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

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.

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