Iclaprim, a Novel Diaminopyrimidine for the Treatment of Resistant Gram-Positive Infections
Autor: | Carrie A. Sincak, Justin M. Schmidt |
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Rok vydání: | 2009 |
Předmět: |
medicine.drug_class
Antibiotics Microbial Sensitivity Tests Pharmacology Gram-Positive Bacteria chemistry.chemical_compound Drug Resistance Bacterial Dihydrofolate reductase medicine Humans Pharmacology (medical) Gram-Positive Bacterial Infections Antibacterial agent Clinical Trials as Topic biology business.industry Antimicrobial Trimethoprim Anti-Bacterial Agents Clinical trial Tetrahydrofolate Dehydrogenase Pyrimidines Diaminopyrimidine chemistry Iclaprim biology.protein Folic Acid Antagonists business medicine.drug |
Zdroj: | Annals of Pharmacotherapy. 43:1107-1114 |
ISSN: | 1542-6270 1060-0280 |
Popis: | Objective To review the pharmacology, microbiology, in vitro susceptibility, pharmacokinetics, clinical trial data, safety, and tolerability of iclaprim, a novel dihydrofolate reductase (DHFR) inhibitor. Data Sources A MEDLINE search was conducted from 1966 through December 2008. Additional sources included abstracts from meetings of the Interscience Conference on Antimicrobial Agents and Chemotherapy and the Infectious Diseases Society of America from 2001 to 2008 and information available from the manufacturer's Web site. Study Selection And Data Extraction In vitro and clinical studies, in addition to Phase 1, 2, and 3 clinical trials, were included. Data Synthesis Iclaprim, a novel diaminopyrimidine and DHFR antagonist, has a mechanism of action similar to that of trimethoprim. It has in vitro activity mainly against gram-positive organisms, including resistant Staphylococcus aureus. In Phase 2 and 3 clinical trials, oral and intravenous administration of iclaprim was effective and well tolerated for the treatment of complicated skin and skin structure infections (cSSSI). Trials are currently ongoing for the treatment of ventilator-associated and healthcare-associated pneumonia. Conclusions Iclaprim is a promising antimicrobial agent for the treatment of gram-positive organisms, including resistant S. aureus and trimethoprim-, macrolide-, fluoroquinolone-, and glycopeptide-resistant strains. Additionally, in vitro activity similar to that of trimethoprim has been observed against gram-negative and atypical organisms. |
Databáze: | OpenAIRE |
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