A Study to Explore Pharmacokinetics/Pharmacodynamics and Safety of Tegoprazan BID Dosing in Healthy Subjects

A Phase 1 Clinical Trial to Explore Pharmacokinetics, Pharmacodynamics and Safety After Twice-daily Dosing of Tegoprazan Tablets in Healthy Subjects

The main purpose of this study is to explore the pharmacokinetics, pharmacodynamics and safety after twice-daily dosing of tegoprazan tablets in healthy subjects.

Study Overview

• Status: Unknown
• Conditions: Healthy
• Intervention / Treatment: Drug: Tegoprazan dose A or placebo; Drug: Tegoprazan dose B or placebo; Drug: Tegoprazan dose C or placebo; Drug: Tegoprazan dose D or placebo

Detailed Description

• To explore the pharmacokinetics, pharmacodynamics and safety in accordance with the dose escalation when tegoprazan is given orally twice daily for 3 days in healthy subjects.
• To compare the pharmacodynamics and safety of tegoprazan oral administration and esomeprazole infusion for 24 hours

• Study Type: Interventional
• Enrollment (Anticipated): 40
• Phase: Phase 1

Contacts and Locations

Study Locations

• Korea, Republic of
  • Busan, Korea, Republic of, 47392
    • Recruiting
    • Inje University Busan Paik Hospital
    • Contact: Jon Lyul Kim, MD, PhD

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 19 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy subjects aged 19 to 45(inclusive) years at screening.
• Subjects with body mass index (BMI) in the range of 18.5 kg/m^2 to 28.0 kg/m^2(inclusive)
• Subjects who voluntarily agreed to participate in the study after being fully informed of the purpose, content, and characteristics of the investigational product(IP) prior to the study participation.

Exclusion Criteria:

1. Past medical history

   • Subjects who are determined by the investigator to have clinically significant history or disease related to the liver, kidney, digestive system, respiratory system, musculoskeletal system, endocrine system, neuropsychiatric system, hemato-oncology system, urinary system and cardiovascular system including cardiac arrhythmia.
   • Subjects who are determined by the investigator to have past history of gastrointestinal diseases (ex.: gastritis, GERD, Crohn's disease, ulcers etc.) or abdominal surgery (except simple appendectomy or herniotomy) that may affect the IP absorption.

2. Diagnostic test and electrocardiogram (ECG)

   • If H. pylori test result is positive at screening
   • If the AST or ALT value is more than 1.25 times the upper limit of normal under the screening test
   • If the total bilirubin value is more than 1.5 times the upper limit of normal under the screening test
   • If the eGFR calculated by CKD-EPI formula is less than 80 mL/min at screening
   • Subjects showing clinically significant abnormalities on ECG at screening

3. Allergy and drug abuse

   • Subjects who are hypersensitive to the investigational product or its active ingredient and any other medications (aspirin, antibiotics etc.)
   • Subjects with history of substance abuse or positive results from drug screening test.

4. Contraindicated drugs/foods

   • Subjects who have been taking any medications (including herbal medicines) or on an abnormal diet (ex: consuming more than 1L of grapefruit juice per day, large amounts of garlic, broccoli and kale, etc.) that can affect the absorption, distribution, metabolism and excretion of the IP within 28 days from the first IP administration date
   • Subjects who took any prescription drugs(ETC) or any over-the-counter drugs(OTC) within 10 days from the first IP administration date
   • Subjects who participated in other clinical trials or bioequivalence test and received other investigational product within 6 months from the first day of the IP administration (allowed to participate only if the other investigational product(s) was(were) not taken)

5. Blood donation and transfusion

   • Subjects who donated whole blood within 60 days from the first day of the investigational product administration
   • Subjects who received blood transfusion or made apheresis blood donation within 30 days from the first day of the IP administration

6. Pregnancy, Breastfeeding, and Contraception

   • Women who are pregnant, breast-feeding or have positive result on pregnancy test.
   • Subjects who are unable to use medically proven dual contraceptive methods or medically acceptable contraceptive method (intrauterine device with proven pregnancy failure rate, concurrent use of physical barrier method and spermicide, vasectomy, tubectomy/ligation, and hysterectomy, etc.) by the subject or spouse or partner from the screening date to 30 days after the last IP administration date.

7. Others

   • Subjects whose weekly alcohol intake exceeds 30g/day in the last 4 weeks prior to the screening visit or found positive on alcohol test
   • Subjects who smoke more than 10 cigarettes/day per week over the last 4 weeks prior to the screening visit
   • Subjects with caffeine consumption of more than 400mg/day per week over the last 4 weeks prior to the screening visit
   • Subjects with clinically significant findings that the investigator determined to be unqualified for participation in the clinical trial

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Sequential Assignment
• Masking: Single

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: T1; Tegoprazan A mg or placebo	Drug: Tegoprazan dose A or placebo; Tegoprazan A mg or placebo taken orally twice daily for 3 days.
Experimental: T2; Tegoprazan B mg or placebo	Drug: Tegoprazan dose B or placebo; Tegoprazan B mg or placebo taken orally twice daily for 3 days.
Experimental: T3; Tegoprazan C mg or placebo	Drug: Tegoprazan dose C or placebo; Tegoprazan C mg or placebo taken orally twice daily for 3 days.
Experimental: T4; Tegoprazan D mg or placebo	Drug: Tegoprazan dose D or placebo; Tegoprazan D mg or placebo taken orally twice daily for 3 days.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetics Evaluation	Cmax of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	AUC0-t of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	AUC0-∞ of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	Tmax of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	t1/2β of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	CL/F of Tegoprazan	Up to 24 hours
Pharmacokinetics Evaluation	Vd/F of Tegoprazan	Up to 24 hours
Pharmacokinetics Evaluation	Css,max of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	Css,min of Tegoprazan and M1	Up to 24 hours
Pharmacokinetic Evaluation	Css,avg of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	AUC48-72h of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	Tmax,ss of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	t1/2β,ss of Tegoprazan and M1	Up to 24 hours
Pharmacokinetics Evaluation	CLss/F of Tegoprazan	Up to 24 hours
Pharmacokinetics Evaluation	Vdss/F of Tegoprazan	Up to 24 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacodynamics Evaluation	Mean pH	24 hours
Pharmacodynamics Evaluation	Median pH	24 hours
Pharmacodynamics Evaluation	TpH>4(%)	24 hours
Pharmacodynamics Evaluation	TpH>6(%)	24 hours
Pharmacodynamics Evaluation	Basal pH	24 hours
Pharmacodynamics Evaluation	Δ TpH>4(%)	24 hours
Pharmacodynamics Evaluation	Δ TpH>6(%)	24 hours
Pharmacodynamics Evaluation	Δ mean pH	24 hours
Pharmacodynamics Evaluation	Δ median pH	24 hours

Collaborators and Investigators

• Sponsor: HK inno.N Corporation
• Investigators: Principal Investigator: Jong Lyul Kim, MD, PhD, Inje University

Study record dates

Study Major Dates

• Study Start (Actual): September 24, 2020
• Primary Completion (Anticipated): March 1, 2021
• Study Completion (Anticipated): June 1, 2021

Study Registration Dates

• First Submitted: October 7, 2020
• First Submitted That Met QC Criteria: October 7, 2020
• First Posted (Actual): October 14, 2020

Study Record Updates

• Last Update Posted (Actual): December 28, 2020
• Last Update Submitted That Met QC Criteria: December 23, 2020
• Last Verified: August 1, 2020

More Information

Terms related to this study

• Other Study ID Numbers: IN_APA_119

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No