Study to Evaluate Pharmacokinetic and Pharmacodynamic Drug Interactions and Safety of IY-NS250 and IY-NT-SR

A Randomized, Open-label, Multiple-dose, Crossover Phase 1 Clinical Trial to Compare and Evaluate the Safety, PK and PD Characteristics After Oral Administration of IY-NS250 and IY-NT-SR in Healthy Adult Volunteers

This study comparative evaluation of safety and pharmacokinetic and pharmacodynamic properties in oral repeat administration of IY-NS250 and IY-NT-SR in healthy adult

Study Overview

• Status: Completed
• Conditions: Pharmacokinetics; Pharmacodynamics
• Intervention / Treatment: Drug: IY-NS250; Drug: IY-NT-SR

Detailed Description

Not provided

• Study Type: Interventional
• Enrollment (Actual): 56
• Phase: Phase 1

Contacts and Locations

Study Locations

• Korea, Republic of
  • Seowon-gu
    • Seoul, Seowon-gu, Korea, Republic of, 28644
      • Chungbuk National University Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

1. Healthy adult volunteers aged 19 years or older at screening

2. Individuals with a weight of 50.0 kg or more and a body mass index (BMI) of 18.0 kg/m2 to 30.0 kg/m2 at screening

   • BMI (kg/m2) = Weight (kg) / {Height (m)}2
3. ndividuals without congenital or chronic diseases requiring treatment and with no pathological symptoms or findings from internal medical examinations (if necessary, brain waves, electrocardiograms, chest and upper gastrointestinal endoscopy or gastrointestinal radiographic examinations)
4. Individuals deemed suitable for the clinical trial based on clinical trial laboratory tests, vitality signs, physical examinations, and 12-lead electrocardiogram results conducted according to the characteristics of the investigational product at screening
5. Individuals with negative H. pylori antibody results at screening
6. Individuals who have heard a detailed explanation of the clinical trial, fully understand it, voluntarily decide to participate, and agree in writing to comply with the subject compliance requirements during the clinical trial period

Exclusion Criteria:

1. Individuals with a current or past medical history of clinically significant conditions affecting the liver, kidneys, nervous system, psychiatric system, respiratory system, endocrine system, hematologic disorders, tumors, genitourinary system, cardiovascular system, digestive system, musculoskeletal system, or any of the following current or past conditions:

   • Renal impairment

     • Hepatic impairment
2. Individuals with a history of gastrointestinal disorders (such as Crohn's disease, ulcers, acute or chronic pancreatitis) or gastrointestinal surgery (excluding simple appendectomy or hernia repair) that may affect the absorption of investigational drugs
3. Women who are pregnant (as indicated by positive Urine-HCG) or lactating
4. Individuals with a history of hypersensitivity reactions (such as anaphylaxis or angioedema) or clinically significant hypersensitivity reactions to drugs containing Ilaprazole, excipients (Tartrazine, Sunset Yellow FCF), or other drugs (such as aspirin, penicillin antibiotics, macrolide antibiotics)

5. Individuals with clinically significant findings, including the following, on the 12-lead electrocardiogram performed at screening:

   • QTc > 450 ms for males or QTc > 470 ms for females
   • PR interval > 200 ms
   • QRS duration > 120 ms

6. Individuals with clinically significant results, including the following, on clinical trial laboratory tests performed at screening:

