Clinical Study to Investigate the Pharmacokinetics and Safety/Tolerability of SA001 in Healthy Male Volunteers

NCT05303961 | Completed Phase 1

• 1 other identifier: SJSA001_02
• Study Type: interventional
• Target: 56
• Locations: 0 countries
• Sites: N/A

Brief Summary

This study consists of Part 1 followed Part 2. Part 1 The purpose of this phase1 study is to investigate the pharmacokinetics, safety and tolerability of a single oral dose of SA001 and active comparator(Rebamipide) in healthy male volunteers. Part 2 The purpose of this phase1 study is to investigate the pharmacokinetics, safety and tolerability of multiple oral dose of SA001 in healthy male volunteers.

Conditions

Healthy

Outcome Measures

Primary Outcomes (19)

• Measure the Area Under the plasma concentration versus time Curve from the first observed to last(AUClast) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0.25~48hours, Day 15 0.25~48hours)

• Measure the Area Under the plasma concentration versus time Curve from the first sampled data extrapolated to infinity(AUCinf) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 1: Predose9Day 1 0hour, Day 15 0hour), Postdose(Day 1 0.25~48hours, Day 15 0.25~48hours)

• Measure the Peak Plasma Concentration (Cmax) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0.25~48hours, Day 15 0.25~48hours)

• Measure the Time to peak drug concentration(Tmax) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting blood and urine before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0.25~48hours, Day 15 0.25~48hours)

• Measure the Half Life(t1/2) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0.25~48hours, Day 15 0.25~48hours)

• Measure the apparent total body clearance(CL/F) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0~48hours, Day 15 0~24hours)

• Measure the apparent volume of distribution(Vz/F) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0~48hours, Day 15 0~24hours)

• Measure the Renal Clearance(CLr) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0~48hours, Day 15 0~24hours)

• Measure the cumulative fraction excreted unchanged parent in urine(Fe) of SA001 and Rebamipide

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 1: Predose(Day 1 0hour, Day 15 0hour), Postdose(Day 1 0~48hours, Day 15 0~24hours)

• Measure the Trough Drug Concentration at steady state(Cmin,ss) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the Peak Plasma Concentration at steady state(Cmax,ss) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the average drug concentration in plasma during a dosing interval at steady state(Cav,ss) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the area under the plasma concentration-time curve for dosing interval(AUCτ) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the Time to peak drug concentration at steady state(Tmax,ss) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the Half Life(t1/2) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the Peak-trough Fluctuation (PTF) of SA001

  Investigate the pharmacokinetic parameters by collecting blood before and during administration of the investigational product.

  Part 2: Predose(Day 1 0, 12hour, Day 2 0hour, Day 5 0hour, Day 7 12hour, Day 8 0, 12hour), Postdose(Day 1 0.25~8hours, Day 8 0.25~8hours)

• Measure the Fraction recovered unchanged in urine (FR) of SA001

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 2: Predose(Day 1 0hour, Day 8 0hour, Day 16 0hour), Postdose(Day 1 0~24hours, Day 8 0~24hours, Day 16 0~24hours, Day 17 0~24hours)

• Measure the apparent total body clearance(CL/F) of SA001

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 2: Predose(Day 1 0hour, Day 8 0hour, Day 16 0hour), Postdose(Day 1 0~24hours, Day 8 0~24hours, Day 16 0~24hours, Day 17 0~24hours)

• Measure the Renal Clearance(CLr) of SA001

  Investigate the pharmacokinetic parameters by collecting urine before and during administration of the investigational product.

