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The solithromycin journey-It is all in the chemistry

Prabhavathi Fernandes1, Evan Martens1, Daniel Bertrand2

  • 1Cempra Inc., Chapel Hill, NC 27517, USA.

Bioorganic & Medicinal Chemistry
|September 6, 2016
PubMed

Insights

New macrolide antibiotic solithromycin shows promise for respiratory infections. Unlike older drugs, it is well-tolerated and effective, offering a needed alternative due to rising bacterial resistance and safety concerns with other treatments.

Area of Science:

  • Infectious Diseases
  • Pharmacology
  • Microbiology

Background:

  • Macrolide antibiotics (e.g., erythromycin, azithromycin) are common for respiratory infections.
  • Increasing bacterial resistance (48% in US, >80% in Asia) limits their effectiveness.
  • Fluoroquinolones and telithromycin have safety concerns, necessitating new treatment options.

Purpose of the Study:

  • To evaluate the safety and efficacy of solithromycin, a novel fluoroketolide antibiotic.
  • To address the need for alternative antibiotics for community-acquired bacterial pneumonia.
  • To differentiate solithromycin from telithromycin regarding safety and mechanism of action.

Main Methods:

  • Clinical trials (two Phase 3) were conducted to assess solithromycin's performance.
  • Chemical and biological comparisons were made between solithromycin and telithromycin.
  • Safety and tolerability were evaluated in trial participants.

Main Results:

  • Solithromycin demonstrated successful outcomes in Phase 3 trials.
  • The drug is chemically and biologically distinct from telithromycin.
  • Solithromycin did not significantly block nicotinic acetylcholine receptors, unlike telithromycin.
  • Solithromycin was well-tolerated and effective in clinical studies.

Conclusions:

  • Solithromycin represents a new class of macrolide antibiotic (fluoroketolide).
  • It offers a potentially safer and effective alternative for respiratory tract infections.
  • Regulatory review by the FDA is pending for this promising new agent.
Keywords:
Antibiotic-resistanceFluroketolideMacrolidePneumoniaSolithromycin

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