   • AST, ALT, ALP, γ-GT, and total bilirubin levels exceeding twice the upper limit of the normal range for liver function evaluation
   • Serum creatinine levels outside the reference range or estimated glomerular filtration rate (eGFR) calculated by CKD-EPI formula < 60 mL/min/1.73m2
7. Individuals with a history of drug abuse or positive urine drug test results for abused drugs
8. Individuals with systolic blood pressure ≥ 150 mmHg or ≤ 90 mmHg, or diastolic blood pressure ≥ 100 mmHg or ≤ 60 mmHg, or heart rate ≤ 40 bpm or ≥ 100 bpm upon measurement in the supine position after resting for more than 3 minutes at screening
9. Individuals with abnormal diets that may affect the absorption, distribution, metabolism, and excretion of investigational drugs or affect drug metabolism
10. Individuals who have taken any prescription drugs or herbal medicines that may affect the characteristics of investigational drugs within 2 weeks prior to the first dosing day or any over-the-counter drugs or vitamin supplements within 10 days prior to the first dosing day (however, participation in the clinical trial may be allowed based on the participant's judgment if the drug does not affect the pharmacokinetic properties of the investigational drug)
11. Individuals who have been administered inducers or inhibitors of drug metabolism, such as barbiturates, within 1 month prior to the first dosing day
12. Individuals who have participated in another clinical trial and received treatment within 6 months prior to the first dosing day (however, the end date of participation in another clinical trial is calculated as 1 day after the last dosing day)
13. Individuals who have donated whole blood within 2 months or component blood within 1 month prior to the first dosing day, received blood transfusions within 1 month, or cannot abstain from blood donation from the time of written consent until PSV
14. Individuals who have consumed alcohol excessively (more than 21 units/week, 1 unit = 10 g = 12.5 mL of pure alcohol) within 6 months prior to the first dosing day or cannot abstain from the time of written consent until PSV
15. Individuals who have consumed grapefruit-containing foods from 48 hours before the first dosing to PSV or cannot abstain from consumption
16. Individuals who have engaged in vigorous exercise exceeding their usual daily activities from 48 hours before the first dosing to PSV or cannot abstain from such exercise
17. Individuals who, from the time of written consent until 2 weeks after the last dosing day based on the date of the last administration of investigational drugs, are not using or planning to use recognized contraceptive methods for planning or not planning pregnancy (e.g., contraceptive pills and implants, intrauterine devices, infertility procedures (vasectomy, tubal ligation), barrier methods (combined use of spermicides with condoms, vaginal sponges, cervical caps))
18. Individuals for whom insertion and maintenance of a pH meter catheter for gastric pH measurement is difficult
19. Individuals who are deemed unsuitable for participation in the clinical trial by the investigator for reasons other than the selection/exclusion criteria mentioned above.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: A group; Period 1 : Ilaprazole 10mg 2Tab, one a day Period 2 : IY-NS250 1Tab, one a day	Drug: IY-NS250; Ilaprazole 20mg + Sodium bicarbonate 500mg; Drug: IY-NT-SR; Ilaprazole 10mg; Other Names: Noltec(the brand name)
Active Comparator: B group; Period 1 : IY-NS250 1Tab, one a day Period 2 : Ilaprazole 10mg 2Tab, one a day	Drug: IY-NS250; Ilaprazole 20mg + Sodium bicarbonate 500mg; Drug: IY-NT-SR; Ilaprazole 10mg; Other Names: Noltec(the brand name)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Ilaprazole AUCτ,ss	Ilaprazole AUCτ,ss	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
integrated gastric acidity	Percentage decrease in integrated gastric acidity over 24 hours from Day -1 to Day 7	Day -1 -24hour ~ 0h Day7 Predose(0hour) ~ 24hour

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUCinf,ss	AUCinf,ss, of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Cmax,ss	Cmax,ss of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Cmin,ss	Cmin,ss of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Cav,ss	Cav,ss of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Tmax,ss	Tmax,ss of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
t1/2,ss	t1/2,ss of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
CLss/F	CLss/F of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Vss/F, R (accumulation ratio)	Vss/F, R (accumulation ratio) of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
PTF (Peak to Trough fluctuation)	PTF (Peak to Trough fluctuation) of Ilaprazole after repeated administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour / Day 5, Day 6 Predose(0hour) / Day 7 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Cmax	Cmax of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
AUClast	AUClast of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
AUCinf	AUCinf of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Tmax	Tmax of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
t1/2	t1/2 of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
CL/F	CL/F of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
Vz/F	Vz/F of Ilaprazole after single administration	Day 1 Predose(0hour), after dose 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 hour
integrated gastric acidity	Percentage decrease in integrated gastric acidity at different time points from Day -1 to Day 1 and Day 7	Day -1 -24hour ~ 0h Day 1 Predose(0hour) ~ 24h Day7 Predose(0hour) ~ 24hour
nocturnal acid breakthrough (NAB)	Percentage of subjects experiencing nocturnal acid breakthrough (NAB) on Day -1, Day 1, and Day 7, defined as maintaining a pH below 4 for more than 60 consecutive minutes during nighttime (supine position)	Day -1 -24hour ~ 0h Day 1 Predose(0hour) ~ 24h Day7 Predose(0hour) ~ 24hour

Collaborators and Investigators

• Sponsor: Il-Yang Pharm. Co., Ltd.
• Investigators: Principal Investigator: Min Kyu Park, MD, PhD, Chungbuk National University Hospital

Study record dates

Study Major Dates

• Study Start (Actual): January 30, 2024
• Primary Completion (Actual): April 13, 2024
• Study Completion (Actual): August 14, 2024

Study Registration Dates

• First Submitted: February 21, 2024
• First Submitted That Met QC Criteria: December 8, 2024
• First Posted (Estimated): December 10, 2024

Study Record Updates

• Last Update Posted (Estimated): December 10, 2024
• Last Update Submitted That Met QC Criteria: December 8, 2024
• Last Verified: December 1, 2024

More Information

Terms related to this study

• Other Study ID Numbers: IY-NS250SB

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No