Delafloxacin

Delafloxacin
Clinical data
ATC code none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number 189279-58-1
PubChem (CID) 487101
ChemSpider 427049
UNII 6315412YVF YesY
KEGG D09330
ChEMBL CHEMBL2105637
Chemical and physical data
Formula C18H12ClF3N4O4
Molar mass 440.76 g/mol
3D model (Jmol) Interactive image

Delafloxacin (developmental code name RX-3341) is a fluoroquinolone antibiotic being developed by Rib-X Pharmaceuticals, Inc.

It is more active (lower MIC90) than other quinolones against Gram-positive bacteria such as MRSA. In contrast to most approved fluoroquinolones, which are zwitterionic, delafloxacin has an anionic character, which results in a 10-fold increase in delafloxacin accumulation in both bacteria and cells at acidic pH. This property is believed to confer to delafloxacin an advantage for the eradication of Staphylococcus aureus in acidic environments, including intracellular infections.[1]

Clinical trials

Phase II clinical trials have been completed,[2][3][4] including a trial with tigecycline as a comparator[5] The company states delafloxacin met its primary and secondary efficacy endpoints based on the draft guidance from the FDA.

A Phase III trial for acute bacterial skin and skin structure infections (ABSSSI) is due to begin in the 2nd half of 2012.[6]

References

  1. ↑ Lemaire, S. et al. Contrasting Effects of Acidic pH on the Extracellular and Intracellular Activities of the Anti-Gram-Positive Fluoroquinolones Moxifloxacin and Delafloxacin against Staphylococcus aureus Antimicrob. Agents Chemother. February 2011; 55:649-658 doi:10.1128/AAC.01201-10
  2. ↑ http://www.bio-medicine.org/biology-technology-1/Rib-X-Pharmaceuticals-Announces-Positive-Phase-2-Study-Results-for-Delafloxacin-and-a--2425-Million-Financing-10093-1/
  3. ↑ http://clinicaltrials.gov/ct2/show/NCT00719810
  4. ↑ http://www.medicalnewstoday.com/articles/132200.php "Rib-X Pharmaceuticals Reports Positive Top-Line Results From Phase 2 Study Of Delafloxacin" 9 Dec 2008
  5. ↑ http://www.citybizlist.com/lstg/lstgDetail.aspx?id=45749 "ABS Ventures Joins $25M Series D Rib-X Pharmaceuticals Inc." 5 Feb 2009
  6. ↑ Delafloxacin - Pipeline - Rib-X Pharmaceuticals. Accessed: 6/27/2012.


This article is issued from Wikipedia - version of the 6/2/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.