|Chemical and physical data|
|Molar mass||845.01 g/mol|
|3D model (Jmol)|
|(what is this?)|
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.
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.
- Reinert RR (June 2004). "Clinical efficacy of ketolides in the treatment of respiratory tract infections". The Journal of Antimicrobial Chemotherapy. 53 (6): 918–27. doi:10.1093/jac/dkh169. PMID 15117934.
- Woolsey LN; Castaneira M; Jones RN. (May 2010). "CEM-101 activity against Gram-positive organisms". Antimicrobial Agents and Chemotherapy. 54 (5): 2182–2187. doi:10.1128/AAC.01662-09. PMC . PMID 20176910.
- Farrell DJ; Sader HS; Castanheira M; Biedenbach DJ; Rhomberg PR; Jones RN. (June 2010). "Antimicrobial characterization of CEM-101 activity against respiratory tract pathogens including multidrug-resistant pneumococcal serogroup 19A isolates". International Journal of Antimicrobial Agents. 35 (6): 537–543. doi:10.1016/j.ijantimicag.2010.01.026. PMID 20211548.
- McGhee P; Clark C; Kosowska-Shick K; Nagai K; Dewasse B; Beachel L; Appelbaum PC. (January 2010). "In Vitro Activity of Solithromycin against Streptococcus pneumoniae and Streptococcus pyogenes with Defined Macrolide Resistance Mechanisms". Antimicrobial Agents and Chemotherapy. 54 (1): 230–238. doi:10.1128/AAC.01123-09. PMC . PMID 19884376.
- Putnam, Shannon D.; Castanheira, Mariana; Moet, Gary J.; Farrell, David J.; Jones, Ronald N. (2010). "CEM-101, a novel fluoroketolide: antimicrobial activity against a diverse collection of Gram-positive and Gram-negative bacteria". Diagnostic Microbiology and Infectious Disease. 66 (4): 393–401. doi:10.1016/j.diagmicrobio.2009.10.013. PMID 20022192.
- Putnam, Shannon D.; Sader, Helio S.; Farrell, David J.; Biedenbach, Douglas J.; Castanheira, Mariana (2011). "Antimicrobial characterisation of solithromycin (CEM-101), a novel fluoroketolide: activity against staphylococci and enterococci". International Journal of Antimicrobial Agents. 37 (1): 39–45. doi:10.1016/j.ijantimicag.2010.08.021. PMID 21075602.
- "Intravenous (IV) Administration of Cempra Pharmaceutical's Solithromycin (CEM-101) Demonstrates Excellent Systemic Tolerability in a Phase 1 Clinical Trial". 7 May 2011.
- "Cempra antibiotic compound as effective, safer than levofloxacin". 15 Sep 2011.
- http://investor.cempra.com/releasedetail.cfm?ReleaseID=889300. 4 Jan 2015
- http://investor.cempra.com/releasedetail.cfm?ReleaseID=920866. 7 July 2015
- Llano-Sotelo B, Dunkle J, Klepacki D, Zhang W, Fernandes P, Cate JH, Mankin AS (2010). "Binding and Action of CEM-101, a New Fluoroketolide Antibiotic That Inhibits Protein Synthesis". Antimicrobial Agents and Chemotherapy. 54 (12): 4961–4970. doi:10.1128/AAC.00860-10. PMC . PMID 20855725.
- Bertrand D, Bertrand S, Neveu E, Fernandes P (2010). "Molecular characterization of off-target activities of telithromycin: a potential role for nicotinic acetylcholine receptors". Antimicrobial Agents and Chemotherapy. 54 (12): 599–5402. doi:10.1128/AAC.00840-10. PMC . PMID 20855733.
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