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: The first three doses studied in the study will be 0.5 mg, 1.0 mg and 2.5 mg.
Pharmacokinetics from each dose cohort will be characterized before initiation of dosing in
the subsequent cohorts. Based on the PK data from the first 3 dose cohorts, subsequent dose
escalation levels will be determined based on predicted AUC(0-24h). Eight subjects in each
dose cohort will receive active drug. The total number of cohorts will be up to 6. 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. The dose level will be determined from the PK data obtained from Part 1.
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