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The primary objective of this trial is to assess the effect of probenecid on the pharmacokinetics (PK) of single-dose pexidartinib in healthy subjects.
Secondary objectives are to assess the safety and tolerability of pexidartinib alone and in combination with probenecid.
Participants will be confined to the clinic for approximately 32 days. Blood samples will be collected for PK analysis of pexidartinib and metabolites at predose and up to 312 hours (h) post dose.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Pexidartinib then Probenecid | Experimental | Participants receive Sequence AB: Treatment A (pexidartinib) first, then Treatment B (probenecid), with a washout period between them |
|
| Probenecid then Pexidartinib | Experimental | Participants receive Sequence BA: Treatment B (probenecid) first, then Treatment A (pexidartinib), with a washout period between them |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Pexidartinib | Drug | Orally, on Day 2 |
|
| Measure | Description | Time Frame |
|---|---|---|
| Maximum Plasma Concentration (Cmax) | Maximum concentration of the drug and its metabolite in plasma | predose to 312 hours post dose |
| Time to Maximum Concentration (Tmax) | Time at which the maximum concentration is reached | within 312 hours post dose |
| Area under the curve to the last quantifiable measurement (AUClast) | Area under the drug concentration time curve from the first measurement to the last | within 312 hours post dose |
| Measure | Description | Time Frame |
|---|---|---|
| Number of participants experiencing an adverse event | Total number of participants experiencing any adverse event | within 312 hours post dose |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Clinical Study Leader | Daiichi Sankyo | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Worldwide Clinical Trials Early Phase Services | San Antonio | Texas | 78217 | United States |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 36264536 | Derived | Zahir H, Greenberg J, Shuster D, Hsu C, Watanabe K, LaCreta F. Evaluation of Absorption and Metabolism-Based DDI Potential of Pexidartinib in Healthy Subjects. Clin Pharmacokinet. 2022 Nov;61(11):1623-1639. doi: 10.1007/s40262-022-01172-9. Epub 2022 Oct 20. |
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| ID | Term |
|---|---|
| C000600259 | pexidartinib |
| D011339 | Probenecid |
| ID | Term |
|---|---|
| D013449 | Sulfonamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D013450 | Sulfones |
| D013457 |
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This is an open-label, 2-treatment sequence, 2-period, crossover study with a washout between doses and treatment periods
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| Probenecid | Drug | Orally, on Day 2 |
|
|
| Sulfur Compounds |