A Study to Evaluate Effect of IN-A001 on Pharmacokinetics of Tacrolimus in Healthy Volunteers

Phase 1

• Conditions: Healthy
• Interventions: Drug: Tacrolimus; Drug: IN-A001(Tegoprazan); Drug: IN-A001(Tegoprazan) + Tacrolimus

• Registration Number: NCT05353010
• Lead Sponsor: HK inno.N Corporation

Brief Summary

This study aims to investigate the effect of IN-A001 50mg on the pharmacokinetics of Tacrolimus 5mg in healthy volunteers

Detailed Description

This is a open-label, 1-sequence, 2-period, multiple oral dose, phase 1 study. Healthy subjects will be assigned to a group and sequentially administerd Tacrolimus and IN-A001.

Study Timeline

• Status Verified: 2022-03
• Study First Submitted: 2022-04-25
• Study First Submitted QC: 2022-04-25
• Last Update Submitted: 2022-04-25
• Study First Posted: 2022-04-29
• Last Update Posted: 2022-04-29
• Study Start: 2022-05-01
• Primary Completion: 2022-07-01
• Study Completion: 2022-11-01

Recruitment & Eligibility

• Status: UNKNOWN
• Sex: All
• Target Recruitment: 12

Inclusion Criteria

1. Body mass index(BMI) ≥ 19.0 and ≤ 28.0 kg/m^2 at the time of screening.
2. Those who agreed to use combination of effective or medically approved contraceptive method from the date of first administration of investigational product(IP) to the end of the clinical trial (when testing for final safety evaluation).
3. In the case of female participant, who has negative result at the hCG urine pregnancy test and is not pregnant or currently breastfeeding.

Exclusion Criteria

1. Has clinically significant infections

2. Has a history of malignancy

3. Has a history of gastrointestinal disease that may affect the absorption of investigational product.

4. Has genetic problems such as galactose intolerance, Lapp lactase deficiency, or glucose-galactose absorption disorder etc.

5. History of hypersensitivity and severe allergic reaction to any of the components of IP.

6. Has participated in any other clinical study, etc. and received IPs within 180 days prior to the screening visit.

7. Excessive smoking (> 10 cigarettes/day) within 14 days prior to the screening visit.

8. Excessive drinking ((> 21 units/week) within 14 days prior to the screening visit.

9. Has shown the following results from the laboratory test during the screening period.

   • AST, ALT level > 1.5 × ULN at screening;
   • eGFR(estimated glomerular filtration rate) estimated on the basis of CKD-EPI is less than 60 mL/min/1.73 m2;

10. Has shown the following results during the 12-lead electrocardiogram during the screening period.

    • QTc > 450 ms
    • Clinically significant abnormal rhythm and findings when the investigator medically determines

11. Determined ineligible for study participation by the investigator for other reasons.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Period 1: A; Period 2: B and C	IN-A001(Tegoprazan)	A: Oral Administration of Tacrolimus 5mg once / B: Oral Administration of IN-A001(Tegoprazan) 50mg QD for 7 days / C: Oral Administration of IN-A001(Tegoprazan) 50mg + Tacrolimus 5mg once
Period 1: A; Period 2: B and C	IN-A001(Tegoprazan) + Tacrolimus	A: Oral Administration of Tacrolimus 5mg once / B: Oral Administration of IN-A001(Tegoprazan) 50mg QD for 7 days / C: Oral Administration of IN-A001(Tegoprazan) 50mg + Tacrolimus 5mg once
Period 1: A; Period 2: B and C	Tacrolimus	A: Oral Administration of Tacrolimus 5mg once / B: Oral Administration of IN-A001(Tegoprazan) 50mg QD for 7 days / C: Oral Administration of IN-A001(Tegoprazan) 50mg + Tacrolimus 5mg once

Primary Outcome Measures

Name	Time	Method
Cmax of Tacrolimus	up to 72 hours(period 1), up to 240 hours(period 2)	Maximum Plasma Concentration at Steady State of Tacrolimus
Tmax of Tacrolimus	up to 72 hours(period 1), up to 240 hours(period 2)	Time to Cmax at steady state
AUClast of Tacrolimus	up to 72 hours(period 1), up to 240 hours(period 2)	Area under the concentration-time curve from dosing (time 0) to the time of the last measured concentration
AUCinf of Tacrolimus	up to 72 hours(period 1), up to 240 hours(period 2)	Area under the curve from time 0 extrapolated to infinite time
T1/2β of Tacrolimus	up to 72 hours(period 1), up to 240 hours(period 2)	Half-life of the drug during elimination phase

Secondary Outcome Measures

Name	Time	Method
Point estimates and 90% CI for log (GMR of Period 2 Cmax, AUClast, AUCinf) / log (GMR of Period 1 Cmax, AUClast, AUCinf) of Tacrolimus	up to 72 hours(period 1), up to 240 hours(period 2)	log(GMR of Period 2 Cmax, AUClast, AUCinf) / log (GMR of Period 1 Cmax, AUClast, AUCinf)
Cmax of Tegoprazan	up to 240 hours(period 2)	Maximum Plasma Concentration at Steady State of Tegoprazan
Tmax of Tegoprazan	up to 240 hours(period 2)	Time to Cmax at steady state
AUClast of Tegoprazan	up to 240 hours(period 2)	Area under the concentration-time curve from dosing (time 0) to the time of the last measured concentration
AUCinf of Tegoprazan	up to 240 hours(period 2)	Area under the curve from time 0 extrapolated to infinite time
T1/2β of Tegoprazan	up to 240 hours(period 2)	Half-life of the drug during elimination phase

Trial Locations

Locations (1)

Asan Medical Center; 🇰🇷 Seoul, Korea, Republic of