The purpose of this study was to explore the safety, tolerability and pharmacokinetics (PK) of single ascending oral doses of SKLB1028 in healthy subjects. This study has also explored the effect of food on the PK of SKLB1028.
The study was divided into 2 parts. Part 1(Dose Escalation) included 2 cohorts (Cohort 1 and Cohort 2) and subjects received a single oral dose of SKLB1028 50 or 100 mg on Day 1. In Part 2 (Food Effect) included 2 cohorts (Cohort A and Cohort B), subjects received a single oral dose of SKLB1028 150 mg in a fasting and a fed state, with a 10-day washout period between the 2 doses.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
26
SKLB1028, capsule, oral
Beijing Friendship Hospital, Capital Medical University
Beijing, China
Number of participants with treatment-related adverse events (TEAEs)
TEAEs were assessed by CTCAE v5.0 in Part 1
Time frame: Throughout the study period, with an average of 10 days.
Maximum plasma concentration (Cmax) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Area under the concentration-time curve from time 0 to last quantifiable concentration (AUC0-last) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Area under the concentration-time curve from time 0 to infinity (AUCinf) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Time to Cmax (Tmax) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Terminal-elimination half-life (T1/2) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Apparent volume of distribution (Vz/F) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Apparent clearance (CLz/F) of SKLB1028 in Part 2
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Maximum plasma concentration ( Cmax) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
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Area under the concentration-time curve from time 0 to last quantifiable concentration (AUC0-last) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Area under the concentration-time curve from time 0 to infinity (AUCinf) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Time to Cmax (Tmax) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Terminal-elimination half-life (T1/2) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Apparent volume of distribution (Vz/F) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Apparent Clearance (CLz/F) of SKLB1028 in Part 1
Time frame: Pre-dose and multiple timepoints up to 144 hours post-dose
Number of participants with TEAEs
TEAEs were assessed by CTCAE v5.0 in Part 2
Time frame: Throughout the study period, with an average of 20 days