  Part 2: Predose(Day 1 0hour, Day 8 0hour, Day 16 0hour), Postdose(Day 1 0~24hours, Day 8 0~24hours, Day 16 0~24hours, Day 17 0~24hours)

Secondary Outcomes (1)

• Incidence of Adverse Event(AE)

  Part 1: Day-1(before the administration) to approximately Day 24 (Post study Visit) / Part 2: Day-1(before the administration) to approximately Day 29 (Post study Visit)

Study Arms (3)

SA001

EXPERIMENTAL

Part 1: 24 subjects are assigned to single dose groups(240mg, 480mg, 720mg, 1080mg of SA001) in a ratio of 1:1:1:1 and receiving each dose of SA001 in the period 1. Part2: 18 subjects are assinged to multiple dose groups(360mg, 720mg, 1080mg of SA001) in a ratio of 1:1:1 and receiving each dose of SA001.

Drug: SA001 240mg + Rebamipide 200mg or Placebo; Drug: SA001 480mg or Placebo; Drug: SA001 710mg + Rebamipide 600mg or Placebo; Drug: SA001 1,080mg or Placebo; Drug: SA001 360mg or Placebo; Drug: SA001 720mg or Placebo

Rebamipide

ACTIVE COMPARATOR

Part 1: 12 subjects are assigned to single dose groups(200mg, 600mg of Rebamipide) in a ratio of 1:1 and receiving each dose of Rebamipide in the period 2.

Drug: SA001 240mg + Rebamipide 200mg or Placebo; Drug: SA001 710mg + Rebamipide 600mg or Placebo

Placebo

PLACEBO COMPARATOR

Part 1: 8 subjects receiving a single dose of Placebo in the period 1. Part2: 6 subjects receiving multiple dose of Placebo.

Drug: SA001 240mg + Rebamipide 200mg or Placebo; Drug: SA001 480mg or Placebo; Drug: SA001 710mg + Rebamipide 600mg or Placebo; Drug: SA001 1,080mg or Placebo; Drug: SA001 360mg or Placebo; Drug: SA001 720mg or Placebo

Interventions

SA001 240mg + Rebamipide 200mg or Placebo DRUG

Cohort 1 in the Part1(Single dose): Study drug(SA001 240mg + Rebamipide 200mg), Comparator: Placebo

Placebo; Rebamipide; SA001

SA001 480mg or Placebo DRUG

Cohort 2 in the Part1(Single dose): Study drug(SA001 480mg), Comparator(Placebo)

Placebo; SA001

SA001 710mg + Rebamipide 600mg or Placebo DRUG

Cohort 3 in the Part1(Single dose): Study drug(SA001 720mg + Rebamipide 600mg), Comparator(Placebo)

Placebo; Rebamipide; SA001

SA001 1,080mg or Placebo DRUG

Cohort 4 in the Part1(Single dose): Study drug(SA001 1,080mg), Comparator(Placebo)

Placebo; SA001

SA001 360mg or Placebo DRUG

Cohort 5 in the Part2(Multiple dose): Study drug(SA001 360mg), Comparator(Placebo)

Placebo; SA001

SA001 720mg or Placebo DRUG

Cohort 6 in the Part2(Multiple dose): Study drug(SA001 720mg), Comparator(Placebo)

Placebo; SA001

Eligibility Criteria

• Age: 19 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• years to 45 years (Healthy male Korean)
• Body weight of 55 to 90kg; and BMI of 18.0 to 27.0 kg/m2
• 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

You may not qualify if:

• 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/1.73m2
• 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)
• PR interval \> 200msec or \< 110msec
• QRS complex \> 120msec
• Evidence of 2nd- or 3rd-degree atrioventricular (AV) block
• Pathologic Q waves (defined as Q-wave \> 40msec or depth \> 0.5mV)
• Evidence of ventricular preexicitation, left bundle branch block (LBBB), right bundle branch block (RBBB, Incomplete RBBB)

Sponsors & Collaborators

• Samjin Pharmaceutical Co., Ltd.: lead

MeSH Terms

Interventions

rebamipide

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: OTHER
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 22, 2022
• First Posted: March 31, 2022
• Study Start: June 7, 2016
• Primary Completion: November 11, 2016
• Study Completion: November 11, 2016
• Last Updated: March 31, 2022

Record last verified: 2022-03