PK, PD and Safety of Tegoprazan 12.5 mg After Oral Administration in Healthy Subjects

Healthy Clinical Trial

Official title:

Phase 1 Clinical Trial to Explore Pharmacokinetics, Pharmacodynamics and Safety of Tegoprazan 12.5 mg After Oral Administration in Healthy Subjects

Clinical Trial Details — Status: Enrolling by invitation

Administrative data

• NCT number: NCT06332638
• Other study ID #: IN_APA_124
• Status: Enrolling by invitation
• Phase: Phase 1
• Start date: March 19, 2024
• Est. completion date: July 31, 2024

Study information

• Verified date: March 2024
• Source: HK inno.N Corporation
• Contact: n/a
• Is FDA regulated: No
• Study type: Interventional

Clinical Trial Summary

The primary objective of this study is to explore pharmacokinetics, pharmacodynamics, and safety of tegoprazan 12.5 mg in healthy subjects when orally administered as a single dose or as multiple doses twice daily.

Description:

The secondary objectives of this study are

• To compare pharmacokinetics and pharmacodynamics of tegoprazan 12.5 mg in healthy subjects between oral multiple-dose administration twice daily for 1 day and oral single-dose administration.

• To evaluate pharmacokinetics and pharmacodynamics of tegoprazan 12.5 mg administered orally twice daily for 14 days in healthy subjects in comparison with tegoprazan 25 mg administered orally once daily for 14 days in healthy subjects.

• To evaluate pharmacodynamics of tegoprazan 12.5 mg administered orally twice daily for 14 days or tegoprazan 25 mg administered orally once daily for 14 days in healthy subjects in comparison with famotidine 20 mg administered orally twice daily for 14 days in healthy subjects.

Recruitment information / eligibility

• Status: Enrolling by invitation
• Enrollment: 36
• Est. completion date: July 31, 2024
• Est. primary completion date: July 31, 2024
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: All
• Age group: 19 Years to 45 Years

Eligibility

Inclusion Criteria:

1. Healthy adults aged = 19 years to = 45 years at the time of screening testing

2. Body mass index (BMI) = 18.5 kg/m2 to = 28.0 kg/m2 (BMI = weight (kg) / height (m)2)

3. Those who have been fully informed of study purpose and procedures, properties of the investigational products(IPs), etc. and have voluntarily decide to participate in this study and signed an informed consent form (ICF), prior to participation in the study

Exclusion Criteria:

1. Medical history

1. Previous history or presence of clinically significant hepatic, renal, gastrointestinal, respiratory, musculoskeletal, endocrine, neuropsychiatric, hemato-oncologic, urinary and cardiovascular (including cardiac arrhythmia) disorders in the judgment of the investigator

2. Previous history of gastrointestinal diseases (e.g., gastritis, gastrospasm, gastroesophageal reflux disease (GERD), Crohn's disease, ulcers, etc.) or abdominal surgery (excluding simple appendectomy or hernia surgery) which may affect drug absorption in the judgment of the investigator

3. Presence of anatomical disorders that make it difficult to insert and maintain a catheter for intragastric pH measurement, or expected intolerance to catheterization for intragastric pH measurement

4. Hereditary problems such as galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption

2. Clinical laboratory tests and electrocardiogram (ECG)

1. AST or ALT value = 1.5 x upper limit of normal (ULN) as a result of clinical laboratory testing at screening

2. Total bilirubin value = 2.0 x upper limit of normal (ULN) as a result of clinical laboratory testing at screening

3. eGFR value calculated using the CKD-EPI formula < 80 mL/min as a result of clinical laboratory testing at screening

4. Any clinically significant abnormality as a result of ECG at screening

5. Positive test result for H. pylori at screening

3. Allergies and drug abuse

1. History of hypersensitivity to the IPs, components of the IPs, and other drugs (benzimidazoles, H2 receptor antagonists, aspirin, antibiotics, etc.)

2. Previous history of drug abuse or positive drug screening test result

4. Prohibited concomitant medications/diets

1. Consumption of medicines (including herbal medicines) or abnormal diets (e.g., at least 1L/day of grapefruit juice, much garlic, broccoli, kale, etc.) which may affect the absorption, distribution, metabolism, and excretion of the IP within 28 days before the screening visit

2. Administration of the drugs affecting gastric pH within 14 days before the screening visit (including potassium-competitive acid blockers, proton pump inhibitors, H2-receptor antagonists, and antacids) or administration of ethical-the-counter (ETC) drugs, any over-the-counter (OTC) drugs, vitamins, etc. within 10 days before the screening visit

3. Administration of another IP by participating in another clinical trial within 6 months prior to the screening visit (but those who are not administered the IP can participate in this study)

5. Blood donation and transfusion

1. Whole blood donation within 60 days before the screening visit

2. Blood component donation or transfusion within 30 days before the screening visit

6. Pregnancy, breastfeeding, and non-use of contraceptives

1. Pregnant women, women who tested positive for pregnancy, or breastfeeding women

2. Failure to use medically recognized and proper double contraceptive methods or medically acceptable contraceptive methods (intrauterine device showing a demonstrated pregnancy failure rate, combined use of physical barrier method and spermicide, vasectomy, salpingectomy/tubal ligation, hysterectomy, etc.) in the subject or his/her spouse or partner from the date of screening visit until 30 days after the last dose of the IP

7. Others

1. Mean alcohol intake exceeding 30 g/day per week for recent 4 weeks before the screening visit or positive alcohol breath test result

2. Mean number of smoked cigarettes exceeding 10 cigarettes/day per week for recent 4 weeks before the screening visit

3. Mean caffeine intake exceeding 400 mg/day per week for recent 4 weeks before the screening visit

4. Presence of clinically significant findings that make the subject ineligible for this study in the judgment of the investigator

Related Conditions & MeSH terms

• Healthy

Intervention

Drug:
• Tegoprazan 12.5mg
Oral administration of one tablet of Tegoprazan 12.5mg twice daily for 14 days.
• Tegoprazan 25mg
Oral administration of one tablet of Tegoprazan 25mg once daily for 14 days.
• Famotidine 20mg
Oral administration of one tablet of Famotidine 20mg twice daily for 14 days.

Locations

Country	Name	City	State
Korea, Republic of	Inje University Busan Paik Hospital	Busan

Sponsors (1)

Lead Sponsor	Collaborator
HK inno.N Corporation

Country where clinical trial is conducted

Korea, Republic of, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Cmax of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	AUC0-t of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	AUC0-8 of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	Tmax of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	t1/2ß of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	CL/F of tegoprazan	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	Vd/F of tegoprazan	Pharmacokinetic evaluation (Day 1)	Pre-dose(0 hour) up to 24 hours on Day 1
Primary	Css,max of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning) (-12, 0 hour) up to 24 hours on Day 14
Primary	Css,min of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	Css,avg of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	AUCtau,ss of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	Tmax,ss of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	t1/2ß,ss of tegoprazan and tegoprazan's metabolite M1	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	CLss/F of tegoprazan	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	Vdss/F of tegoprazan	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	Accumulation index of tegoprazan	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Primary	Fluctuation of tegoprazan	Pharmacokinetic evaluation (Day 14)	Pre-dose(morning)(-12, 0 hour) up to 24 hours on Day 14
Secondary	24-hour, daytime and nighttime mean pH	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime median pH	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime TpH>3(%)	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime TpH>4(%)	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime ? TpH>3(%)	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime ? TpH>4(%)	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime ? mean pH	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14
Secondary	24-hour, daytime and nighttime ? median pH	Pharmacodynamic evaluation	24 hours on Day -1, Day 1, Day 7, and Day 14