A Phase1, Double-blind, Randomized, Placebo-control, Single Center, Single Dose Administration, Dose Escalation Study to Investigate the Pharmacokinetics, Safety and Tolerability of SA001 in Healthy Male Volunteers.
Overview
- Phase
- Phase 1
- Intervention
- SA001 120mg or Placebo
- Conditions
- Healthy
- Sponsor
- Samjin Pharmaceutical Co., Ltd.
- Enrollment
- 40
- Locations
- 1
- Primary Endpoint
- The incidence of treated related adverse event
- Status
- Completed
- Last Updated
- 4 years ago
Overview
Brief Summary
The purpose of this phase1 study is to investigate the pharmacokinetics, safety and tolerability of a single oral dose of SA001 and its active metabolite in healthy male volunteers.
Detailed Description
This study consists of Part 1 followed Part 2. Part 1 (Dose escalation study, SA001 60mg\~300mg dose group) The part 1 is a dose escalation study. The starting dose is SA001 60mg, and the maximum dose is 300mg. Each dose group is assigned to SA001 or Placebo in a ratio of 3:1. The pharmacokinetics, safety and tolerability of SA001 and its metabolite are investigated after a single oral administration on the fasting state. Part 2 (Single dose and food effect study, SA001 120mg and 300mg dose group) The purpose of this part 2 is to evaluate the food effect of a high-fat diets(HFDs) on the single oral dose pharmacokinetics of SA001 and its metabolite.
Investigators
Eligibility Criteria
Inclusion Criteria
- •19 years to 45 years (Healthy male Korean)
- •Body weight of 55 to 90kg; and BMI of 18.0 to 27.0 kg/m\^2
- •Subject who voluntarily agrees to participate in this study and has given a written informed consent, after fully understanding the detailed explanation of this study
Exclusion Criteria
- •Subject with a disease history of any clinically significant condition as below.
- •Liver, Kidney, nervous system, immune system, respiratory system, endocrine system, tumor, cardiovascular disease or mental illness (mood disorder or obsessive-compulsive disorder etc.) etc.
- •Subject with a history of gastrointestinal disease (Crohn's disease, ulcer, acute or chronic pancreatitis, etc.) or gastrointestinal surgery (except simple appendicectomy or hernia surgery) that may affect the absorption of the study drug
- •Subject with a history of clinically significant hypersensitivity or hypersensitivity reactions to drugs (aspirin, antibiotics, etc.)
- •Serum ALT(SGPT)/AST(SGOT) \>1.5×institutional upper limit normal (ULN)
- •eGFR\< 90mL/min/1.73m\^2
- •Systolic blood pressure \<100 mmHg or \>160 mmHg
- •Diastolic blood pressure \<60 mmHg or \>100 mmHg
- •Inadequate cardiac function confirmed by 12-lead ECG findings at screening as followings:
- •QTcF \> 430msec (males)
Arms & Interventions
Cohort 2 (SA001 120mg or Placebo)
6 subjects receiving a single dose of 120mg SA001 and 2 subjects receiving placebo
Intervention: SA001 120mg or Placebo
Cohort 1 (SA001 60mg or Placebo)
6 subjects receiving a single dose of 60mg SA001 and 2 subjects receiving placebo
Intervention: SA001 60mg or Placebo
Cohort 3 (SA001 180mg or Placebo)
6 subjects receiving a single dose of 180mg SA001 and 2 subjects receiving placebo
Intervention: SA001 180mg or Placebo
Cohort 4 (SA001 240mg or Placebo)
6 subjects receiving a single dose of 240mg SA001 and 2 subjects receiving placebo
Intervention: SA001 240mg or Placebo
Cohort 5 (SA001 300mg or Placebo)
6 subjects receiving a single dose of 300mg SA001 and 2 subjects receiving placebo
Intervention: SA001 300mg or Placebo
Outcomes
Primary Outcomes
The incidence of treated related adverse event
Time Frame: Part1: Day-2(administration) to approximately Day 15 (Post study visit)
Safety/Tolerability Assessment in the part 1
Secondary Outcomes
- Area under the curve (AUC) from time 0 extrapolated to infinity (AUC0-∞) of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)
- Maximum observed plasma concentration (Cmax) of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)
- Area under the curve (AUC) from time 0 to the time of the last quantifiable concentration (AUC0-tlast) of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)
- Fraction recovered unchanged in urine (FR) of SA001 and its metabolite(Part1: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose, Part2: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose)
- CLR of SA001 and its metabolite(Part1: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose, Part2: predose and 0 ~ 4, 4 ~ 8, 8 ~ 12, 12 ~ 24, 24 ~ 32 and 32 ~ 48 hours postdose)
- Time to reach the maximum observed plasma concentration (tmax) of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)
- t1/2 of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)
- Vz/F of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)
- CL/F of SA001 and its metabolite(Part1: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose, Part2: predose and 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 32, and 48 hours postdose)