The purpose of this study is to evaluate the safety and tolerability of X842 after administration of single and multiple doses in healthy subjects
This is a single-center, open label, First-In-human (FIH), Phase I clinical study to evaluate the safety, tolerability, pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of single dose and multiple doses of X842 capsules in healthy subjects. The study comprises a Single Ascending Dose (SAD) part, a Multiple Ascending Dose (MAD) part, and a Food Effect (FE) study.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
80
A total of 7 dose groups will be set for the ascending dose: 5.6 mg, 12.5 mg, 25 mg, 50 mg, 100 mg, 150 mg, 225 mg. In the 5.6 mg dose group, 4 subjects will receive X842; in the 12.5 mg, 25 mg, 50 mg, 100 mg, 150 mg, 225 mg dose groups, 8 subjects in each group will receive X842. Each subject can only receive a certain dose level and cannot enter in multiple dose groups repeatedly.
Two dose groups will be set, including the groups receiving the recommended phase II dose and a higher dose; Eight subjects will be enrolled in each group, with half male and half female, who will receive X842 once daily for 5 consecutive days. Each subject can only receive a certain dose level and cannot enter in multiple dose groups repeatedly.
The Affiliated Hospital of Guizhou Medical University
Guiyang, Guizhou, China
Occurrence and frequency of AEs after single and multiple doses of X842.
Safety and tolerability will be assessed by occurrence and frequency of AEs. The adverse event assessment will follow the recommendations and grading system of Common Terminology Criteria for Adverse Events (CTCAE) v5.0. Summary statistics will be applied.
Time frame: Five Weeks
Vital signs of body temperature
Time frame: Five Weeks
Vital signs of blood pressure
Blood pressure measurements included systolic (mmHg) and diastolic (mmHg).
Time frame: Five Weeks
Vital signs of respiratory rate
Time frame: Five Weeks
Physical Examination of height
Time frame: Five Weeks
Physical Examination of weight
Time frame: Five Weeks
Number of clinically significant changes in Electrocardiograms (ECGs)
The investigator or the sub-investigator interpreted the ECG using one of the following categories: "within normal limits", "abnormal but not clinically significant", or "abnormal and clinically significant".
Time frame: Five Weeks
Number of Clinically significant changes in lab assessment of blood serum
Time frame: Five Weeks
Number of Clinically significant changes in the lab assessment of blood
Time frame: Five Weeks
Number of Clinically significant changes in the lab assessment of urine
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Twelve subjects (appropriate ratio of male to female) screened for eligibility will be randomized into Group A and B. The 6 subjects in Group A will take the study drug (X842) in fasted condition and subject in Group B will take the study drug in fed condition in the 1st cycle. In the 2nd Cycle, subjects in Group A will take the study drug in fed condition, and subjects in Group B will take the study drug in fasted condition. The interval between the two cycles is at least 7 days.
Time frame: Five Weeks
Measurement of the PK profile (Cmax)
To assess the Maximum Plasma Concentration (Cmax)
Time frame: Up to 48 hours after dosing
Measurement of the PK profile (t1/2)
To assess the plasma half life (t1/2) of drug
Time frame: Up to 48 hours after dosing
Measurement of the PD profile (intragastric pH)
To assess and characterize the PD profile with measurements of intragastric pH
Time frame: Up to 24 hours after dosing