A Study to Investigate the Pharmacokinetics and ECG Effects of Linaprazan Glurate

A Phase I Study to Investigate the Pharmacokinetics and ECG Effects of Two Single Ascending Doses of Linaprazan Glurate Given as Oral Tablets to Healthy Subjects

This is a Phase I, single-center, double blind, placebo-controlled, parallel-group, randomized study designed to evaluate the PK, cardiodynamic ECG effects, safety, and tolerability of 2 single ascending oral doses of linaprazan glurate. The study will explore the PK properties of linaprazan glurate and linaprazan as well as the cardiodynamic ECG effects, safety, and tolerability after the administration of single doses (300 mg, 600 mg, 200 mg and a final dose level of maximum 400 mg) of linaprazan glurate, using 25 mg base formulation (300 mg and 600 mg doses) and 25 mg and 100 mg HCl formulation (200 mg and final dose level of maximum 400 mg) oral tablets.

Study Overview

• Status: Recruiting
• Conditions: GERD; Pharmacokinetics; Cardiodynamic ECG; Safety, and Tolerability
• Intervention / Treatment: Drug: Linaprazan glurate; Drug: Placebo

• Study Type: Interventional
• Enrollment (Estimated): 113
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Simon Rubinstein, MD, PhD; Phone Number: +44 786 780 70 60; Email: simon.rubinstein@cincluspharma.com

Study Locations

• Sweden
  • Uppsala, Sweden, SE-75237
    • Recruiting
    • CTC Clinical Trial Consultants AB
    • Contact: Måns Jergil, PhD; Phone Number: +4618303300; Email: mans.jergil@ctc-ab.se
    • Principal Investigator: Erik Rein-Hedin, MD

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

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
3. Body mass index ≥18.5 and ≤35.0 kg/m2.
4. Prospective subjects, as well as their partners, must agree to contraception requirements

Main 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: Parallel Assignment
• Masking: Quadruple

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo; Oral administration as a singel dose	Drug: Placebo; Single dose, oral tablets
Experimental: Linaprazan glurate; Oral administration as a single dose of 300 mg, 600 mg, 200 mg, and a final dose level of maximum 400 mg.	Drug: Linaprazan glurate; Linaprazan glurate base formulation, 25 mg oral tablets (300 mg and 600 mg doses). Linaprazan glurate hydrochloride (HCl), 25 mg and 100 mg (as base) oral tablets (200 mg and final dose level of maximum 400 mg).; Other Names: 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)	To assess the Area under the plasma concentration vs. time curve (AUC) from time 0 to infinity (AUCinf)	Up to 24 hours
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (AUClast)	To assess the AUC from time 0 to the last measurable concentration (AUClast)	Up to 24 hours
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (Cmax)	To assess the Maximum plasma concentration (Cmax)	Up to 24 hours
Measurement of pharmacokinetic profile of linprazan glurate and linaprazan (T1/2)	To assess the Terminal elimination half-life (T1/2)	Up to 24 hours
Measurement of Cardiodynamic ECG (QTcF)	To assess the change from baseline in QTcF	Up to 24 hours
Measurement of Cardiodynamic ECG (heart rate)	To assess the change from baseline in heart rate	Up to 24 hours
Measurement of Cardiodynamic ECG (PR interval)	To assess the change from baseline in PR interval	Up to 24 hours
Measurement of Cardiodynamic ECG (QRS interval)	To assess the change from baseline in QRS interval	Up to 24 hours
Measurement of Cardiodynamic ECG (placebo-corrected QTcF)	To assess the change from baseline in placebo-corrected QTcF	Up to 24 hours
Measurement of Cardiodynamic ECG (placebo-corrected heart rate)	To assess the change from baseline in placebo-corrected heart rate	Up to 24 hours
Measurement of Cardiodynamic ECG (placebo-corrected PR interval)	To assess the change from baseline in placebo-corrected PR interval	Up to 24 hours
Measurement of Cardiodynamic ECG (placebo-corrected QRS interval)	To assess the change from baseline in placebo-corrected QRS interval	Up to 24 hours
Measurement of Cardiodynamic ECG (categorical outliers)	Number of categorical outliers for ECG parameters (QTcF, HR, PR interval, QRS interval)	Up to 24 hours
Measurement of Cardiodynamic ECG (changes of T-wave)	Frequency of treatment emergent changes of T-wave abnormalities	Up to 24 hours
Measurement of Cardiodynamic ECG (changes of U-wave)	Frequency of treatment emergent changes of U-wave abnormalities	Up to 24 hours

Collaborators and Investigators

• Sponsor: Cinclus Pharma AG
• Investigators: Principal Investigator: Erik Rein-Hedin, MD, CTC Clinical Trial Consultants AB

Study record dates

Study Major Dates

• Study Start (Actual): July 13, 2022
• Primary Completion (Estimated): December 2, 2024
• Study Completion (Estimated): December 2, 2024

Study Registration Dates

• First Submitted: July 15, 2022
• First Submitted That Met QC Criteria: July 19, 2022
• First Posted (Actual): July 22, 2022

Study Record Updates

• Last Update Posted (Estimated): February 7, 2024
• Last Update Submitted That Met QC Criteria: February 6, 2024
• Last Verified: February 1, 2024

More Information

Terms related to this study

• Other Study ID Numbers: CX842A2104

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No