Otamixaban

Otamixaban (FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. IC50 value: Target: Factor Xa Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. This review article chronicles the discovery and pre-clinical data surrounding the fXa inhibitor Otamixaban as well as the recent clinical findings in humans.

Product Specifications

CAS Number

[193153-04-7]

Product Name Alternative

FXV673

UNSPSC

12352005

Target

Factor Xa

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Otamixaban.html

Purity

98.25

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

N=C(C1=CC=CC(C[C@@H](C(OC)=O)[C@H](NC(C2=CC=C(C=C2)C3=CC=[N+]([O-])C=C3)=O)C)=C1)N

Molecular Formula

C25H26N4O4

Molecular Weight

446.50

References & Citations

[1]Eikelboom JW, Weitz JI.Otamixaban in acute coronary syndromes.Lancet. 2009 Sep 5;374 (9692) :762-4. Epub 2009 Aug 28.|[2]Sabatine MS, Antman EM, et al. Otamixaban for the treatment of patients with non-ST-elevation acute coronary syndromes (SEPIA-ACS1 TIMI 42) : a randomised, double-blind, active-controlled, phase 2 trial.Lancet. 2009 Sep 5;374 (9692) :787-95. Epub 2009 Aug 28.|[3]Guertin KR, Choi YM.The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development.Curr Med Chem. 2007;14 (23) :2471-81.|[4]Cohen M, Bhatt DL, et al. SEPIA-PCI Trial Investigators.Randomized, double-blind, dose-ranging study of otamixaban, a novel, parenteral, short-acting direct factor Xa inhibitor, in percutaneous coronary intervention: the SEPIA-PCI trial.Circulation. 2007 May 22;115 (20) :2642-51. Epub 2007 May 14.|[5]Guertin, Kevin R.; Choi, Yong-Mi.The discovery of the factor Xa inhibitor Otamixaban: from lead identification to clinical development.Current Medicinal Chemistry (2007), 14 (23), 2471-2481.