Phase 1
Completed N=35
Effect of Clarithromycin on PK of Linaprazan, Linaprazan on PK of Clarithromycin and Linaprazan on PK of Midazolam
Safety Issues · Pharmacokinetics · Drug Interaction · Tolerability
Source: ClinicalTrials.gov NCT05633147 ↗
Enrolled (actual)
35
Serious AEs
0.0%
Results posted
Jan 2025
Primary outcomePrimary: Period I, Part I - Linaprazan Glurate and Linaprazan PK Parameters With and Without Co-administration of Clarithromycin - AUC0-inf — 13950; 42840; 137.3; 165.9 h*nmol/L
Summary
This is a phase I, open-label, fixed sequence design, drug-drug-interaction (DDI) study divided in 2 parts. Part I is designed to evaluate whether concomitant treatment with linaprazan glurate and clarithromycin, a strong inhibitor of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein P (PgP), leads to an effect on the systemic exposure to linaprazan glurate and linaprazan and whether there is an effect on the pharmacokinetics of clarithromycin after a single dose of linaprazan glurate. Part II is designed to evaluate the effect of repeated doses of linaprazan glurate on the pharmacokinetics (PK) of a sensitive substrate of CYP3A (midazolam).
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Period I, Part I - Linaprazan Glurate and Linaprazan PK Parameters With and Without Co-administration of Clarithromycin - AUC0-inf |
13950; 42840; 137.3; 165.9 | — |
| PRIMARY Period I, Part I - Linaprazan Glurate and Linaprazan PK Parameters With and Without Co-administration of Clarithromycin - AUC0-t |
13870; 39870; 133.6; 160.6 | — |
| PRIMARY Period I, Part I - Linaprazan Glurate and Linaprazan PK Parameters With and Without Co-administration of Clarithromycin - Cmax |
1844; 2742; 131.1; 176.8 | — |
| PRIMARY Period II, Part II- Midazolam PK Parameters in the Presence and Absence of Linaprazan Glurate Administration - AUC0-inf |
38.57; 40.78; 33.06 | — |
| PRIMARY Period II, Part II- Midazolam PK Parameters in the Presence and Absence of Linaprazan Glurate Administration - AUC0-t |
37.12; 39.66; 32.19 | — |
| PRIMARY Period II, Part II- Midazolam PK Parameters in the Presence and Absence of Linaprazan Glurate - Cmax |
12.24; 13.69; 13.53 | — |
Eligibility Criteria
Main Inclusion Criteria:
- Willing and able to give written informed consent for participation in the study.
- Healthy male and female subjects of non-childbearing potential aged 18 to 60 years, inclusive.
- Body mass index ≥ 18.0 and ≤ 30.0 kg/m2.
- Subjects as well as their partners, must agree to contraception requirements. Male subjects must refrain from donating sperm.
Main Exclusion Criteria:
- Have known allergies to any components of the linaprazan glurate formulation, to clarithromycin/midazolam or to any drugs of a similar class including excipients associated with any of the drugs.
- Use of CYP3A4 inhibitors, antacids, PPIs or any medication that changes gastric pH.
- Use of any prescribed or non-prescribed CYP3A4-inducing medication or other metabolic enzyme inducers.
- History of any clinically significant disease or disorder defined in the protocol.
Data sourced from ClinicalTrials.gov (NCT05633147). 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.