Betrixaban: Difference between revisions

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==Overview==
==Overview==
'''Betrixaban''' ([[International Nonproprietary Name|INN]], codenamed '''PRT-054,021''') is an [[anticoagulant]] drug which acts as a [[direct factor Xa inhibitor]].<ref name="pmid19071881">{{cite journal |author=Eriksson BI, Quinlan DJ, Weitz JI |title=Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development |journal=Clinical Pharmacokinetics |volume=48 |issue=1 |pages=1–22 |year=2009 |pmid=19071881 |doi= |url=}}</ref> It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low [[hERG]] affinity.<ref name="pmid19297154">{{cite journal |author=Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY |title=Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor |journal=Bioorganic & Medicinal Chemistry Letters |volume=19 |issue=8 |pages=2179–85 |year=2009 |month=April |pmid=19297154 |doi=10.1016/j.bmcl.2009.02.111 |url=}}</ref> Betrixaban has undergone human [[clinical trials]] for prevention of embolism after knee surgery,<ref name="pmid19132191">{{cite journal |author=Turpie AG, Bauer KA, Davidson BL, Fisher WD, Gent M, Huo MH, Sinha U, Gretler DD |title=A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT) |journal=Thrombosis and Haemostasis |volume=101 |issue=1 |pages=68–76 |year=2009 |month=January |pmid=19132191 |doi= |url=}}</ref> and prevention of [[stroke]] following [[atrial fibrillation]],<ref>{{cite pmid|20520539}}</ref> with promising results.<ref>{{cite pmid|19739042}}</ref>
'''Betrixaban''' ([[International Nonproprietary Name|INN]], codenamed '''PRT-054,021''') is an [[anticoagulant]] drug which acts as a direct [[factor Xa]] inhibitor.<ref name="pmid19071881">{{cite journal |author=Eriksson BI, Quinlan DJ, Weitz JI |title=Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development |journal=Clinical Pharmacokinetics |volume=48 |issue=1 |pages=1–22 |year=2009 |pmid=19071881 |doi= |url=}}</ref> It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low [[hERG]] affinity.<ref name="pmid19297154">{{cite journal |author=Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY |title=Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor |journal=Bioorganic & Medicinal Chemistry Letters |volume=19 |issue=8 |pages=2179–85 |year=2009 |month=April |pmid=19297154 |doi=10.1016/j.bmcl.2009.02.111 |url=}}</ref> Betrixaban has undergone human [[clinical trials]] for prevention of embolism after knee surgery,<ref name="pmid19132191">{{cite journal |author=Turpie AG, Bauer KA, Davidson BL, Fisher WD, Gent M, Huo MH, Sinha U, Gretler DD |title=A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT) |journal=Thrombosis and Haemostasis |volume=101 |issue=1 |pages=68–76 |year=2009 |month=January |pmid=19132191 |doi= |url=}}</ref> and prevention of [[stroke]] following [[atrial fibrillation]],<ref>{{cite pmid|20520539}}</ref> with promising results.<ref>{{cite pmid|19739042}}</ref>


==References==
==References==

Revision as of 00:06, 14 June 2012

Betrixaban
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
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Chemical and physical data
FormulaC23H22ClN5O3
Molar mass451.905 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Overview

Betrixaban (INN, codenamed PRT-054,021) is an anticoagulant drug which acts as a direct factor Xa inhibitor.[1] It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low hERG affinity.[2] Betrixaban has undergone human clinical trials for prevention of embolism after knee surgery,[3] and prevention of stroke following atrial fibrillation,[4] with promising results.[5]

References

  1. ↑ Eriksson BI, Quinlan DJ, Weitz JI (2009). "Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development". Clinical Pharmacokinetics. 48 (1): 1–22. PMID 19071881.
  2. ↑ Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY (2009). "Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor". Bioorganic & Medicinal Chemistry Letters. 19 (8): 2179–85. doi:10.1016/j.bmcl.2009.02.111. PMID 19297154. Unknown parameter |month= ignored (help)
  3. ↑ Turpie AG, Bauer KA, Davidson BL, Fisher WD, Gent M, Huo MH, Sinha U, Gretler DD (2009). "A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT)". Thrombosis and Haemostasis. 101 (1): 68–76. PMID 19132191. Unknown parameter |month= ignored (help)
  4. ↑ PMID 20520539 (PMID 20520539)
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  5. ↑ PMID 19739042 (PMID 19739042)
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