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Sutezolid (PNU-100480)

on Tue, 07/17/2012 - 19:25

Last updated July 2012

ACTIVE TB DISEASE 

Sutezolid, or PNU-100480, is a new oxazolidinone—the same class of drugs as linezolid. Sutezolid appears to have more potent antituberculosis activity in vitro, in ex vivo whole blood cultures, and in a murine (mouse) model. A whole-blood study also predicted that sutezolid and two drugs described above—SQ109 and bedaquiline—would be additive, and deserve testing as part of a novel regimen. Pfizer recently completed a phase IIa, open-label, early bactericidal activity and whole-blood activity study. This study of adults with pulmonary DS-TB compared two experimental arms—one with sutezolid twice daily at 600 mg, the other with sutezolid once daily at 1,200 mg—with Rifafour. Results should be available soon.


References:

  • Wallis RS, Jakubiec WM, Kumar V, et al. Pharmacokinetics and whole-blood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers. J Infect. Dis. 2010 Sep 1;202(5):745–51.
  • Williams KN, Brickner SJ, Stover CK, et al. Addition of PNU-100480 to first-line drugs shortens the time needed to cure murine tuberculosis. Am J Respir Crit Care Med. 2009 Aug 15;180(4):371–6.
  • Williams KN, Stover CK, Zhu T, et al. Promising antituberculosis activity of the oxazolidinone PNU-100480 relative to that of linezolid in a murine model. Antimicrob Agents Chemother. 2009 Apr;53(4):1314–9.