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

NCT05627518 | Completed Phase 1 Results

• 1 other identifier: CX842A2106
• Study Type: interventional
• Target: 67
• Locations: 1 country
• Sites: 1

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.

Conditions

Safety; Bioavailability; Pharmacokinetics

Outcome Measures

Primary Outcomes (4)

• Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratios of AUCinf and AUClast

  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.

  From pre-dose up to 72 h post dose

• Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax

  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.

  From pre-dose up to 72 h post dose

• Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf and AUClast

  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.

  From pre-dose up to 72 h post dose

• Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for Cmax

  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.

  From pre-dose up to 72 h post dose

Secondary Outcomes (4)

• 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

• 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

• 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

• 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

Study Arms (3)

Reference formulation (Treatment A)

ACTIVE COMPARATOR

100 mg linaprazan glurate reference formulation (4x25 mg oral tablets) in fasting conditions

Drug: Linaprazan glurate

Test formulation (Treatment B)

EXPERIMENTAL

100 mg linaprazan glurate test formulation (1x100 mg oral tablet) in fasting conditions

Drug: Linaprazan glurate

Test Formulation (Treatment C)

EXPERIMENTAL

100 mg linaprazan glurate test formulation (1x100 mg oral tablet) in fed conditions

Drug: Linaprazan glurate

Interventions

Linaprazan glurate DRUG

100 mg

Also known as: formerly X842

Reference formulation (Treatment A); Test Formulation (Treatment C); Test formulation (Treatment B)

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 aged 18 to 65 years, inclusive.
• Body mass index ≥18.5 and ≤30.0 kg/m2.
• Medically healthy, without abnormal clinically significant medical history
• Female subjects of childbearing potential, as well as their partners and male subjects and their partners, who agree to using methods of contraception
• Willing and able to consume the high-fat, high calorie breakfast

You may not qualify if:

• 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.
• 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
• History of or current clinically significant disease as defined in the protocol.
• History of GERD, significant acid reflux.
• 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).

Sponsors & Collaborators

• Cinclus Pharma Holding AB: lead

Study Sites (1)

CRS d.o.o.

Ljubljana, Ukmarjeva Ulica 6, 1000, Slovenia

Location

Results Point of Contact

• Title: Kristofer Katkits Nilsson, Global Trial Manager
• Organization: Cinclus Pharma AB

kristofer.katkits@cincluspharma.com

+46 7064955

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: LTE60
• Restrictive Agreement: Yes

Study Design

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

Study Record Dates

• First Submitted: November 16, 2022
• First Posted: November 25, 2022
• Study Start: November 15, 2022
• Primary Completion: December 30, 2022
• Study Completion: January 3, 2023
• Last Updated: April 3, 2025
• Results First Posted: April 3, 2025

Record last verified: 2025-02

Data Sharing

• IPD Sharing: Will not share

Locations

SL (1)