Investigate Linaprazan Glurate/Linaprazan in Healthy Subjects

Cinclus Pharma Holding AB75 enrolled

Overview

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.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

TREATMENT

Masking

NONE

Enrollment

Conditions

GERD

Interventions

linaprazan glurate 25 mg QDDRUG

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).

linaprazan glurate 50 mg QDDRUG

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).

linaprazan glurate 75 mg QDDRUG

Eligibility

Sex: ALLMin age: 18 YearsMax age: 65 YearsHealthy volunteers:

Medical Language ↔ Plain English

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.

Locations (1)

CRS d.o.o,Ukmarjeva ulica 6

Ljubljana, Slovenia

Outcomes

Primary Outcomes

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.

Time frame: 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.

Time frame: 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.

Time frame: 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.

Time frame: 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.

Time frame: 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.

Time frame: 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.

Time frame: 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.

Data from ClinicalTrials.gov

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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).

linaprazan glurate 25 mg BIDDRUG

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).

linaprazan glurate 50 mg BIDDRUG

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).

linaprazan glurate 75 mg BIDDRUG

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).

Time frame: 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.

Time frame: Day 1 and day 14