Investigate Linaprazan Glurate/Linaprazan in Healthy Subjects

Phase 1

Completed

• Conditions: GERD
• Interventions: Drug: linaprazan glurate 25 mg QD; Drug: linaprazan glurate 50 mg QD; Drug: linaprazan glurate 75 mg QD; Drug: linaprazan glurate 25 mg BID; Drug: linaprazan glurate 50 mg BID; Drug: linaprazan glurate 75 mg BID

• Registration Number: NCT05742984
• Lead Sponsor: Cinclus Pharma Holding AB

Brief Summary

This is a Phase I, single-center, open label parallel-group, randomized study designed to evaluate the pharmacokinetics (PK), pharmacodynamics (PD, by continuous intragastric pH measurment), safety and tolerability of single and repeated oral doses of linaprazan glurate in 3 different dose levels given once- (QD) or twice daily (BID), for 14 days, with an additional single dose after 2, 4 or 6 days of drug holiday. The population will include healthy male and female subjects.

The subjects will be followed up to 28 days post IMP dosing.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2023-01-02
• Study Start: 2023-01-26
• Study First Submitted QC: 2023-02-23
• Study First Posted: 2023-02-24
• Primary Completion: 2023-03-24
• Study Completion: 2023-04-13
• Results First Submitted: 2024-08-26
• Status Verified: 2025-05
• Results First Submitted QC: 2025-05-06
• Last Update Submitted: 2025-05-06
• Results First Posted: 2025-05-07
• Last Update Posted: 2025-05-07

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 75

Inclusion Criteria

1. Willing and able to give written informed consent for participation in the study.
2. Healthy male or female subject aged 18 to 65 years, inclusive.
3. Body mass index ≥ 18.5 and ≤ 30.0 kg/m2.
4. Medically healthy, without abnormal clinically significant medical history, physical findings, vital signs, ECGs, or laboratory values at the time of screening, as judged by the Investigator.

Exclusion Criteria

1. Female subjects of childbearing potential (defined as all subjects physiologically capable of becoming pregnant)
2. Male subjects with a partner of childbearing potential
3. History of any clinically significant disease or disorder which, in the opinion of the Investigator, may either put the subject at risk because of participation in the study, or influence the results or the subject's ability to participate in the study.
4. History of GERD or clinically significant acid reflux, as judged by the Investigator.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Group 1: 25 mg linaprazan glurate QD	linaprazan glurate 25 mg QD	25 mg (one 25 mg oral tablet) linaprazan glurate once daily (QD) for 14 days
Group 2: 50 mg Linaprazan Glurate QD	linaprazan glurate 50 mg QD	50 mg (two 25 mg oral tablets) linaprazan glurate once daily (QD) for 14 days
Group 3: 75 mg Linaprazan Glurate QD	linaprazan glurate 75 mg QD	75 mg (three 25 mg oral tablet) linaprazan glurate once daily (QD) for 14 days
Group 4: 25 mg Linaprazan Glurate BID	linaprazan glurate 25 mg BID	25 mg (one 25mg oral tablet) linaprazan glurate twice daily (BID) for 14 days
Group 5: 50 mg Linaprazan Glurate BID	linaprazan glurate 50 mg BID	50 mg (two 25 mg oral tablets) linaprazan glurate twice daily (BID) for 14 days
Group 6: 75 mg Linaprazan Glurate BID	linaprazan glurate 75 mg BID	75 mg (three 25 mg oral tablet) linaprazan glurate twice daily (BID) for 14 days

Primary Outcome Measures

Name	Time	Method
AUC0-24h Linaprazan (QD)	Day 1 and Day 14	Linaprazan area under the plasma concentration curve, from 0 to 24h post dose on Day 1 and Day 14. QD groups only.
AUC0-24h Linaprazan Glurate (QD)	Day 1 and day 14	Linaprazan glurate area under the plasma concentration curve, from 0-24h post dose on Day 1 and Day 14. QD groups only.
AUC0-12, 12-24h Linaprazan (BID)	Day 1 and Day 14	Linaprazan area under the plasma concentration curve, from 0 to 12h and 12-24h post dose on Day 1 and Day 14. BID groups only.
Cmax Linaprazan (QD)	Day 1 and day 14	Linaprazan maximum plasma concentration 0-24h post dose for QD groups, at day 1 and day 14.
Cmax Linaprazan (BID)	Day 1 and day 14	Linaprazan maximum plasma concentration 0-12h, and 12-24h post dose for BID groups, at day 1 and day 14.
AUC0-12h, 12-24h Linaprazan Glurate (BID)	Day 1 and Day 14	Linaprazan glurate area under the plasma concentration curve, from 0 to 12h and 12-24h post dose on Day 1 and Day 14. BID groups only.
Cmax Linaprazan Glurate (QD)	Day 1 and day 14	Linaprazan glurate maximum plasma concentration 0-24h post dose for QD groups, at day 1 and day 14.
Cmax Linaprazan Glurate (BID)	Day 1 and day 14	Linaprazan glurate maximum plasma concentration 0-12h and 12-24h post dose for BID groups, at day 1 and day 14.
Percentage of Time Gastric pH >4 Over a 24-hour Monitoring Period (Holding Time Ratio, HTR)	Day 1 and day 14	Percentage of time gastric pH \>4 at Days 1 and 14 over a 24-hour monitoring period following linaprazan glurate administration.; Intragastric pH was measured every second with an intragastric probe. The measurements were compressed into 10-minute median intervalls before calculating the % of time with intragastric \>pH 4 (HTR). The HTR is presented with descriptive statistics, by dosing group.

Trial Locations

Locations (1)

CRS d.o.o,Ukmarjeva ulica 6; 🇸🇮 Ljubljana, Slovenia