Reid J J
Primary Care Faculty of Medicine, Dunedin School of Medicine, University of Otago, New Zealand.
Curr Opin Investig Drugs. 2001 Jan;2(1):68-71.
Abbott's ABT-761 is a 5-lipoxygenase inhibitor with 8-fold increased potency over Bay-X-1005 and 150-fold over zileuton [171665]. It has a longer duration of action than its closest competitor, ZD-2138 (AstraZeneca), and has entered phase III trials for asthma [224216]. ABT-761 is the follow-up compound for zileuton and, due to its increased potency, requires only once-daily dosing [187700]. ABT-761 has shown excellent oral bioavailability and an extended duration of plasma levels in man, and initial results for a single 200 mg po dose have shown a significant protective effect against exercise- and adenosine-induced bronchoconstriction in asthmatics [215839]. The drug is well tolerated in healthy volunteers and shows linear pharmacokinetics. The pharmacokinetics in children are similar to that of adults.
雅培公司的ABT - 761是一种5 - 脂氧合酶抑制剂，其效力比Bay - X - 1005高8倍，比齐留通高150倍[171665]。与最接近的竞争对手阿斯利康公司的ZD - 2138相比，它的作用持续时间更长，并且已进入哮喘治疗的III期试验[224216]。ABT - 761是齐留通的后续化合物，由于其效力增强，只需每日给药一次[187700]。ABT - 761在人体中显示出优异的口服生物利用度和延长的血浆水平，单次口服200毫克剂量的初步结果表明，它对哮喘患者运动和腺苷诱导的支气管收缩具有显著的保护作用[215839]。该药物在健康志愿者中耐受性良好，并显示出线性药代动力学。儿童的药代动力学与成人相似。
