC inhibitor. ..
  24. doi request reprint Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid
    Jonas Boström
    AstraZeneca Mölndal, CVGI iMED, Molndal, Sweden
    J Med Chem 56:3273-80. 2013
    ..Remarkably, 4-PIOL was found to be more than four times as potent as the drug TXA...
  25. ncbi request reprint 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
    Bengt I Eriksson
    Department of Orthopaedic Surgery, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    Thromb Haemost 87:231-7. 2002
    ..Ximelagatran and melagatran were well tolerated. In conclusion, ximelagatran and its active form melagatran appear to be promising agents for the prevention of venous thromboembolism following orthopaedic surgery...
  26. ncbi request reprint Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial
    Bengt I Eriksson
    Department of Orthopaedic Surgery, Sahlgrenska University Hospital Ostra, Goteborg, Sweden
    Lancet 360:1441-7. 2002
    ..We aimed to compare the efficacy and safety with that of dalteparin...