A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits

作者: Pancras C. Wong , Earl J. Crain , Carol A. Watson , William A. Schumacher

DOI: 10.1007/S11239-011-0599-0

关键词:

摘要: … (aPTT) with EC 2x (concentration required to double aPTT) of … BMS-262084 increased ex vivo aPTT dose-dependently … with its ex vivo aPTT, supporting the use of ex vivo aPTT as a …

参考文章(47)
Armando D'Angelo, Maria Paola Seveso, Silvana Vigano' D'Angelo, Felicetta Gilardoni, Anton G. Dettori, Pierangelo Bonini, Effect of clot-detection methods and reagents on activated partial thromboplastin time (APTT). Implications in heparin monitoring by APTT. American Journal of Clinical Pathology. ,vol. 94, pp. 297- 306 ,(1990) , 10.1093/AJCP/94.3.297
Earl J Crain, Alan R Rendina, William A Schumacher, Martin L Ogletree, Pancras C Wong, Carol A Watson, Abstract 631: Nonpeptide Factor XIa (FXIa) Inhibitor. In vitro Kinetic Evaluation and in vivo Studies of BMS-262084 on Arterial Thrombosis and Hemostasis in Rabbits Circulation. ,vol. 114, ,(2006)
X. WANG, Q. CHENG, L. XU, G. Z. FEUERSTEIN, M-Y. HSU, P. L. SMITH, D. A. SEIFFERT, W. A. SCHUMACHER, M. L. OGLETREE, D. GAILANI, Effects of factor IX or factor XI deficiency on ferric chloride‐induced carotid artery occlusion in mice Journal of Thrombosis and Haemostasis. ,vol. 3, pp. 695- 702 ,(2005) , 10.1111/J.1538-7836.2005.01236.X
P. C. WONG, E. J. CRAIN, B. XIN, R. R. WEXLER, P. Y. S. LAM, D. J. PINTO, J. M. LUETTGEN, R. M. KNABB, Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. Journal of Thrombosis and Haemostasis. ,vol. 6, pp. 820- 829 ,(2008) , 10.1111/J.1538-7836.2008.02939.X
Hongfeng Deng, Thomas D. Bannister, Lei Jin, Robert E. Babine, Jesse Quinn, Pamela Nagafuji, Cassandra A. Celatka, Jian Lin, Tsvetelina I. Lazarova, Michael J. Rynkiewicz, Frank Bibbins, Pramod Pandey, Joan Gorga, Harold V. Meyers, Sherin S. Abdel-Meguid, James E. Strickler, Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine. Bioorganic & Medicinal Chemistry Letters. ,vol. 16, pp. 3049- 3054 ,(2006) , 10.1016/J.BMCL.2006.02.052
Gregory Lip, Karlheinz Peter, Ingo Ahrens, New oral anticoagulant drugs in cardiovascular disease Thrombosis and Haemostasis. ,vol. 104, pp. 49- 60 ,(2010) , 10.1160/TH09-05-0327
William A. Schumacher, Steven E. Seiler, Thomas E Steinbacher, Anne B. Stewart, Jeffrey S. Bostwick, Karen S. Hartl, Eddie C. Liu, Martin L. Ogletree, Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats European Journal of Pharmacology. ,vol. 570, pp. 167- 174 ,(2007) , 10.1016/J.EJPHAR.2007.05.043
Tsvetelina I. Lazarova, Lei Jin, Michael Rynkiewicz, Joan C. Gorga, Frank Bibbins, Harold V. Meyers, Robert Babine, James Strickler, Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa. Bioorganic & Medicinal Chemistry Letters. ,vol. 16, pp. 5022- 5027 ,(2006) , 10.1016/J.BMCL.2006.07.043