METHODS: This was a Phase 1, single-center, open-label, parallel-group, randomized study in healthy Chinese adults who were randomized to receive a single dose of iGlarLixi with either 1:1 (10 U/10 μg) or 2:1 (30 U/15 μg) ratio of iGlar and lixisenatide. Primary objectives include assessment of pharmacokinetics of iGlar in iGlarLixi 30 U/15 μg group and the pharmacokinetics of lixisenatide in both the groups (iGlarLixi 10 U/10 μg and iGlarLixi 30 U/15 μg). Safety and tolerability were also assessed.
RESULTS: In iGlarLixi 30 U/15 μg group, iGlar concentrations were low and quantifiable in three of ten participants, while its main metabolite (M1) was quantifiable in all participants, reflecting rapid conversion of iGlar to M1. Median INS-tmax was 14.00 h for iGlar and 13.00 h post-dose for M1. Absorption of lixisenatide was similar in both dose groups with median tmax of 3.25 and 2.00 h post-dose in both groups. The exposure increase was dose proportionate with a 1.5-fold increase in the lixisenatide dose. Adverse events observed were consistent with those previously reported with iGlar or lixisenatide.
CONCLUSIONS: iGlarLixi administration resulted in early absorption of both iGlar and lixisenatide with a good tolerability profile in healthy Chinese participants. These results are consistent with the previously published data from other geographic regions.
BACKGROUND: U1111-1194-9411.
方法:这是第一阶段,单中心,开放标签,平行组,在健康的中国成年人中进行随机研究,这些成年人被随机分配接受1:1(10U/10μg)或2:1(30U/15μg)比例的iGlar和利西拉来单剂量iGlarLixi。主要目标包括评估iGlarLixi30U/15μg组中iGlar的药代动力学和两组中利西拉来的药代动力学(iGlarLixi10U/10μg和iGlarLixi30U/15μg)。还评估了安全性和耐受性。
结果:在iGlarLixi30U/15μg组中,十个参与者中有三个人的iGlar浓度较低且可量化,虽然它的主要代谢物(M1)在所有参与者中都是可量化的,反映iGlar到M1的快速转换。iGlar的INS-tmax中位数为14.00h,M1的给药后为13.00h。利西拉来的吸收在两个剂量组中相似,在两个组中,中位tmax为3.25和给药后2.00小时。暴露增加与利西拉来剂量增加1.5倍成比例。观察到的不良事件与以前报道的iGlar或利西拉来的不良事件一致。
结论:iGlarLixi给药导致iGlar和利西拉来在健康中国参与者中早期吸收,具有良好的耐受性。这些结果与以前发布的其他地理区域的数据一致。
背景:U1111-1194-9411。