Investigate Linaprazan Glurate/Linaprazan in Healthy Subjects

NCT05742984 | Completed Phase 1 Results

• 1 other identifier: CX842A2107
• Study Type: interventional
• Target: 75
• Locations: 1 country
• Sites: 1

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.

Conditions

GERD

Outcome Measures

Primary Outcomes (9)

• AUC0-24h Linaprazan (QD)

  Linaprazan area under the plasma concentration curve, from 0 to 24h post dose on Day 1 and Day 14. QD groups only.

  Day 1 and Day 14

• AUC0-12, 12-24h Linaprazan (BID)

  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.

  Day 1 and Day 14

• Cmax Linaprazan (QD)

  Linaprazan maximum plasma concentration 0-24h post dose for QD groups, at day 1 and day 14.

  Day 1 and day 14

• Cmax Linaprazan (BID)

  Linaprazan maximum plasma concentration 0-12h, and 12-24h post dose for BID groups, at day 1 and day 14.

  Day 1 and day 14

• AUC0-24h Linaprazan Glurate (QD)

  Linaprazan glurate area under the plasma concentration curve, from 0-24h post dose on Day 1 and Day 14. QD groups only.

  Day 1 and day 14

• AUC0-12h, 12-24h Linaprazan Glurate (BID)

  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.

  Day 1 and Day 14

• Cmax Linaprazan Glurate (QD)

  Linaprazan glurate maximum plasma concentration 0-24h post dose for QD groups, at day 1 and day 14.

  Day 1 and day 14

• Cmax Linaprazan Glurate (BID)

  Linaprazan glurate maximum plasma concentration 0-12h and 12-24h post dose for BID groups, at day 1 and day 14.

  Day 1 and day 14

• Percentage of Time Gastric pH >4 Over a 24-hour Monitoring Period (Holding Time Ratio, HTR)

  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.

  Day 1 and day 14

Study Arms (6)

Group 1: 25 mg linaprazan glurate QD

EXPERIMENTAL

25 mg (one 25 mg oral tablet) linaprazan glurate once daily (QD) for 14 days

Drug: linaprazan glurate 25 mg QD

Group 2: 50 mg Linaprazan Glurate QD

EXPERIMENTAL

50 mg (two 25 mg oral tablets) linaprazan glurate once daily (QD) for 14 days

Drug: linaprazan glurate 50 mg QD

Group 3: 75 mg Linaprazan Glurate QD

EXPERIMENTAL

75 mg (three 25 mg oral tablet) linaprazan glurate once daily (QD) for 14 days

Drug: linaprazan glurate 75 mg QD

Group 4: 25 mg Linaprazan Glurate BID

EXPERIMENTAL

25 mg (one 25mg oral tablet) linaprazan glurate twice daily (BID) for 14 days

Drug: linaprazan glurate 25 mg BID

Group 5: 50 mg Linaprazan Glurate BID

EXPERIMENTAL

50 mg (two 25 mg oral tablets) linaprazan glurate twice daily (BID) for 14 days

Drug: linaprazan glurate 50 mg BID

Group 6: 75 mg Linaprazan Glurate BID

EXPERIMENTAL

75 mg (three 25 mg oral tablet) linaprazan glurate twice daily (BID) for 14 days

Drug: linaprazan glurate 75 mg BID

Interventions

linaprazan glurate 25 mg QD DRUG

The subjects will receive 25 mg dose in the evening, in a non-fasted condition 30 minutes after the evening meal, for 14 days. Subjects are to follow a standardized food intake schedule. After a drug holiday period of either 2, 4 or 6 days, linaprazan glurate will be given once more in the evening (non-fasted).

Group 1: 25 mg linaprazan glurate QD

linaprazan glurate 50 mg QD DRUG

The subjects will receive 50 mg dose in the evening, in a non-fasted condition 30 minutes after the evening meal, for 14 days. Subjects are to follow a standardized food intake schedule. After a drug holiday period of either 2, 4 or 6 days, linaprazan glurate will be given once more in the evening (non-fasted).

