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.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
NONE
Enrollment
11
Rosuvastatin will be administered as follows: Day 1: single dose of 10 mg Rosuvastatin tablet.
Rosuvastatin will be administered as follows: Day 8: single dose of 10 mg Rosuvastatin tablet.
Eltrombopag will be administered as follows: Day 8: single dose of 75 mg Eltrombopag tablet.
Ucsf Ctsi Crc
San Francisco, California, United States
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
Time frame: 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
Time frame: 24 hour
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
Time frame: 24 and 72 hours
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