This is an open-label study. This study includes 2 parts, in which part 1 is a relative BA study, Part 2 is a DDI study. Part 1 and Part 2 could be performed in parallel.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
37
An oral small molecule prodrug that effectively inhibits the SARS-CoV-2 main protease (Mpro).
A strong CYP3A4 inhibitor
A strong CYP3A4 inducer
Zhejiang Xiaoshan Hospital
Hangzhou, Zhejiang, China
Comparison of Area Under the Curve (AUC) from time 0 to last time point(AUC0-t) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
To compare AUC0-t of a single 600mg dose of two different oral strength of STI-1558(200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules)in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Time frame: Up to 2 weeks.
Comparison of AUC from time 0 extrapolated to infinity(AUC0-inf ) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
To compare AUC0-inf of a single 600mg dose of two different oral strength of STI-1558(200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules)in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Time frame: Up to 2 weeks.
Comparison of maximum observed concentration(Cmax) profiles of two different oral strength of STI-1558 to determine the Relative Bioavailability
To compare Cmax of a single 600mg dose of two different oral strength of STI-1558(200 mg/capsule × 3 capsules and 100 mg/capsule × 6 capsules)in healthy adult, human subjects under fasting conditions, to establish relative bioavailability.
Time frame: Up to 2 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the pharmacokinetics(PK) of STI-1558 by collecting serum at protocol-specified time points: Cmax
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-t
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inhibitor (itraconazole) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-inf.
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Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: Cmax
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-t
Time frame: Up to 3 weeks.
To determine the effect of repeat doses of a strong CYP3A4 inducer (rifampin) on the PK of STI-1558 by collecting serum at protocol-specified time points: AUC0-inf
Time frame: Up to 3 weeks.
Cmax of AC1115(an active metabolite of STI-1558)
Time frame: Up to 2 weeks for part 1 and 3 weeks for part 2.
AUC0-t of AC1115(an active metabolite of STI-1558)
Time frame: Up to 2 weeks for part 1 and 3 weeks for part 2.
AUC0-inf of AC1115(an active metabolite of STI-1558)
Time frame: Up to 2 weeks for part 1 and 3 weeks for part 2.