Group 2: 50 mg Linaprazan Glurate QD

linaprazan glurate 75 mg QD DRUG

The subjects will receive 75 mg dose in the evening, in a non-fasted condition 30 minutes after the evening meal, for 14 days. Subjects are to follow a standardized food intake schedule. After a drug holiday period of either 2, 4 or 6 days, linaprazan glurate will be given once more in the evening (non-fasted).

Group 3: 75 mg Linaprazan Glurate QD

linaprazan glurate 25 mg BID DRUG

The subjects will receive 25 mg dose twice daily, in the morning and in the evening for 14 days. Subjects will be fasted for ≥10 hours overnight before dosing on Day 1 and day 14, until 30 minutes post-dose. During fasting, tap water, but no other drinks, are allowed as desired, except for 1 hour before and 30 minutes after dosing. The second daily dose will be administered 30 minutes after the evening meal, i.e. in a non-fasted condition. The subjects are to follow a standardized food intake schedule. After a drug holiday period of either 2, 4 or 6 days, linaprazan glurate will be given once more (in fasted condition in the morning, non-fasted in the evening).

Group 4: 25 mg Linaprazan Glurate BID

linaprazan glurate 50 mg BID DRUG

The subjects will receive 50 mg dose twice daily, in the morning and in the evening for 14 days. Subjects will be fasted for ≥10 hours overnight before dosing on Day 1 and day 14, until 30 minutes post-dose. During fasting, tap water, but no other drinks, are allowed as desired, except for 1 hour before and 30 minutes after dosing. The second daily dose will be administered 30 minutes after the evening meal, i.e. in a non-fasted condition. The subjects are to follow a standardized food intake schedule. After a drug holiday period of either 2, 4 or 6 days, linaprazan glurate will be given once more (in fasted condition in the morning, non-fasted in the evening).

Group 5: 50 mg Linaprazan Glurate BID

linaprazan glurate 75 mg BID DRUG

The subjects will receive 75 mg dose twice daily, in the morning and in the evening for 14 days. Subjects will be fasted for ≥10 hours overnight before dosing on Day 1 and day 14, until 30 minutes post-dose. During fasting, tap water, but no other drinks, are allowed as desired, except for 1 hour before and 30 minutes after dosing. The second daily dose will be administered 30 minutes after the evening meal, i.e. in a non-fasted condition. The subjects are to follow a standardized food intake schedule. After a drug holiday period of either 2, 4 or 6 days, linaprazan glurate will be given once more (in fasted condition in the morning, non-fasted in the evening).

Group 6: 75 mg Linaprazan Glurate BID

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Willing and able to give written informed consent for participation in the study.
• Healthy male or female subject aged 18 to 65 years, inclusive.
• Body mass index ≥ 18.5 and ≤ 30.0 kg/m2.
• 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.

You may not qualify if:

• Female subjects of childbearing potential (defined as all subjects physiologically capable of becoming pregnant)
• Male subjects with a partner of childbearing potential
• 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.
• History of GERD or clinically significant acid reflux, as judged by the Investigator.

Sponsors & Collaborators

• Cinclus Pharma Holding AB: lead

Study Sites (1)

CRS d.o.o,Ukmarjeva ulica 6

Ljubljana, 1000, Slovenia

Location

MeSH Terms

Conditions

Gastroesophageal Reflux

Interventions

BID protein, human

Condition Hierarchy (Ancestors)

Esophageal Motility Disorders; Deglutition Disorders; Esophageal Diseases; Gastrointestinal Diseases; Digestive System Diseases

Results Point of Contact

• Title: Cinclus Pharma Holding AB
• Organization: Cinclus Pharma

gosta.hiller@cincluspharma.com

+46 8 13 33 10

Study Officials

• Tanja Turk, M.Pharm

  CRS d.o.o Ljubljana, Ukmarjeva Ulica 6, Slovenia, 1000 Contact: Tanja Turk, M.pharm +38651619388 tanja.turk@crs.si

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: No

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 2, 2023
• First Posted: February 24, 2023
• Study Start: January 26, 2023
• Primary Completion: March 24, 2023
• Study Completion: April 13, 2023
• Last Updated: May 7, 2025
• Results First Posted: May 7, 2025

Record last verified: 2025-05

Data Sharing

• IPD Sharing: Will not share

Locations

SL (1)