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2003 1
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Page 1
Razaxaban, a direct factor Xa inhibitor, in combination with aspirin and/or clopidogrel improves low-dose antithrombotic activity without enhancing bleeding liability in rabbits.
Wong PC, Crain EJ, Watson CA, Wexler RR, Lam PY, Quan ML, Knabb RM. Wong PC, et al. J Thromb Thrombolysis. 2007 Aug;24(1):43-51. doi: 10.1007/s11239-007-0017-9. Epub 2007 Feb 24. J Thromb Thrombolysis. 2007. PMID: 17323133
Razaxaban at concentrations up to 10 muM did not alter in vitro platelet aggregation responses to ADP, gamma-thrombin or collagen. ...In summary, razaxaban was an effective antithrombotic agent in a rabbit model of arterial thrombosis. ...
Razaxaban at concentrations up to 10 muM did not alter in vitro platelet aggregation responses to ADP, gamma-thrombin or collagen. .. …
Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs.
Zhang D, Raghavan N, Chen SY, Zhang H, Quan M, Lecureux L, Patrone LM, Lam PY, Bonacorsi SJ, Knabb RM, Skiles GL, He K. Zhang D, et al. Drug Metab Dispos. 2008 Feb;36(2):303-15. doi: 10.1124/dmd.107.018416. Epub 2007 Nov 5. Drug Metab Dispos. 2008. PMID: 17984286
Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa. ...Among the 12 metabolites identified, formation of an isoxazole-ring opened benzamidine metabolite (M1) represented a major metabolic pathway of razaxaban in rats and dog …
Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa. ...Among the 12 metabolites identified, …
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR. Quan ML, et al. J Med Chem. 2005 Mar 24;48(6):1729-44. doi: 10.1021/jm0497949. J Med Chem. 2005. PMID: 15771420
On the basis of its excellent in vitro potency and selectivity profile, high free fraction in human plasma, good oral bioavailability, and in vivo efficacy in antithrombotic models, the HCl salt of this compound was selected for clinical development as razaxaban (DPC 906, …
On the basis of its excellent in vitro potency and selectivity profile, high free fraction in human plasma, good oral bioavailability, and i …
Inhibition of Factor Xa : a potential target for the development of new anticoagulants.
Alexander JH, Singh KP. Alexander JH, et al. Am J Cardiovasc Drugs. 2005;5(5):279-90. doi: 10.2165/00129784-200505050-00001. Am J Cardiovasc Drugs. 2005. PMID: 16156684 Review.
Idraparinux sodium, a long-acting synthetic pentasaccharide, is currently being investigated as a once-weekly alternative to other long-term anticoagulants. DX-9065a and razaxaban are two of many direct selective Factor Xa inhibitors currently in development. DX-9065a has …
Idraparinux sodium, a long-acting synthetic pentasaccharide, is currently being investigated as a once-weekly alternative to other long-term …
New anticoagulants and their potential impact on the treatment of thromboembolic disease.
Ansell J. Ansell J. Curr Hematol Rep. 2004 Sep;3(5):357-62. Curr Hematol Rep. 2004. PMID: 15341703 Review.
Idraparinux has a prolonged half-life and is dosed once weekly. Razaxaban is a small-molecule, oral, direct FXa inhibitor with demonstrated efficacy in orthopedic surgery for primary prevention of venous thromboembolism. ...
Idraparinux has a prolonged half-life and is dosed once weekly. Razaxaban is a small-molecule, oral, direct FXa inhibitor with demons …
Heterogeneity of synthetic factor Xa inhibitors.
Gerotziafas GT, Samama MM. Gerotziafas GT, et al. Curr Pharm Des. 2005;11(30):3855-76. doi: 10.2174/138161205774580552. Curr Pharm Des. 2005. PMID: 16305517 Review.
DX-9065a is the first direct synthetic inhibitor which has been studied in patients with coronary disease. Razaxaban, BAY59-7939, ZK-807834 and JTV-803 are orally active direct FXa inhibitors, which have been studied in phase II trials. ...
DX-9065a is the first direct synthetic inhibitor which has been studied in patients with coronary disease. Razaxaban, BAY59-7939, ZK- …
Gateways to clinical trials.
Bayes M, Rabasseda X, Prous JR. Bayes M, et al. Methods Find Exp Clin Pharmacol. 2004 May;26(4):295-318. Methods Find Exp Clin Pharmacol. 2004. PMID: 15319808
This issue focuses on the following selection of drugs: 166Ho-DOTMP 5A8; A-179578, abetimus sodium, adefovir dipivoxil, AGI-1067, AIDSVAX gp120 B/B, AK-602, alefacept alemtuzumab, aliskiren fumarate, ALVAC vCP1433, ALVAC vCP1452, anecortave acetate, arzoxifene hydrochloride, ataz …
This issue focuses on the following selection of drugs: 166Ho-DOTMP 5A8; A-179578, abetimus sodium, adefovir dipivoxil, AGI-1067, AIDSVAX gp …
Small molecule coagulation cascade inhibitors in the clinic.
Saiah E, Soares C. Saiah E, et al. Curr Top Med Chem. 2005;5(16):1677-95. doi: 10.2174/156802605775009702. Curr Top Med Chem. 2005. PMID: 16375748 Review.
The most advanced drugs reviewed include DPC-423, DPC-602, razaxaban, GSK's 813893, Portola's Xa inhibitors (formerly Millennium), otamixaban, DU-176b, KFA-1982, BAY-59-7939, DX-9065a, YM-150, LY-517717, Exanta, 3DP's thrombin inhibitors, SSR-182289, LB-30057, LB-30870, BI …
The most advanced drugs reviewed include DPC-423, DPC-602, razaxaban, GSK's 813893, Portola's Xa inhibitors (formerly Millennium), ot …
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
Varnes JG, Wacker DA, Pinto DJ, Orwat MJ, Theroff JP, Wells B, Galemo RA, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR. Varnes JG, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):749-54. doi: 10.1016/j.bmcl.2007.11.040. Epub 2007 Nov 17. Bioorg Med Chem Lett. 2008. PMID: 18054227
Efforts to further optimize the clinical candidate razaxaban have led to a new series of pyrazole-based factor Xa (fXa) inhibitors. ...Optimization by conversion from a P1 aminobenzisoxazole to a P1 p-methoxyphenyl residue, replacing the 3-trifluoromethylpyrazole with a 3- …
Efforts to further optimize the clinical candidate razaxaban have led to a new series of pyrazole-based factor Xa (fXa) inhibitors. . …
Preparing for the new anticoagulants.
Davidson BL. Davidson BL. J Thromb Thrombolysis. 2003 Aug-Oct;16(1-2):49-54. doi: 10.1023/B:THRO.0000014593.16147.bf. J Thromb Thrombolysis. 2003. PMID: 14760212 Review.
These drugs do not act by enhancing antithrombin activity, but rather act directly to inhibit the active site of thrombin (melagatran and its orally absorbed derivative, ximelagatran) or factor Xa (razaxaban [DPC-906]). Several studies have been performed with ximelagatran …
These drugs do not act by enhancing antithrombin activity, but rather act directly to inhibit the active site of thrombin (melagatran and it …
21 results