AIM: To evaluate the safety and tolerability of single dose oral BTK inhibitor YZJ-3058 tablets under fasting conditions in healthy adults, as well as the pharmacokinetic and pharmacological characteristics of YZJ-3058 and its metabolites. METHODS: A total of 22 healthy subjects were enrolled 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 subjects 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, respectively. 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 administration were 88.95%, 96.73%, and 99.24%, respectively. 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 occurred, and all subjects had good tolerability. CONCLUSION: 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 terminal elimination rate gradually slows down with dose increase, and it has a significant and sustained occupying effect on BTK targets.