Relative Bioavailability of Linaprazan for the Test Formulation vs. Reference Formulation (BA)

A Randomized, Single Dose, Crossover Study in Healthy Volunteers to Investigate the Relative Bioavailability of Linaprazan for a New Oral Tablet Formulation of Linaprazan Glurate, and to Assess the Effect of Food on the Pharmacokinetics of Linaprazan

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.

Study Overview

• Status: Completed
• Conditions: Pharmacokinetics; Bioavailability; Safety
• Intervention / Treatment: Drug: Linaprazan glurate

• Study Type: Interventional
• Enrollment (Actual): 54
• Phase: Phase 1

Contacts and Locations

Study Locations

• Slovenia
  • Ukmarjeva Ulica 6
    • Ljubljana, Ukmarjeva Ulica 6, Slovenia, 1000
      • CRS d.o.o.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Main 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 Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: Reference formulation (Treatment A); 100 mg linaprazan glurate reference formulation, fasting conditions	Drug: Linaprazan glurate; 100 mg; Other Names: formerly X842
Experimental: Test formulation (Treatment B); 100 mg linaprazan glurate reference formulation, fasting conditions	Drug: Linaprazan glurate; 100 mg; Other Names: formerly X842
Experimental: Test Formulation (Treatment C); 100 mg linaprazan glurate test formulation, fed conditions	Drug: Linaprazan glurate; 100 mg; Other Names: formerly X842

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (AUCinf)	Area under the plasma concentration vs. time curve (AUC) from time 0 to infinity (AUCinf)	pre dose, 0,25h, 0,5h, 1h, 1,25h, 1,5h, 2h, 3h, 4h, 6h, 8h, 12h, 14h, 20h, 24h, 36h, 48h and 72 h post dose
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (AUClast)	AUC from time 0 to the last measurable concentration (AUClast)	pre dose, 0,25h, 0,5h, 1h, 1,25h, 1,5h, 2h, 3h, 4h, 6h, 8h, 12h, 14h, 20h, 24h, 36h, 48h and 72 h post dose
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (Cmax)	Maximum plasma concentration (Cmax)	pre dose, 0,25h, 0,5h, 1h, 1,25h, 1,5h, 2h, 3h, 4h, 6h, 8h, 12h, 14h, 20h, 24h, 36h, 48h and 72 h post dose

Collaborators and Investigators

• Sponsor: Cinclus Pharma AG
• Investigators: Study Director: Tanja Turk, M. Pharm, CRS d.o.o.

Study record dates

Study Major Dates

• Study Start (Actual): November 15, 2022
• Primary Completion (Actual): December 30, 2022
• Study Completion (Actual): January 2, 2023

Study Registration Dates

• First Submitted: November 16, 2022
• First Submitted That Met QC Criteria: November 16, 2022
• First Posted (Actual): November 25, 2022

Study Record Updates

• Last Update Posted (Actual): January 18, 2023
• Last Update Submitted That Met QC Criteria: January 17, 2023
• Last Verified: January 1, 2023

More Information

Terms related to this study

• Other Study ID Numbers: CX842A2106

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes