10077. Ximelagatran

Description and references

Orally active direct thrombin inhibitor; prodrug of melagatran, q.v. Prepn: T. Antonsson et al., WO 9723499; D. Gustafsson et al., US 5965692 (1997, 1999 both to Astra). CE determn in drug formulations: P. K. Owens et al., J. Pharm. Biomed. Anal. 27, 587 (2002). LC-MS determn in biological samples: M. Larsson et al., J. Chromatogr. B 783, 335 (2003). Clinical pharmacokinetics: K. Wahlander et al., Thromb. Res. 107, 93 (2002); in deep vein thrombosis: M. Cullberg et al., Clin. Pharmacol. Ther. 77, 279 (2005). Clinical study vs warfarin as thromboprophylactic: C. W. Francis et al., Ann. Intern. Med. 137, 648 (2002). Review of clinical experience in acute coronary syndromes: J. S. Kalus, M. F. Caron, Expert Opin. Invest. Drugs 13, 465-477 (2004); of clinical development: C. J. Boos et al., Eur. J. Int. Med. 16, 267-278 (2005).