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The study comprises three parts: single ascending dose (SAD) studies of CX2101A tablets at 40 mg, 100 mg, and 160 mg; a relative bioavailability (BA) study comparing single-dose administration of 100 mg CX2101A tablets and enteric-coated tablets; and a multiple ascending dose (MAD) study of CX2101A tablets. The BA study (100 mg) is integrated into the SAD study(Nested within the SAD protocol to optimize resource utilization).
Randomized, Double-Blind, Placebo-Controlled Design All studies are conducted under standardized fasting conditions to eliminate food interference Blinding is maintained throughout the entire study period for both subjects and investigators
Single Ascending Dose (SAD) Study Dose Groups: 40 mg, 100 mg, 160 mg (3 cohorts) Subject Allocation: 10 subjects/cohort (8 CX2101A + 2 placebo)
Integration with BA Study:
The 100 mg cohort will serve as the reference for bioavailability evaluation Subjects completing SAD phase will proceed to receive enteric-coated formulations
Multiple Ascending Dose (MAD) Study Dose Groups: Same 40 mg, 100 mg, 160 mg cohorts Subject Allocation: 10 subjects/cohort (8 CX2101A + 2 placebo) Administration Schedule: Daily dosing for 5 consecutive days Relative Bioavailability (BA) Study
Cohort Integration: Conducted within the 100 mg SAD group (N=10)
Treatment Sequence:
Initial single-dose administration of CX2101A tablets
≥7-day washout period (PK data-driven adjustment) Second single-dose administration of enteric-coated tablets
Subject Allocation:
CX2101A tablets group: 8 subjects (CX2101A + 8 placebo) Enteric-coated group: 8 subjects (CX2101A + 8 placebo)
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| CX2101A Placebo Tablet | Placebo Comparator | Participants from SAD cohort received single dose of CX2101A placebo tablet orally. Participant from MAD cohort received CX2101A placebo tablet orally once daily for 5 days. |
|
| CX2101A Tablet | Experimental | Participants from SAD cohort received single dose of CX2101A tablet orally. Participant from MAD cohort received CX2101A tablet orally once daily for 5 days. Dose levels are 40 mg, 100mg, 160mg. |
|
| CX2101A Placebo Enteric-Coated Tablet | Placebo Comparator | Participants received single dose of CX2101A placebo enteric-coated tablet. |
|
| CX2101A Enteric-Coated Tablet | Experimental | Participants received single dose of 100 mg CX2101A enteric-coated tablet. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| CX2101A tablet | Drug | CX2101A tablet |
| |
| CX2101A placebo tablet |
| Measure | Description | Time Frame |
|---|---|---|
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Peak Concentration (Cmax): The maximum plasma concentration of the drug. | From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Area Under the Curve from Time Zero to the Last Measurable Concentration (AUC0-t): The area under the plasma concentration-time curve from time zero to the last measurable concentration. | From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Area Under the Curve from Time Zero Extrapolated to Infinity (AUC0-∞): The area under the plasma concentration-time curve from time zero extrapolated to infinity. | From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Time to Reach Peak Concentration (Tmax): The time at which the peak plasma concentration is reached. | From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Elimination Half-Life (T1/2): The time required for the plasma concentration to decrease by half. | From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Apparent Volume of Distribution (Vz/F): The volume into which the drug appears to be distributed, corrected for bioavailability. |
| Measure | Description | Time Frame |
|---|---|---|
| Rate and severity of treatment-emergent adverse events (TEAEs) | Based on the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) Version 5.0 | From day 1 until 4 days after treatment |
| Vital signs |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Zhejiang Xiaoshan Hospital | Hangzhou | 311202 | China |
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| ID | Term |
|---|---|
| D000086382 | COVID-19 |
| D018352 | Coronavirus Infections |
| ID | Term |
|---|---|
| D011024 | Pneumonia, Viral |
| D011014 | Pneumonia |
| D012141 | Respiratory Tract Infections |
| D007239 | Infections |
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| Drug |
CX2101A placebo tablet |
|
| CX2101A enteric-coated tablet | Drug | CX2101A enteric-coated tablet |
|
| CX2101A placebo enteric-coated tablet | Drug | CX2101A placebo enteric-coated tablet |
|
| From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Apparent Clearance (CL/F): The clearance of the drug from the plasma, corrected for bioavailability. | From time zero up to 96 hours post-dose following last dose of CX2101A |
| PK profile of CX2101A and its metabolite CX210101 and CX210108 | Percentage of AUC Extrapolated (AUC_%Extrap): The percentage of the total AUC that is extrapolated beyond the last measurable concentration. | From time zero up to 96 hours post-dose following last dose of CX2101A |
Number of participants with abnormal results of vital signs.
| From day 1 until 4 days after treatment |
| Electrocardiogram (ECG) | Number of participants with abnormal results of electrocardiogram. | From day 1 until 4 days after treatment |
| Physical examinations | Number of participants with abnormal results of physical examinations | From day 1 until 4 days after treatment |
| Complete blood count test | Number of participants with abnormal results of complete blood count test. | From day 1 until 4 days after treatment |
| Clinical Chemistry | Number of participants with abnormal results of clinical chemistry. | From day 1 until 4 days after treatment |
| D014777 |
| Virus Diseases |
| D003333 | Coronaviridae Infections |
| D030341 | Nidovirales Infections |
| D012327 | RNA Virus Infections |
| D008171 | Lung Diseases |
| D012140 | Respiratory Tract Diseases |