ArticleAntimicrobial agents and chemotherapy2010
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 66 citations in OpenAlex.
- Pharmacokinetics of solithromycin (CEM-101) after single or multiple oral doses and effects of food on single-dose bioavailability in healthy adult subjects.Antimicrobial agents and chemotherapy · 2011Trial
- Molecular and phenotypic characterization ofFrontiers in cellular and infection microbiology · 2024Article
- New Resistance Mutations Linked to Decreased Susceptibility to Solithromycin in Streptococcus pneumoniae Revealed by Chemogenomic Screens.Antimicrobial agents and chemotherapy · 2023Article
- The transcriptome of Balamuthia mandrillaris trophozoites for structure-guided drug design.Scientific reports · 2021Article
- Actinomycete-Derived Polyketides as a Source of Antibiotics and Lead Structures for the Development of New Antimicrobial Drugs.Antibiotics (Basel, Switzerland) · 2019Review
- Staphylococcus aureus with an erm-mediated constitutive macrolide-lincosamide-streptogramin B resistance phenotype has reduced susceptibility to the new ketolide, solithromycin.BMC infectious diseases · 2019Article
- Synthesis and antibacterial activity of novel lincomycin derivatives. III. Optimization of a phenyl thiadiazole moiety.The Journal of antibiotics · 2017Article
- Spotlight on solithromycin in the treatment of community-acquired bacterial pneumonia: design, development, and potential place in therapy.Drug design, development and therapy · 2017Review
- Solithromycin: A Novel Fluoroketolide for the Treatment of Community-Acquired Bacterial Pneumonia.Drugs · 2016Review
- Efficacy of Solithromycin (CEM-101) for Experimental Otitis Media Caused by Nontypeable Haemophilus influenzae and Streptococcus pneumoniae.Antimicrobial agents and chemotherapy · 2016Article
- Article
- Biological and Epidemiological Features of Antibiotic-Resistant Streptococcus pneumoniae in Pre- and Post-Conjugate Vaccine Eras: a United States Perspective.Clinical microbiology reviews · 2016Review
- A New, Potent, and Placenta-Permeable Macrolide Antibiotic, Solithromycin, for the Prevention and Treatment of Bacterial Infections in Pregnancy.Frontiers in immunology · 2016Review
- Safety and Pharmacokinetics of Solithromycin in Subjects with Hepatic Impairment.Antimicrobial agents and chemotherapy · 2015Article
- Antimicrobial activity of solithromycin against serotyped macrolide-resistant Streptococcus pneumoniae isolates collected from U.S. medical centers in 2012.Antimicrobial agents and chemotherapy · 2015Article
- A novel ketolide, RBx 14255, with activity against multidrug-resistant Streptococcus pneumoniae.Antimicrobial agents and chemotherapy · 2014Article
- In vitro activity of the new fluoroketolide solithromycin (CEM-101) against macrolide-resistant and -susceptible Mycoplasma genitalium strains.Antimicrobial agents and chemotherapy · 2014Article
- In vitro activity of solithromycin against erythromycin-resistant Streptococcus agalactiae.Antimicrobial agents and chemotherapy · 2014Article
- Antibiotic activity against naive and induced Streptococcus pneumoniae biofilms in an in vitro pharmacodynamic model.Antimicrobial agents and chemotherapy · 2014Article
- Pipeline of Known Chemical Classes of Antibiotics.Antibiotics (Basel, Switzerland) · 2013Review
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
CEM-101 had MIC ranges of 0.002 to 0.016 microg/ml against macrolide-susceptible pneumococci and 0.004 to 1 microg/ml against macrolide-resistant phenotypes. Only 3 strains with erm(B), with or without mef(A), had CEM-101 MICs of 1 microg/ml, and 218/221 strains had CEM-101 MICs of <or=0.5 microg/ml. CEM-101 MICs were as much as 4-fold lower than telithromycin MICs against all strains. For Streptococcus pyogenes, CEM-101 MICs ranged from 0.008 to 0.03 microg/ml against macrolide-susceptible strains and from 0.015 to 1 microg/ml against macrolide-resistant strains. Against erm(B) strains, erythromycin, azithromycin, and clarithromycin MICs were 32 to >64 microg/ml, while 17/19 strains had telithromycin MICs of 4 to 16 microg/ml; CEM-101 MICs were 0.015 to 1 microg/ml. By comparison, erm(A) and mef(A) strains had CEM-101 MICs of 0.015 to 0.5 microg/ml, clindamycin and telithromycin MICs of <or=1 microg/ml, and erythromycin, azithromycin, and clarithromycin MICs of 0.5 to >64 microg/ml. Pneumococcal multistep resistance studies showed that although CEM-101 yielded clones with higher MICs for all eight strains tested, seven of eight strains had clones with CEM-101 MICs that rose from 0.004 to 0.03 microg/ml (parental strains) to 0.06 to 0.5 microg/ml (resistant clones); for only one erm(B) mef(A) strain with a parental MIC of 1 microg/ml was there a resistant clone with a MIC of 32 microg/ml, with no detectable mutations in the L4, L22, or 23S rRNA sequence. Among two of five S. pyogenes strains tested, CEM-101 MICs rose from 0.03 to 0.25 microg/ml, and only for the one strain with erm(B) did CEM-101 MICs rise from 1 to 8 microg/ml, with no changes occurring in any macrolide resistance determinant. CEM-101 had low MICs as well as low potential for the selection of resistant mutants, independent of bacterial species or resistance phenotypes in pneumococci and S. pyogenes.
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