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Phase 1 Single Ascending Dose Study to Evaluate Safety, Tolerability and Pharmacokinetics of KBP-5074

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02228733
Lead Sponsor
KBP Biosciences
Brief Summary

This single ascending dose (SAD) study in healthy subjects will evaluate the safety, tolerability and pharmacokinetics of KBP-5074. PK/PD (plasma aldosterone, serum potassium and urine albumin levels) relationships will be explored to support the selection of dosing regimens of KBP-5074 that are suitable for the Phase 2 dose-finding study to evaluate the efficacy, safety and tolerability of KBP-5074 in patients that could slow the progression of nephropathy as well as control hypertension.

Detailed Description

This is an open-label, parallel-group, dose-escalation study to evaluate the safety, tolerability and pharmacokinetics of KBP-5074 following a single dose administration of KBP-5074 with and without food. The study includes 2 parts.

Part 1: Pharmacokinetics from each dose cohort will be characterized before initiation of dosing in the subsequent cohorts. Eight subjects in each dose cohort will receive active drug. The total number of cohorts will be up to 5. Extensive PK samplings will be collected prior to and following administration of single dose of KBP-5074.

Part 2: A separate panel of 6 subjects will receive a single dose of KBP-5074 under fed conditions. Extensive PK samplings will be collected prior to and following administration of single dose of KBP-5074 under fed conditions.

Serum and plasma samples for pharmacodynamic markers (plasma aldosterone and serum potassium levels) will be collected at pre-dose and postdose in both Part 1 and Part 2.

The urine samples will be also used for quantitative determination of urinary albumin in both Part 1 and Part 2.

Safety assessments will include monitoring of adverse events (AEs), vital signs (blood pressure, pulse rate, respiratory rate and oral temperature), clinical laboratory findings, 12-lead electrocardiograms (ECGs), and physical examination findings.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
46
Inclusion Criteria
  • Body mass index (BMI) 19 ≤ BMI ≤ 30 kg/m2, no significant medical history, normal renal function and in good general health
Exclusion Criteria
  • Clinically significant history of gastrointestinal, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, bronchopulmonary, neurologic, immunologic, lipid metabolism disorders, or drug hypersensitivity; A history of prescription drug abuse, or illicit drug use within 6 months prior to screening

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
KBP-5074: Cohort 2KBP-5074Healthy Volunteers will receive one dose of KBP-5074
KBP-5074: Cohort 1KBP-5074Healthy Volunteers will receive one dose of KBP-5074
KBP-5074: Cohort 5KBP-5074Healthy Volunteers will receive one dose of KBP-5074
KBP-5074: Cohort 3KBP-5074Healthy Volunteers will receive one dose of KBP-5074
KBP-5074: Fed GroupKBP-5074Healthy Volunteers will receive one dose of KBP-5074
KBP-5074: Cohort 4KBP-5074Healthy Volunteers will receive one dose of KBP-5074
Primary Outcome Measures
NameTimeMethod
The safety and tolerability14 days

Assessing the number of participants with adverse events, abnormal vital signs, clinical laboratory findings, 12-lead ECGs and physical examinations): pre dose and post dose

Area Under Curve (AUC) Time Frame14 days

Assessing drug exposure across time. AUC is a useful metric when trying to determine whether two formulations of the same dose (for example a capsule and a tablet) result in equal amounts of tissue or plasma exposure. Predose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 72, 96, 120, 168, 216, 264 and 312 hours post-dose

Secondary Outcome Measures
NameTimeMethod
The plasma aldosterone, serum potassium and urine albumin levels14 days

Assessing blood levels of aldosterone, potassium and urine albumin at pre dose and postdose

The effect of food on Area Under Curve (AUC) Time Frame14 days

Assessing the food effect on drug exposure across time at pre dose, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 10, 12, 18, 24, 36, 48, 72, 96, 120, 168, 216, 264 and 312 hours post-dose

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