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This is a phase I, single-center, open-label, single-sequence, 3-period, PK drug interaction study evaluating the effect of napabucasin in healthy volunteers on the single-dose PK of several cytochrome P450 (CYP450) probe drugs as well as a BCRP substrate.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Single-sequence 3-period | Experimental | Period 1: napabucasin 240 mg BID on days 1-2 Period 2: cytochrome P450 probe drugs during days 1-4 Period 3: napabucasin 240 mg BID on days 1-11, cytochrome P450 probe drugs during days 6-9 |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| napabucasin | Drug | Napabucasin will be administered at dose of 240 mg twice daily, every 12 hours (BID) on days 1-2 in period 1, and on days 1-11 in period 3. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Pharmacokinetics for napabucasin by assessing plasma concentration | Predose and up to 7 days post dose | |
| Pharmacokinetics for probe drugs by assessing plasma concentration | Predose and up to 7 days post dose |
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Inclusion Criteria
A subject will be eligible for inclusion in this study only if all the following criteria apply:
Exclusion Criteria
A Subject will not be eligible for inclusion in this study if any of the following criteria apply:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Accel Research Sites | DeLand | Florida | 32720 | United States |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 34107166 | Derived | Dai X, Karol MD, Hitron M, Hard ML, Goulet MT, McLaughlin CF, Brantley SJ. Napabucasin Drug-Drug Interaction Potential, Safety, Tolerability, and Pharmacokinetics Following Oral Dosing in Healthy Adult Volunteers. Clin Pharmacol Drug Dev. 2021 Aug;10(8):824-839. doi: 10.1002/cpdd.961. Epub 2021 Jun 9. |
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|
| cytochrome P450 (CYP450) probe drugs or BCRP transporter substrate | Drug | CYP450 probe drugs or BCRP transporter substrate will be administered once every period during days 1-4 in period 2, and days 6-9 in period 3. |
|
| ID | Term |
|---|---|
| C000621033 | napabucasin |
| D003577 | Cytochrome P-450 Enzyme System |
| ID | Term |
|---|---|
| D003580 | Cytochromes |
| D045762 | Enzymes and Coenzymes |
| D006899 | Mixed Function Oxygenases |
| D010105 | Oxygenases |
| D010088 | Oxidoreductases |
| D004798 | Enzymes |
| D006420 | Hemeproteins |
| D011506 | Proteins |
| D000602 | Amino Acids, Peptides, and Proteins |
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