Aimed at evaluating the safety, tolerability, and pharmacokinetic characteristics of single and multiple doses of XTYW007 in healthy subjects and healthy subjects with elevated LDL-C, as well as studying the effects of food on the pharmacokinetics and metabolic transformation of XTYW007, and preliminarily assessing the pharmacodynamics of XTYW007.
This study is a single-center, randomized, double-blind Phase I/IIa clinical trial assessing the safety, tolerability, and pharmacokinetics of single and multiple doses.Aimed at evaluating the safety, tolerability, and pharmacokinetic characteristics of single and multiple doses of XTYW007 in healthy subjects and healthy subjects with elevated LDL-C, as well as studying the effects of food on the pharmacokinetics and metabolic transformation of XTYW007, and preliminarily assessing the pharmacodynamics of XTYW007.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
94
Each group consists of 8 people, with 6 receiving the trial drug XTYW007 and 2 receiving a placebo. The sentinel method is used for enrollment, meaning that the first 2 subjects (one male and one female, both receiving the trial drug) are enrolled and observed for 96 hours (after the Day 5 tolerance assessment). If there are no intolerable reactions, the remaining 6 subjects are enrolled and randomly assigned to receive the trial drug or placebo in a 2:1 ratio.
A two-period crossover administration was used, with a 14-day washout period. In Group A, 8 subjects received the drug on D1 under fasting conditions in the first period, and on D15 under fed conditions in the second period. In Group B, 6 subjects taking the investigational drug received it on D1 under fed conditions in the first period, and on D15 under fasting conditions in the second period.
The First Hospital of Jilin University
Jilin, Changchun, China
Treatment-related adverse events
Number of participants who experienced treatment-related adverse events as assessed by CTCAE v5.0.
Time frame: Days 1-11 of administration
Cmax
Cmax
Time frame: Days 1-11 of administration
Tmax
Tmax
Time frame: Days 1-11 of administration
t1/2
t1/2
Time frame: Days 1-11 of administration
AUC
AUC
Time frame: Days 1-11 of administration
CL/F
CL/F
Time frame: Days 1-11 of administration
Vz/F
Vz/F
Time frame: Days 1-11 of administration
CLr/F
CLr/F
Time frame: Days 1-11 of administration
Ae0-72 h
Ae0-72 h
Time frame: Days 1-4 of administration
Fe0-72 h
Fe0-72 h
Time frame: Days 1-4 of administration
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Each group consists of 8 subjects, with 6 receiving the investigational drug XTYW007 and 2 receiving a placebo. A sentinel dosing approach is used, where 2 subjects (one male and one female) are first enrolled and administered the investigational drug. After 96 hours of observation (tolerance evaluation on Day 5), if no intolerable issues occur, the remaining 6 subjects are enrolled and randomized 2:1 to receive the investigational drug or placebo. In the multiple-dose group, the drug is administered once every morning on an empty stomach (QD) for 14 consecutive days.
Blood lipids
TC , TG , LDL-C, HDL-C, Apo A1, Apo B, Lp(a)
Time frame: Days 1-11 of administration
Thyroid function
TSH, TT4, TT3, FT4, FT3
Time frame: Days 1-11 of administration
Sex hormone-binding globulin (SHBG)
SHBG
Time frame: Days 1-11 of administration