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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part 1: TR | Experimental | Subjects will take a single dose of test product 200mg/capsule on Day 1 of the study, then reference product 100mg/capsule on Day 8 of the study. |
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| Part 1: RT | Experimental | Subjects will take a single dose of reference product 100mg/capsule on Day 1 of the study, then test product 200mg/capsule on Day 8 of the study. |
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| Part 1: Group 1 | Experimental | Subjects will take a single dose of STI-1558 200mg/capsule on Day 1. Starting from Day 4, subjects will orally take 200mg of itraconazole, q.d, for 6 consecutive days (Day 4 to Day 9). The 5th dose (Day 8) of itraconazole will be co-administered with STI-1558 (200 mg/capsule × 3 capsules) to subjects. |
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| Part 1: Group 2 | Experimental | Subjects will take a single dose of STI-1558 200mg/capsule on Day 1. Starting from Day 4, subjects will orally take 600mg of rifampin, q.d, for 9 consecutive days (Day 4 to Day 12). The 8th dose (Day 11) of rifampin will be co-administered with STI-1558 (200 mg/capsule × 3 capsules) to subjects. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| STI-1558 | Drug | An oral small molecule prodrug that effectively inhibits the SARS-CoV-2 main protease (Mpro). |
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| Measure | Description | Time Frame |
|---|---|---|
| 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. | 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. | 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. | 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 | 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 | 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. |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax of AC1115(an active metabolite of STI-1558) | Up to 2 weeks for part 1 and 3 weeks for part 2. | |
| AUC0-t of AC1115(an active metabolite of STI-1558) | Up to 2 weeks for part 1 and 3 weeks for part 2. |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Zhejiang Xiaoshan Hospital | Hangzhou | Zhejiang | China |
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| Itraconazole | Drug | A strong CYP3A4 inhibitor |
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| Rifampin | Drug | A strong CYP3A4 inducer |
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| 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 | 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 | 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 | Up to 3 weeks. |
| AUC0-inf of AC1115(an active metabolite of STI-1558) | Up to 2 weeks for part 1 and 3 weeks for part 2. |
| ID | Term |
|---|---|
| C000722724 | STI-1558 |
| D017964 | Itraconazole |
| D012293 | Rifampin |
| ID | Term |
|---|---|
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D010879 | Piperazines |
| D012294 | Rifamycins |
| D006576 | Heterocyclic Compounds, 4 or More Rings |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D047029 | Lactams, Macrocyclic |
| D047028 | Macrocyclic Compounds |
| D011083 | Polycyclic Compounds |
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