The study included three clinical studies, namely a single ascending dose (SAD) study, a multiple ascending dose (MAD) study, and a high-fat diet food effect (FE) study.
Study 1: SAD study A single-center, randomized, double-blind, placebo-controlled, single ascending dose study of TJ0113 capsules in healthy subjects. Six dose groups (A1-A6) were established, with doses of 80 mg, 160 mg, 260 mg, 400 mg, 540 mg, and 720 mg, respectively. A total of 72 healthy adult subjects (12 per group) were enrolled, including both males and females. Subjects in each dose group were randomized in a 5:1 ratio to receive either the investigational product, TJ0113 capsules, or placebo (10 subjects received the investigational product and 2 subjects received placebo). Two subjects in the 80 mg dose group were set as a sentinel arm and were randomized in a 1:1 ratio to receive either TJ0113 capsules or placebo. After completing the 24-hour safety observation following sentinel dosing, the remaining 10 subjects in the 80 mg dose group were randomized in a 9:1 ratio to receive either TJ0113 capsules or placebo. Study 2: MAD study In the single-center, randomized, double-blind, placebo-controlled, MAD study of TJ0113 capsules in healthy subjects, 3 dose groups (B1 to B3) of 200 mg once daily(QD), 400 mg QD, 300 mg twice daily(BID )were set. A total of 36 healthy adult subjects (12 per group) were enrolled, including both males and females. Subjects in each dose group were randomized in a 5:1 ratio to receive either the investigational product, TJ0113 capsules, or placebo (10 subjects received the investigational product and 2 subjects received placebo). Subjects in the 200 mg and 400 mg dose groups received once-daily (QD) dosing, while subjects in the 300 mg BID dose group received twice-daily (BID) dosing administered with warm water, for 7 consecutive days (only one dose in the morning on Day 7). Study 3: FE study A single-center, single-dose, randomized, open-label, 2-sequence, 2-period, crossover study to evaluate the effect of a standard high-fat diet on the pharmacokinetics of TJ0113 capsules after single oral administration (200 mg) in healthy subjects. A total of 20 healthy adult subjects were enrolled in this period and randomized in a 1:1 ratio to 2 dosing sequences (C1: fasting-fed; C2: fed-fasting), with 10 subjects per group (all receiving the investigational product TJ0113 capsule). Each dosing sequence consisted of 2 cycles with 1 dose administered in each cycle. Group C1 received the dose in a fasting state during the first cycle and in a fed state during the second cycle; Group C2 received the dose in a fed state during the first cycle and in a fasting state during the second cycle . The two cycles were separated by a 7-day washout period.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
130
Participants will receive oral administration of TJ0113.
Participants will receive oral administration of Placebo.
Zhejiang Xiaoshan hospital
Hangzhou, Zhejiang, China
Treatment-emergent adverse event (TEAE) incidence of TJ0113 capsules after single oral administration in SAD study
Types, incidence rates, and severity of adverse events. Safety evaluation indicators include, but are not limited to, the following items: adverse events, physical examination, vital signs, electrocardiogram (ECG), laboratory test results (coagulation function, complete blood count, blood biochemistry, urinalysis plus urine specific gravity, etc.)
Time frame: Within 12 days after the last administration
Treatment-emergent adverse event (TEAE) incidence of TJ0113 capsules after multiple oral administration in MAD study
Types, incidence rates, and severity of adverse events. Safety evaluation indicators include, but are not limited to, the following items: adverse events, physical examination, vital signs, electrocardiogram (ECG), laboratory test results (coagulation function, complete blood count, blood biochemistry, urinalysis plus urine specific gravity, etc.)
Time frame: Within 12 days after the last administration
Maximum concentration (Cmax) of TJ0113 capsules after oral administration in SAD study
PK parameters for the SAD study mainly included maximum concentration (Cmax)
Time frame: Within 72 hours after the last administration
Area under the plasma concentration versus time curve (AUC) of TJ0113 capsules after oral administration in SAD study
PK parameters for the SAD study mainly included area under the plasma concentration versus time curve (AUC)
Time frame: Within 72 hours after the last administration
Half life(t1/2) of TJ0113 capsules after oral administration in SAD study
PK parameters for the food effect study mainly included half life(t1/2)
Time frame: Within 72 hours after the last administration
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Time to maximum concentration (Tmax) of TJ0113 capsules after oral administration in SAD study
PK parameters for the food effect study mainly included time to maximum
Time frame: Within 72 hours after the last administration
Maximum concentration (Cmax) of TJ0113 capsules after oral administration in MAD study
PK parameters for the MAD study mainly included maximum concentration (Cmax)
Time frame: Within 72 hours after the last administration
Area under the plasma concentration versus time curve (AUC) of TJ0113 capsules after oral administration in MAD study
PK parameters for the MAD study mainly included area under the plasma concentration versus time curve (AUC)
Time frame: Within 72 hours after the last administration
Half life(t1/2) of TJ0113 capsules after oral administration in MAD study
PK parameters for the food effect study mainly included half life(t1/2)
Time frame: Within 72 hours after the last administration
Time to maximum concentration (Tmax) of TJ0113 capsules after oral administration in MAD study
PK parameters for the food effect study mainly included time to maximum
Time frame: Within 72 hours after the last administration
Maximum concentration (Cmax) of TJ0113 capsules after oral administration with a standard high-fat diet in FE
PK parameters for the FE study mainly included maximum concentration (Cmax)
Time frame: Within 72 hours after the last administration
Area under the plasma concentration versus time curve (AUC) of TJ0113 capsules after oral administration with a standard high-fat diet in FE study
PK parameters for the FE study mainly included area under the plasma concentration versus time curve (AUC)
Time frame: Within 72 hours after the last administration
Half life(t1/2) of TJ0113 capsules after oral administration with a standard high-fat diet in FE study
PK parameters for the food effect study mainly included half life(t1/2)
Time frame: Within 72 hours after the last administration
Time to maximum concentration (Tmax) of TJ0113 capsules after oral administration with a standard high-fat diet in FE study
PK parameters for the food effect study mainly included time to maximum
Time frame: Within 72 hours after the last administration
Treatment-emergent adverse event (TEAE) incidence of TJ0113 capsules after multiple oral administration with a standard high-fat diet in FE study
Types, incidence rates, and severity of adverse events. Safety evaluation indicators include, but are not limited to, the following items: adverse events, physical examination, vital signs, electrocardiogram (ECG), laboratory test results (coagulation function, complete blood count, blood biochemistry, urinalysis plus urine specific gravity, etc.)
Time frame: Within 15 days after the last administration