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Dose‐proportional pharmacokinetics of a new 5‐lipoxygenase inhibitor, ABT‐761, in healthy volunteers
Author(s) -
Wong Shekman L.,
Drajesk Jeffrey,
Chang Min S.,
Witt Galen,
Awni Walid M.
Publication year - 1998
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199804)19:3<159::aid-bdd80>3.0.co;2-o
Subject(s) - pharmacokinetics , pharmacology , cmax , placebo , medicine , chemistry , alternative medicine , pathology
ABT‐761, 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. © 1998 John Wiley & Sons, Ltd.