Wong S L, Drajesk J, Chang M S, Witt G, Awni W M
Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Biopharm Drug Dispos. 1998 Apr;19(3):159-62. doi: 10.1002/(sici)1099-081x(199804)19:3<159::aid-bdd80>3.0.co;2-o.
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 tmax value of approximately 4 h. The terminal elimination t1/2 averaged 15 h, and was dose independent. ABT-761 mean values of Cmax 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.
ABT-761是一种新型强效5-脂氧合酶抑制剂，正处于治疗哮喘的研发阶段。在一项双盲、安慰剂对照研究中，对24名健康男性志愿者单次服用ABT-761（10 - 160毫克）后的药代动力学和剂量比例关系进行了研究。该化合物耐受性良好，对生命体征测量、血液学参数、临床化学、尿液分析或心电图均无临床显著影响。ABT-761的血浆浓度-时间曲线表明，药物在吸收适度缓慢后以单指数方式下降，tmax值约为4小时。终末消除t1/2平均为15小时，且与剂量无关。ABT-761的Cmax和AUC平均值与药物剂量呈线性相关。ABT-761在健康志愿者中耐受性良好，在10至160毫克的单剂量范围内药代动力学呈线性。
