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The Ribosome
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Delafloxacin (RX-3341)
Delafloxacin is a next generation fluoroquinolone with a broad spectrum
of activity. This compound is significantly more active than other quinolones
against Gram-positive organisms, including potent activity against quinolone
resistant Gram-positive bacteria and methicillin resistant
Staphylococcus aureus
(MRSA), while retaining the broad spectrum advantage expected from the quinolone
class. Delafloxacin has been shown to be at least 16 fold more potent than
levofloxacin, ciprofloxacin, gatifloxacin and moxifloxacin against ciprofloxacin
resistant MRSA (MIC90 of ≤ 0.5 ug/ml for delafloxacin versus > 16 ug/ml for all other quinolones).
Delafloxacin has also been shown to be more potent than existing quinolones against
a range of Gram-positive, anaerobic and Gram-negative organisms. Both oral and
intravenous formulations have been developed for this compound. Clinical development
of delafloxacin includes twelve Phase 1 and three completed Phase 2
clinical trials involving more than 1,300 subjects. These studies have shown delafloxacin
to be both clinically efficacious and safe. The oral formulation of delafloxacin has
been shown to have no evidence of either phototoxicity or QTc prolongation in Phase 1
studies and has demonstrated efficacy in two Phase 2 clinical trials (community acquired
pneumonia (CAP) and bronchitis when compared to levofloxicin). The IV formulation of delafloxacin
has demonstrated efficacy in a recent Phase 2 clinical trial in complicated skin and skin structure
infections (cSSSI) when compared to tigecycline.
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