Study on safety,pharmacokinetics,and pharmacodynamics of YZJ-3058 tablets for single oral administration in healthy Chinese subjects
10.12092/j.issn.1009-2501.2025.06.009
- VernacularTitle:单次口服YZJ-3058片在中国健康受试者中的安全性、药代动力学及药效动力学研究
- Author:
Yan TIAN
1
;
Xinyi YANG
;
Shuangshuang LIN
;
Jinjie HE
;
Jingjing WANG
;
Qiong WEI
;
Xingxing HUANG
;
Xiaojie WU
Author Information
1. 复旦大学附属华山医院临床药理研究中心,上海 200040;国家老年疾病临床医学研究中心,上海 200040;复旦大学附属华山医院研究型病房,上海 200040
- Publication Type:Journal Article
- Keywords:
Chinese healthy subjects;
YZJ-3058 tablets;
pharmacokinetics;
pharmacodynamics
- From:
Chinese Journal of Clinical Pharmacology and Therapeutics
2025;30(6):796-803
- CountryChina
- Language:Chinese
-
Abstract:
AIM:To evaluate the safety and toler-ability of single dose oral BTK inhibitor YZJ-3058 tablets under fasting conditions in healthy adults,as well as the pharmacokinetic and pharmacologi-cal characteristics of YZJ-3058 and its metabolites.METHODS:A total of 22 healthy subjects were en-rolled in this experiment and administered a single dose orally.They were divided into three groups:50 mg,100 mg,and 200 mg.Among them,2 sub-jects were enrolled in the 50 mg dose group,and 10 subjects were enrolled in the 100 mg and 200 mg dose groups,respectively.RESULTS:In healthy subjects,YZJ-3058 tablets were administered orally on an empty stomach at doses of 50,100,and 200 mg,with a median Tmax of 1.25 to 2.00 hours and an average Cmax of 62.85,89.44,and 99.20 ng/mL,re-spectively.The average AUC0-t was 183.87,297.72,and 453.98 h·ng-1·mL,respectively.The average AUC0-∞ was 189.30,321.33,and 551.44 h·ng-1·mL,and the median t1/2 was 1.16,5.06,and 7.97 hours,respectively.After a single oral administration of 50,100,and 200 mg YZJ-3058 tablets,the highest target occupancy rate was achieved at 4 hours.The average BTK occupancy rates at 24 hours after ad-ministration were 88.95％,96.73％,and 99.24％,re-spectively.The average BTK occupancy rates at 48 hours after administration were 75.65％,89.80％,and 96.68％,respectively.No serious adverse events or adverse events leading to withdrawal oc-curred,and all subjects had good tolerability.CON-CLUSION:YZJ-3058 tablets have good safety and tolerability for single oral administration on an empty stomach in healthy subjects within the dose range of 50-200 mg.Cmax and AUC increase with dose,with fast absorption and saturation.The ter-minal elimination rate gradually slows down with dose increase,and it has a significant and sus-tained occupying effect on BTK targets.
