Hypercholesterolemia
Conditions
Brief summary
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.
Detailed description
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.
Interventions
DRUGBKR-017
BKR-017 is an oral tablet formulation designed to target delivery of sodium butyrate to the colon via colon-targeting technology.
Sponsors
BioKier Inc.
National Heart, Lung, and Blood Institute (NHLBI)
Study design
Observational model
COHORT
Time perspective
PROSPECTIVE
Eligibility
Sex/Gender
ALL
Age
18 Years to 70 Years
Inclusion criteria
* Men and women, ages 18-70 inclusive * Subjects currently on statin treatments.
Exclusion criteria
* Presence of cirrhosis, or other causes of liver disease * Substantial alcohol consumption (\>20 g/day for women or \>30 g/day for men) * History of bariatric or intestinal surgery * Active gastrointestinal disease including but not limited to irritable bowel syndrome, inflammatory bowel disease (e.g., Crohn's disease and ulcerative colitis), diverticulitis, gastroparesis. * Active and clinically significant pancreatic disease, or renal disease as determined by the investigator. * History of heart disease that in the opinion of the investigator should exclude the subject from the study. * Untreated or uncontrolled hyperthyroidism or hypothyroidism, or other significant thyroid disease * Active significant infection as determined by the investigator. * Known allergy to butyrate or any of the components of the tablets. * Participation in a clinical trial and/or Dosing with an investigational drug during the 30 days before screening, or within 5 half-lives of receipt of an investigational drug or twice the duration of the biological effect of any investigational drug (whichever is longer) * Pregnant, nursing, or trying to become pregnant. * In the investigator's judgment, the subject is not suitable for the study for any other reason or cannot commit to the requirements of the study. * Taking part in another clinical trial or being in the exclusion period of a previous clinical trial.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Peak Plasma Concentration (Cmax) of butyrate | 8 days | Changes, from pre-dosing levels, in levels of butyrate in plasma after a single dose and after seven days of dosing. |
| Area under the plasma concentration versus time curve (AUC) | 8 days | AUC after 7 days of dosing will be compared to AUC after a single dose to determine if butyrate eaccumulates in the plasma. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Incidence of Treatment-Emergent Adverse Events as assessed by blood pressure | 8 days | An assessment of safety will be made using blood pressure at screening, after single dose, and after 7 days repeat dosing. |
| Incidence of Treatment-Emergent Adverse Events as assessed by heart rate | 8 days | An assessment of safety will be made using heart rate at screening, after single dose, and after 7 days repeat dosing. |
| Incidence of Treatment-Emergent Adverse Events as assessed by a hematology panel | 8 days | Hematology (CBC) will be performed at screening, after single dose, and after 7 days repeat dosing. |
| Incidence of Treatment-Emergent Adverse Events as assessed by chemistry laboratory safety parameters | 8 days | An assessment of chemistry laboratory safety parameters will be performed at screening, after single dose, and after 7 days repeat dosing. |
Countries
United States
Contacts
PRINCIPAL_INVESTIGATORFrank Greenway, MD
Pennington Biomedical Research Center
Outcome results
None listed