Effects of the Des-F(6)-quinolone garenoxacin (BMS-284756), in comparison to those of ciprofloxacin and ofloxacin, on joint cartilage in immature rats.
We did not observe signs of chondrotoxicity in immature rats treated orally with garenoxacin (BMS-284756) at doses up to five times 600 mg/kg of body weight or with ciprofloxacin, whereas ofloxacin induced typical cartilage lesions. The peak plasma garenoxacin concentration was 25.5 mg/liter after administration of a dose of 600 mg/kg once daily for 5 days. Assuming that this model is predictive of human risk, BMS-284756 and ciprofloxacin should be more suitable for pediatric use than ofloxacin.
Kappel
Eva Maria
EM
Institute of Clinical Pharmacology and Toxicology, Benjamin Franklin Medical Center, Freie Universität Berlin, Germany.
Shakibaei
Mehdi
M
Bello
Akintunde
A
Stahlmann
Ralf
R
D000284:Administration, Oral; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000633:toxicity*; D002357:Cartilage Diseases / Q000139:chemically induced*; D002358:Cartilage, Articular / Q000473:pathology; D002939:Ciprofloxacin / Q000008:administration & dosage / Q000633:toxicity*; D024841:Fluoroquinolones; D007211:Indoles; D007719:Knee Joint / Q000473:pathology*; D015242:Ofloxacin / Q000008:administration & dosage / Q000633:toxicity*; D015363:Quinolones; D051381:Rats; D017208:Rats, Wistar
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D007211:Indoles; D015363:Quinolones; D002939:Ciprofloxacin; D015242:Ofloxacin; C419689:garenoxacin