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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Treatment period A & B | Experimental | 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). |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Lucerastat | Drug | Single oral dose of 500 mg lucerastat under fasted conditions |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax of lucerastat | Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine | 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 |
| Tmax of lucerastat | Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine | 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 |
| AUC(0-t) of lucerastat | Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine | 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 |
| AUC(0-inf) of lucerastat | Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine | 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 |
| AUC(0-48) of lucerastat | Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine | 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 |
| Measure | Description | Time Frame |
|---|---|---|
| Number of treatment-emergent AEs | From Day 1 to End-of-Study (for up to 13 days) | |
| Number of treatment-emergent SAEs | From Screening to safety follow-up, i.e., 32 days after End-of-Study (for up to 63 days) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Marie-Laure Boof, PhD | Idorsia Pharmaceuticals Ltd. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| CRS Clinical Research Services Kiel GmbH | Kiel | 24105 | Germany |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 31836927 | Derived | Boof ML, Halabi A, Ufer M, Dingemanse J. Impact of the organic cation transporter 2 inhibitor cimetidine on the single-dose pharmacokinetics of the glucosylceramide synthase inhibitor lucerastat in healthy subjects. Eur J Clin Pharmacol. 2020 Mar;76(3):431-437. doi: 10.1007/s00228-019-02808-9. Epub 2019 Dec 13. |
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| ID | Term |
|---|---|
| C090092 | migalastat |
| D002927 | Cimetidine |
| ID | Term |
|---|---|
| D006146 | Guanidines |
| D000578 | Amidines |
| D009930 | Organic Chemicals |
| D007093 | Imidazoles |
| D001393 |
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Fixed sequence
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| Cimetidine |
| Drug |
Twice daily oral dose of 800 mg cimetidine under fasted conditions |
|
| T1/2 of lucerastat | Plasma PK parameter of lucerastat after single-dose oral administration of lucerastat alone and in combination with cimetidine | 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 |
| Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |