[Antibacterial property and clinical effect of gatifloxacin, a novel quinolone antibacterial agent].
Gatifloxacin, a novel 8-methoxyquinolone, was approved in April 2002 and launched in June 2002. Gatifloxacin shows a broad spectrum of antibacterial activity against Gram-negative, Gram-positive, anaerobic, and atypical pathogens. The activity is higher than those of other quinolones against RTI pathogens of S. pneumoniae including the penicillin-resistant strains, H. influenzae, Mycoplasma, and Chlamydia. This drug strongly inhibits the type II topoisomerase, DNA gyrase, and topoisomerase IV of S. pneumoniae and S. aureus to nearly the same extent, leading to the potent activity and low resistance. After an oral administration in humans, gatifloxacin is well absorbed and distributed, and the majority is excreted in the urine as the unchanged form. Its serum half-life is 7-8 h. The clinical effectiveness was observed for various infectious diseases including RTI and UTI. The bacterial eradication rate is 94.1% for Gram-positives, 90.7% for Gram-negatives, and 97.7% for anaerobes. In particular, gatifloxacin showed a high eradication rate of 98.7% for S. pneumoniae. The total cure rate and eradication rate of gatifloxacin in clinical studies are 91.1% and 93.3%, respectively, indicating that the potent activity and good PK profile account for its clinical efficacy.
Hosaka
Masaki
M
Discovery Research Planning Department, Kyorin Pharmaceutical Co., Ltd., Tokyo, Japan.
D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects* / Q000201:enzymology; D002986:Clinical Trials as Topic; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors; D024881:Drug Resistance, Bacterial; D024841:Fluoroquinolones; D000077734:Gatifloxacin; D006207:Half-Life; D006801:Humans; D012141:Respiratory Tract Infections / Q000188:drug therapy / Q000382:microbiology; D013607:Tablets; D059005:Topoisomerase II Inhibitors; D016896:Treatment Outcome; D014552:Urinary Tract Infections / Q000188:drug therapy / Q000382:microbiology
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D013607:Tablets; D059005:Topoisomerase II Inhibitors; D027101:DNA Topoisomerase IV; D000077734:Gatifloxacin