Baxter Innovations GmbH, Wagramer Straße 17-19, 1221, Vienna, Austria.
Int J Hematol. 2013 Nov;98(5):525-32. doi: 10.1007/s12185-013-1448-z. Epub 2013 Sep 24.
Baxter has developed a new recombinant factor IX (rFIX) drug product (BAX326) for treating patients with hemophilia B, or congenital FIX deficiency. An extensive preclinical program evaluated the pharmacokinetics, efficacy, and safety of BAX326 in different species. The efficacy of BAX326 was tested in three mouse models of primary pharmacodynamics: tail-tip bleeding, carotid occlusion, and thrombelastography. The pharmacokinetics was evaluated after a single intravenous bolus injection in mice, rats, and macaques. Toxicity was assessed in rats and macaques, safety pharmacology in rabbits and macaques, and immunogenicity in mice. BAX326 was shown to be efficacious in all three primary pharmacodynamic studies (P ≤ 0.0076). Hemostatic efficacy was dose related and similar for the three lots tested. Pharmacokinetic results showed that rFIX activity and rFIX antigen concentrations declined in a bi-phasic manner, similar to a previously licensed rFIX product. BAX326 was well tolerated in rabbits and macaques at all dose levels; no thrombogenic events and no adverse clinical, respiratory, or cardiovascular effects occurred. BAX326 was also shown to have a similar immunogenicity profile to the comparator rFIX product in mice. These results demonstrate that BAX326 has a favorable preclinical safety and efficacy profile, predictive of a comparable effect to that of the previously licensed rFIX in humans.
百特公司开发了一种新型重组凝血因子 IX(rFIX)药物(BAX326),用于治疗乙型血友病或先天性 FIX 缺乏症患者。一个广泛的临床前计划评估了 BAX326 在不同物种中的药代动力学、疗效和安全性。BAX326 的疗效在三种原发性药效学的小鼠模型中进行了测试:尾尖出血、颈动脉闭塞和血栓弹性描记术。在小鼠、大鼠和猕猴中进行了单次静脉推注后的药代动力学评估。在大鼠和猕猴中评估了毒性,在兔和猕猴中评估了安全药理学,在小鼠中评估了免疫原性。BAX326 在所有三种原发性药效学研究中均显示出疗效(P ≤ 0.0076)。止血疗效与三种测试批次均呈剂量相关性且相似。药代动力学结果表明,rFIX 活性和 rFIX 抗原浓度呈双相下降,与先前批准的 rFIX 产品相似。BAX326 在兔和猕猴的所有剂量水平下均耐受良好;未发生血栓形成事件,也未出现不良临床、呼吸或心血管效应。BAX326 在小鼠中的免疫原性特征也与对照 rFIX 产品相似。这些结果表明,BAX326 具有良好的临床前安全性和疗效特征,可预测与先前批准的 rFIX 在人类中的疗效相当。