Dose-proportional pharmacokinetics of a new 5-lipoxygenase inhibitor, ABT-761, in healthy volunteers

✍ Scribed by Shekman L. Wong; Jeffrey Drajesk; Min S. Chang; Galen Witt; Walid M. Awni

• Publisher: John Wiley and Sons
• Year: 1998
• Tongue: English
• Weight: 127 KB
• Volume: 19
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/(sici)1099-081x(199804)19:3<159::aid-bdd80>3.0.co;2-o

✦ Synopsis

, a new potent 5-lipoxygenase inhibitor, is under development for the treatment of asthma. The pharmacokinetics and dose proportionality of ABT-761 after single doses (10 -160 mg) of ABT-761 in 24 healthy male volunteers were investigated in a double-blind, placebo-controlled study. The compound was well tolerated, with no clinically significant effects on vital sign measurements, hematological parameters, clinical chemistry, urinalysis, or electrocardiogram. The plasma concentration-time profile of ABT-761 indicates that the drug declines in a monoexponential fashion after moderately slow absorption, with a t max value of approximately 4 h. The terminal elimination t 1/2 averaged 15 h, and was dose independent. ABT-761 mean values of C max and AUC were linearly related to drug dose. ABT-761 is well tolerated in healthy volunteers and the pharmacokinetics are linear in the single-dose range between 10 and 160 mg.