The purpose of this study is to evaluate the pharmacokinetic profile and systemic exposure of BKR-017 in individuals on statin therapy after a single dose and at steady state after seven days repeated twice daily dosing.
BioKier will conduct an open-label study to evaluate the safety and PK profile of BKR-017 in ten hypercholesterolemic (\>100 mg/dL) statin-treated subjects (to reflect the target population), aged 18-70, after a single dose and at steady-state after seven days repeat dosing. On the morning of Study Day 0, subjects will take three tablets (1.5 g of BKR-017), followed by breakfast. Blood samples will be taken for PK analysis at -1, -0.25, 1, 2, 4, 6, 8, 10, 12, and 24 hours after dosing. After an overnight stay in the clinic, the 24-hour PK sample will be taken, and subjects will be provided with one week's supply of BKR-017 tablets and a diary for keeping track of tablets taken, instructed to take three 500-mg tablets (1.5 g) BID, and released from the clinic. On Study Day 8, subjects will return to the clinic, and Study Day 0 procedures will be repeated after dose-compliance is confirmed. PK samples will be analyzed.
Study Type
OBSERVATIONAL
Enrollment
9
BKR-017 is an oral tablet formulation designed to target delivery of sodium butyrate to the colon via colon-targeting technology.
Pennington Biomedical Research Center
Baton Rouge, Louisiana, United States
Peak Plasma Concentration (Cmax) of butyrate
Changes, from pre-dosing levels, in levels of butyrate in plasma after a single dose and after seven days of dosing.
Time frame: 8 days
Area under the plasma concentration versus time curve (AUC)
AUC after 7 days of dosing will be compared to AUC after a single dose to determine if butyrate eaccumulates in the plasma.
Time frame: 8 days
Incidence of Treatment-Emergent Adverse Events as assessed by blood pressure
An assessment of safety will be made using blood pressure at screening, after single dose, and after 7 days repeat dosing.
Time frame: 8 days
Incidence of Treatment-Emergent Adverse Events as assessed by heart rate
An assessment of safety will be made using heart rate at screening, after single dose, and after 7 days repeat dosing.
Time frame: 8 days
Incidence of Treatment-Emergent Adverse Events as assessed by a hematology panel
Hematology (CBC) will be performed at screening, after single dose, and after 7 days repeat dosing.
Time frame: 8 days
Incidence of Treatment-Emergent Adverse Events as assessed by chemistry laboratory safety parameters
An assessment of chemistry laboratory safety parameters will be performed at screening, after single dose, and after 7 days repeat dosing.
Time frame: 8 days
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