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Abstract：
BACKGROUND: To assess the safety, tolerability and pharmacokinetics of a single dose of SYHA1402 in healthy Chinese subjects.
METHODS: This was a randomized, double-blind, placebo-controlled, single-ascending dose study in healthy subjects. Subjects received a single dose of SYHA1402 25 mg, 50 mg, 100 mg, 200 mg, 400 mg or 800 mg, or matching placebo. Safety and tolerability were assessed throughout the study. The pharmacokinetic (PK) parameters of SYHA1402 were estimated using non-compartmental analysis.
RESULTS: In all, 54 subjects were enrolled and completed the study. Specifically, there were no deaths, serious adverse events or withdrawals from study due to adverse events. All treatment-emergent adverse events were mild. The most common drug-related adverse event was sinus bradycardia. The time to maximum concentration ranged from 1.13 to 2.25 h, and the terminal elimination half-life range was 1.51-4.70 h. SYHA1402 exhibited nonlinear PK parameters with less than dose-proportional increases in exposure after single oral doses of 25 to 800 mg.
CONCLUSIONS: SYHA1402 administered as a single dose was well tolerated and safe over the dose range of 25-800 mg. More than 50% of the unchanged SYHA1402 was excreted in urine within the dose range of 25-100 mg.
BACKGROUND: NCT03988413 ( https://www.
RESULTS: gov/ ; registration date: 17 June 2019).
METHODS: This was a randomized, double-blind, placebo-controlled, single-ascending dose study in healthy subjects. Subjects received a single dose of SYHA1402 25 mg, 50 mg, 100 mg, 200 mg, 400 mg or 800 mg, or matching placebo. Safety and tolerability were assessed throughout the study. The pharmacokinetic (PK) parameters of SYHA1402 were estimated using non-compartmental analysis.
RESULTS: In all, 54 subjects were enrolled and completed the study. Specifically, there were no deaths, serious adverse events or withdrawals from study due to adverse events. All treatment-emergent adverse events were mild. The most common drug-related adverse event was sinus bradycardia. The time to maximum concentration ranged from 1.13 to 2.25 h, and the terminal elimination half-life range was 1.51-4.70 h. SYHA1402 exhibited nonlinear PK parameters with less than dose-proportional increases in exposure after single oral doses of 25 to 800 mg.
CONCLUSIONS: SYHA1402 administered as a single dose was well tolerated and safe over the dose range of 25-800 mg. More than 50% of the unchanged SYHA1402 was excreted in urine within the dose range of 25-100 mg.
BACKGROUND: NCT03988413 ( https://www.
RESULTS: gov/ ; registration date: 17 June 2019).
摘要：
背景：为了评估安全性，单剂量SYHA1402在健康中国受试者中的耐受性和药代动力学。
方法：这是一个随机的，双盲,安慰剂对照,健康受试者的单次递增剂量研究。受试者接受单剂量的SYHA140225mg，50毫克，100毫克，200毫克，400毫克或800毫克，或匹配的安慰剂。在整个研究中评估安全性和耐受性。使用非房室分析估计SYHA1402的药代动力学(PK)参数。
结果：总而言之，54名受试者被登记并完成研究。具体来说,没有死亡,严重不良事件或因不良事件退出研究。所有因治疗引起的不良事件均为轻度。最常见的药物相关不良事件是窦性心动过缓。达到最大浓度的时间范围为1.13至2.25h，最终消除半衰期范围为1.51-4.70h。SYHA1402在单次口服剂量为25至800mg后表现出非线性PK参数，暴露量的增加小于剂量比例。
结论：SYHA1402单剂量给药在25-800mg的剂量范围内具有良好的耐受性和安全性。在25-100mg的剂量范围内，超过50％的未改变的SYHA1402在尿液中排泄。
背景：NCT03988413(https://www.
结果：gov/；注册日期：2019年6月17日）。
方法：这是一个随机的，双盲,安慰剂对照,健康受试者的单次递增剂量研究。受试者接受单剂量的SYHA140225mg，50毫克，100毫克，200毫克，400毫克或800毫克，或匹配的安慰剂。在整个研究中评估安全性和耐受性。使用非房室分析估计SYHA1402的药代动力学(PK)参数。
结果：总而言之，54名受试者被登记并完成研究。具体来说,没有死亡,严重不良事件或因不良事件退出研究。所有因治疗引起的不良事件均为轻度。最常见的药物相关不良事件是窦性心动过缓。达到最大浓度的时间范围为1.13至2.25h，最终消除半衰期范围为1.51-4.70h。SYHA1402在单次口服剂量为25至800mg后表现出非线性PK参数，暴露量的增加小于剂量比例。
结论：SYHA1402单剂量给药在25-800mg的剂量范围内具有良好的耐受性和安全性。在25-100mg的剂量范围内，超过50％的未改变的SYHA1402在尿液中排泄。
背景：NCT03988413(https://www.
结果：gov/；注册日期：2019年6月17日）。
