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| Name | Class |
|---|---|
| Food and Drug Administration (FDA) | FED |
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This is an open-label, non-randomized, fixed-sequence study. Subjects will undergo a rosuvastatin phase and eltrombopag and rosuvastatin phase to identify biomarkers for Breast Cancer Resistance Protein (BCRP).
Membrane transporters are critical in the absorption, distribution and elimination of drugs, and are important target sites for drug-drug interactions (DDIs). During drug development, clinical studies characterizing transporter-mediated DDIs are frequently required. There has been enormous interest in identifying and validating serum biomarkers or surrogate probes to be used in predicting in vivo (clinical) DDIs. These biomarkers could complement in vitro studies, reducing false positive and false negative predictions, as well as the cost and time required for clinical development.
In this open-label, non-randomized, fixed-sequence study, subjects will undergo a rosuvastatin phase and eltrombopag and rosuvastatin phase to identify biomarkers for a membrane transporter known as Breast Cancer Resistance Protein (BCRP). The primary goal of this study is to validate and discover BCRP candidate biomarkers in a focused clinical DDI study with healthy volunteers to determine whether they can serve as clinical biomarkers for BCRP-mediated DDIs.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Placebo and Rosuvastatin | Experimental | Subjects will be dosed with placebo tablet and Rosuvastatin 10mg tablet |
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| Eltrombopag and Rosuvastatin | Experimental | Subjects will be dosed with Eltrombopag 75mg tablet and Rosuvastatin 10mg tablet |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Rosuvastatin | Drug | Rosuvastatin will be administered as follows: Day 1: single dose of 10 mg Rosuvastatin tablet. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Composite of pharmacokinetics of co-administration of rosuvastatin and eltrombopag in healthy volunteers. | Mean difference in area under the curve (AUC) between rosuvastatin 10mg + placebo versus rosuvastatin 10mg + eltrombopag 75mg | 24 and 72 hours |
| Composite of pharmacokinetics of co-administration of rosuvastatin and eltrombopag in healthy volunteers. | Mean difference in Cmax between rosuvastatin 10mg + placebo versus rosuvastatin 10mg + eltrombopag 75mg | 24 hour |
| Measure | Description | Time Frame |
|---|---|---|
| Composite of BCRP biomarkers of co-administration of rosuvastatin and eltrombopag in healthy volunteers. | Mean difference in BCRP biomarker Cmax between rosuvastatin 10mg + placebo vs rosuvastatin 10mg + eltrombopag 75mg | 24 and 72 hours |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Kathleen M Giacomini, Ph.D. | University of California, San Francisco | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Ucsf Ctsi Crc | San Francisco | California | 94143 | United States |
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| ID | Term |
|---|---|
| D000068718 | Rosuvastatin Calcium |
| C520809 | eltrombopag |
| ID | Term |
|---|---|
| D013449 | Sulfonamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D005464 | Fluorobenzenes |
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This is a single center, an open-label, non-randomized, fixed-sequence study.
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| Rosuvastatin (Inhibitor arm) | Drug | Rosuvastatin will be administered as follows: Day 8: single dose of 10 mg Rosuvastatin tablet. |
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| Eltrombopag | Drug | Eltrombopag will be administered as follows: Day 8: single dose of 75 mg Eltrombopag tablet. |
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| D006845 |
| Hydrocarbons, Fluorinated |
| D006846 | Hydrocarbons, Halogenated |
| D006838 | Hydrocarbons |
| D013450 | Sulfones |
| D013457 | Sulfur Compounds |
| D011743 | Pyrimidines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |