Supriya Ghosh (Editor)

Solithromycin

Updated on
Edit
Like
Comment
Share on FacebookTweet on TwitterShare on LinkedInShare on Reddit
Trade names
  
Solithera

ATC code
  
J01FA16 (WHO)

CAS Number
  
760981-83-7

Routes of administration
  
Oral, intravenous

Synonyms
  
CEM-101; OP-1068

Molar mass
  
845.01 g/mol

Solithromycin httpsuploadwikimediaorgwikipediacommonsthu

Legal status
  
Under FDA and EMA review for approval

How to pronounce solithromycin


Solithromycin (trade name Solithera) is a ketolide antibiotic undergoing clinical development for the treatment of community-acquired pneumonia (CAP) and other infections.

Contents

Solithromycin exhibits excellent in vitro activity against a broad spectrum of Gram-positive respiratory tract pathogens, including macrolide-resistant strains. Solithromycin has activity against most common respiratory Gram-(+) and fastidious Gram-(-) pathogens, and is being evaluated for its utility in treating gonorrhea.

  • May 2011: Solithromycin is in a Phase 2 clinical trial for serious community-acquired bacterial pneumonia (CABP) and in a Phase 1 clinical trial with an intravenous formulation.
  • September 2011 : Solithromycin demonstrated comparable efficacy to levofloxacin with reduced adverse events in Phase 2 trial in people with community-acquired pneumonia
  • January 2015: In a Phase 3 clinical trial for community-acquired bacterial pneumonia (CABP), Solithromycin administered orally demonstrated statistical non-inferiority to the fluoroquinolone, Moxifloxacin.
  • July 2015: Patient enrollment for the second Phase 3 clinical trial (Solitaire IV) for community-acquired bacterial pneumonia (CABP) was completed with results expected in Q4 2015.
  • Oct 2015: IV to oral solithromycin demonstrated statistical non-inferiority to IV to oral moxifloxacin in adults with CABP.
  • July 2016: Cempra Announces FDA Acceptance of IV and oral formulations of Solithera (solithromycin) New Drug Applications for in the Treatment of Community-Acquired Bacterial Pneumonia.

    • Structure

    X-ray crystallography studies have shown solithromycin, the first fluoroketolide in clinical development, has a third region of interactions with the bacterial ribosome, as compared with two binding sites for other ketolides.

    The only (previously) marketed ketolide, telithromycin, suffers from rare but serious side effects. Recent studies have shown this to be likely due to the presence of the pyridine-imidazole group of the telithromycin side chain acting as an antagonist towards various nicotinic acetylcholine receptors.

    References

    Solithromycin Wikipedia
    (Text) CC BY-SA


    Similar Topics