Clinical Use of Nitroimidazooxazines

PA-824 has oral bioavailability (subdose proportional) and a relatively long halflife (16-20 h in humans) consistent with once a day regimen [155]. Clinical studies showed that even though PA-824 inhibits excretion of creatinine at high dosage, it did not affect the glomerular filtration rate, thereby limiting concerns about neph-rotoxicity [156]. It is non-mutagenic, shows no cross-resistance with current drugs, and can be coadministered with antiretroviral agents. Phase IIa clinical studies on patients with newly diagnosed, uncomplicated, smear-positive, pulmonary tuber-culosis[157] ascertained PA-824 to be safe and well tolerated for 2 weeks with daily dosing varying from 200 to 1,200 mg/day in which time-frame decrease of bacillary burdens in sputum was observed [158].

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