Relative Bioavailability of Linaprazan for the Test Formulation vs. Reference Formulation

Phase 1

Completed

• Conditions: Safety; Pharmacokinetics; Bioavailability
• Interventions: Drug: Linaprazan glurate

• Registration Number: NCT05627518
• Lead Sponsor: Cinclus Pharma Holding AB

Brief Summary

This is a single-center, open-label, randomized, single dose, 3-way crossover study in healthy volunteers designed to evaluate the relative bioavailability of a new oral tablet formulation of linaprazan glurate in comparison to a previously studied oral tablet formulation under fasting conditions, and to assess the effect of a high fat, high calorie meal on the pharmacokinetics (PK) of linaprazan glurate and the active substance linaprazan after the administration of the new oral tablet formulation.

Detailed Description

Not available

Study Timeline

• Study Start: 2022-11-15
• Study First Submitted: 2022-11-16
• Study First Submitted QC: 2022-11-16
• Study First Posted: 2022-11-25
• Primary Completion: 2022-12-30
• Study Completion: 2023-01-03
• Results First Submitted: 2024-04-16
• Status Verified: 2025-02
• Results First Submitted QC: 2025-03-17
• Last Update Submitted: 2025-03-17
• Results First Posted: 2025-04-03
• Last Update Posted: 2025-04-03

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 67

Inclusion Criteria

1. Willing and able to give written informed consent for participation in the study.
2. Healthy male or female 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
5. Female subjects of childbearing potential, as well as their partners and male subjects and their partners, who agree to using methods of contraception
6. Willing and able to consume the high-fat, high calorie breakfast

Exclusion Criteria

1. Female subjects of childbearing potential unless they agree to use highly effective methods of contraception (failure rate of <1%) from 2 weeks prior to dosing until the end-of-study visit.
2. Male subjects with a partner of childbearing potential, unless they agree to use method of contraception from 2 weeks prior to dosing until the end-of-study visit.History of or current clinically significant disease as defined in the protocol
3. History of or current clinically significant disease as defined in the protocol.
4. History of GERD, significant acid reflux.
5. Subjects who are pregnant, currently breastfeeding, or intend to become pregnant (female subjects) or father a child (male subjects) during the course of the study (i.e., from screening to end of study visit).

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Reference formulation (Treatment A)	Linaprazan glurate	100 mg linaprazan glurate reference formulation (4x25 mg oral tablets) in fasting conditions
Test formulation (Treatment B)	Linaprazan glurate	100 mg linaprazan glurate test formulation (1x100 mg oral tablet) in fasting conditions
Test Formulation (Treatment C)	Linaprazan glurate	100 mg linaprazan glurate test formulation (1x100 mg oral tablet) in fed conditions

Primary Outcome Measures

Name	Time	Method
Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratios of AUCinf and AUClast	From pre-dose up to 72 h post dose	The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan, comparing test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased with the new formulation.
Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax	From pre-dose up to 72 h post dose	The Ratio of Cmax (highest measured concentration) of linaprazan comparing the test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased with the new formulation.
Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf and AUClast	From pre-dose up to 72 h post dose	The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan, comparing test formulation vs reference formulation (treatments C vs treatment B) for Relative Bioavailability, i.e. how much linaprazan exposure is increased or decreased in a fed vs fasted state.
Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for Cmax	From pre-dose up to 72 h post dose	The Ratio of Cmax of linaprazan when comparing test formulation vs reference formulation (treatments C vs treatment B), i.e. how much linaprazan exposure is increased or decreased with the new formulation.

Secondary Outcome Measures

Name	Time	Method
Relative Bioavailability of Linaprazan Glurate for the Test Formulation vs. Reference Formulation of Linaprazan Glurate, Based on the Means Ratios of PK Parameters.	From pre-dose up to 72 h post dose	The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprzan glurate, comparing test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation.
Relative Bioavailability of Linaprazan Glurate Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax	From pre-dose up to 72 h post dose	The Ratio of Cmax (highest measured concentration) of linaprazan glurate comparing the test formulation vs reference formulation (treatments B vs treatment A) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation.
Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf, AUClast	From pre-dose up to 72 h post dose	The Ratio of Area Under the plasma concentration vs. time Curve (AUC) from time 0 to infinity (AUCinf), and from time 0 to last measurement (AUClast) of linaprazan glurate, comparing test formulation vs reference formulation (treatments C vs treatment B) for Relative Bioavailability, i.e. how much linaprazan glurate exposure is increased or decreased in a fed vs fasted state.
Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratio of Cmax	From pre-dose up to 72 h post dose	The Ratio of Cmax of linaprazan glurate when comparing test formulation vs reference formulation (treatments C vs treatment B), i.e. how much linaprazan glurate exposure is increased or decreased with the new formulation.

Trial Locations

Locations (1)

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