Effect of Cimetidine on the Pharmacokinetics of Lucerastat in Healthy Subjects

Phase 1

Completed

• Conditions: Healthy Subjects
• Interventions: Drug: Lucerastat; Drug: Cimetidine

• Registration Number: NCT03380455
• Lead Sponsor: Idorsia Pharmaceuticals Ltd.

Brief Summary

A study in healthy male subjects to investigate whether repeated administrations of cimetidine (a medication which decreases the amount of acid in the stomach) can affect the fate in the body (amount and time of presence in the blood) of lucerastat. Safety of the concomitant administration of the two treatments will also be assessed.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2017-12-15
• Study First Submitted QC: 2017-12-15
• Study First Posted: 2017-12-21
• Study Start: 2018-01-09
• Primary Completion: 2018-01-29
• Study Completion: 2018-01-29
• Status Verified: 2022-06
• Last Update Submitted: 2022-06-01
• Last Update Posted: 2022-06-02

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 14

Inclusion Criteria

• Signed informed consent in the local language prior to any study-mandated procedure.
• Body mass index from 18.0 to 30.0 kg/m2 (inclusive) at Screening.
• Normal renal function confirmed by creatinine clearance ≥ 80 mL/min using Cockroft-Gault formula at Screening.

Exclusion Criteria

• Known hypersensitivity to cimetidine, lucerastat, or drugs of the same class, or any of their excipients.
• History or clinical evidence of any disease and/or existence of any surgical or medical condition, which might interfere with the absorption, distribution, metabolism, or excretion of the study treatment(s) (appendectomy and herniotomy allowed, cholecystectomy not allowed).
• Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
Treatment period A & B	Lucerastat	Treatment period A: Subjects receive a single oral dose of 500 mg lucerastat on Day 1 under fasted conditions. Treatment period B: From Day 3 to Day 9, subjects receive a b.i.d. (every 12 h) oral dose of 800 mg cimetidine under fasted conditions (Treatment period B1; from Day 3 to Day 5). On Day 6, subjects receive a single oral dose of 500 mg lucerastat concomitantly with the morning dose of 800 mg cimetidine under fasted conditions (Treatment period B2; from Day 6 to Day 10).
Treatment period A & B	Cimetidine	Treatment period A: Subjects receive a single oral dose of 500 mg lucerastat on Day 1 under fasted conditions. Treatment period B: From Day 3 to Day 9, subjects receive a b.i.d. (every 12 h) oral dose of 800 mg cimetidine under fasted conditions (Treatment period B1; from Day 3 to Day 5). On Day 6, subjects receive a single oral dose of 500 mg lucerastat concomitantly with the morning dose of 800 mg cimetidine under fasted conditions (Treatment period B2; from Day 6 to Day 10).

Primary Outcome Measures

Name	Time	Method
Cmax of lucerastat	Up to 48 h after lucerastat administration on Day 1 (i.e., up to Day 3) and from pre-dose up to 96 h after lucerastat administration on Day 6 (i.e., up to Day 10); in total for up to 7 days	Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine
T1/2 of lucerastat	Up to 48 h after lucerastat administration on Day 1 (i.e., up to Day 3) and from pre-dose up to 96 h after lucerastat administration on Day 6 (i.e., up to Day 10); in total for up to 7 days	Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine
AUC(0-t) of lucerastat	Up to 48 h after lucerastat administration on Day 1 (i.e., up to Day 3) and from pre-dose up to 96 h after lucerastat administration on Day 6 (i.e., up to Day 10); in total for up to 7 days	Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine
AUC(0-inf) of lucerastat	Up to 48 h after lucerastat administration on Day 1 (i.e., up to Day 3) and from pre-dose up to 96 h after lucerastat administration on Day 6 (i.e., up to Day 10); in total for up to 7 days	Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine
AUC(0-48) of lucerastat	Up to 48 h after lucerastat administration on Day 1 (i.e., up to Day 3) and from pre-dose up to 96 h after lucerastat administration on Day 6 (i.e., up to Day 10); in total for up to 7 days	Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine
Tmax of lucerastat	Up to 48 h after lucerastat administration on Day 1 (i.e., up to Day 3) and from pre-dose up to 96 h after lucerastat administration on Day 6 (i.e., up to Day 10); in total for up to 7 days	Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine

Secondary Outcome Measures

Name	Time	Method
Number of treatment-emergent SAEs	From Screening to safety follow-up, i.e., 32 days after End-of-Study (for up to 63 days)
Number of treatment-emergent AEs	From Day 1 to End-of-Study (for up to 13 days)

Trial Locations

Locations (1)

CRS Clinical Research Services Kiel GmbH; 🇩🇪 Kiel, Germany