ICAAC 2014: Delafloxacin Shows Promise as a Single-dose Treatment for Gonorrhea

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A new antibiotic, delafloxacin, demonstrated potent activity against gonorrhea -- including drug-resistant strains -- in a laboratory study, and its pharmacokinetics suggest that single-dose oral treatment will be feasible, according to research presented at the 54th Interscience Conference on Antimicrobial Agents and Chemotherapy this week in Washington, DC.

Delafloxacin, being developed by Melinta Therapeutics, is a novel fluoroquinolone antibiotic. Development of new therapies for gonorrhea is a priority as multidrug-resistant strains become increasingly common around the world.

Researchers tested the activity of delafloxacin, ciprofloxacin, and ceftriaxone against various Neisseria gonorrhoeae isolates in vitro, including ciprofloxacin-sensitive and -resistant strains. They found that delafloxacin showed good activity against all isolates and killed resistant bacteria more rapidly than the other drugs.

In the Phase 1 pharmacokinetic study, Melinta researchers administered delafloxacin to 20 healthy volunteers without gonorrhea to see how the drug is processed in the body.

They found that delafloxacin has a pharmacokinetic profile that supports a single oral dose for the treatment of people with uncomplicated gonorrhea. The mean time to peak plasma concentration following administration of a single 900 mg dose was approximately 1.4 hours, with a half-life of approximately 18 hours, according to a press release issued by the company. The most common side effects were diarrhea, nausea, and nosebleeds.

"These metrics combined with the rapid oral bioavailability and long half-life following a single oral dose of delafloxacin are supportive of our U.S. Phase 3 gonorrhea clinical program, in which we are comparing a single oral dose of delafloxacin to ceftriaxone," said Melinta executive vice president Eugene Sun, MD.

9/12/14

References

L Lawrence, R Hoover, M Benedict, et al. Pharmacokinetics of a 900 mg Oral Formulation of Delafloxacin in Healthy Subjects Supporting a Gonorrhea Phase 3 Study. 54th Interscience Conference on Antimicrobial Agents and Chemotherapy(ICAAC 2014), September 5-9, in Washington, DC.Abstract A-056a.

OO Soge, MC Roberts, CJ Lenderman, EM Duffy, et al. Evaluation Of In Vitro Activity of Delafloxacin Against Contemporary Neisseria Gonorrhoeae Isolates. 54th Interscience Conference on Antimicrobial Agents and Chemotherapy(ICAAC 2014), September 5-9, in Washington, DC.Abstract C-1401.

JM Remy and E Duffy. Evaluation of the Bactericidal Activity of Delafloxacin against Neisseria gonorrhoeae Isolates by Time-Kill Methodology. 54th Interscience Conference on Antimicrobial Agents and Chemotherapy(ICAAC 2014), September 5-9, in Washington, DC.Abstract F-283.

Other Source

Melinta Therapeutics. Melinta Therapeutics Reports on PK Profile of a Single Oral Dose of Delafloxacin in Support of U.S. Phase 3 Gonorrhea Program. Press release. September 6, 2014.