Phase 1
Completed N=67
Relative Bioavailability of Linaprazan for the Test Formulation vs. Reference Formulation
Safety · Bioavailability · Pharmacokinetics
Source: ClinicalTrials.gov NCT05627518 ↗
Enrolled (actual)
67
Serious AEs
0.6%
Results posted
Apr 2025
Primary outcomePrimary: Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratios of AUCinf and AUClast — 12341; 25001; 10016.2; 24175.8 hours * nmol/Liter — p=<0.0001
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratios of AUCinf and AUClast |
12341; 25001; 10016.2; 24175.8 | <0.0001 sig |
| PRIMARY Relative Bioavailability of Linaprazan Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax |
1430; 3462.2 | <0.0001 sig |
| PRIMARY Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf and AUClast |
25001; 19448.9; 24175.8; 19022.8 | <0.0001 sig |
| PRIMARY Relative Bioavailability of Linaprazan Test Formulation in Fed vs. Fasting Conditions, Based on the Means Ratios for Cmax |
3462.2; 1608 | <0.0001 sig |
| SECONDARY Relative Bioavailability of Linaprazan Glurate for the Test Formulation vs. Reference Formulation of Linaprazan Glurate, Based on the Means Ratios of PK Parameters. |
114.2; 320.2; 83.9; 293 | <0.0001 sig |
| SECONDARY Relative Bioavailability of Linaprazan Glurate Comparing Test Formulation vs. Reference Formulation of Linaprazan Glurate. Ratio of Cmax |
86.8; 214.3 | <0.0001 sig |
| SECONDARY Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratios for AUCinf, AUClast |
320.2; 166.3; 293.0; 144.3 | <0.0001 sig |
| SECONDARY Relative Bioavailability of Linaprazan Glurate in Fed vs. Fasting Conditions, Based on the Means Ratio of Cmax |
214.3; 55.0 | <0.0001 sig |
Eligibility Criteria
Main Inclusion Criteria:
- 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
Exclusion Criteria
- 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).
Data sourced from ClinicalTrials.gov (NCT05627518). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.