Healthy Subjects
Conditions
Keywords
safety, pharmacokinetics
Brief summary
The objectives of this study were to evaluate the safety and tolerability of lucerastat, and to determine its pharmacokinetic profile as single oral doses at different strengths.
Detailed description
The subjects were enrolled sequentially to five dose groups, starting with the lowest dose level. Subjects could participate in only one Group.
Interventions
DRUGLucerastat
Hard gelatin capsule for oral administration containing lucerastat
DRUGPlacebo
Matching placebo capsules
Sponsors
Idorsia Pharmaceuticals Ltd.
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
OTHER
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Signed informed consent form. * Male subjects aged from 18 to 45 years at screening. * Body weight between 50 and 100 kg and body mass index (BMI) between 18.0 and 29.0 kg/m2 at screening. * Healthy on the basis of physical examination, cardiovascular assessments and laboratory tests.
Exclusion criteria
* History or clinical evidence of any disease or medical / surgical condition or treatment, which may put the subject at risk of participation in the study or may interfere with the absorption, distribution, metabolism or excretion of the study treatments. * Serious adverse reaction or hypersensitivity to any drug. * Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Terminal elimination half-life (t1/2) of lucerastat after two daily doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 48 hours after the first administration | t1/2 was calculated from the plasma concentrations-time curves for subjects receiving lucerastat twice daily |
| Time to reach Cmax (tmax) of lucerastat after two daily doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 48 hours after the first administration | tmax was determined directly from the observed plasma concentration-time curves of lucerastat in subjects receiving lucerastat twice daily. |
| Area under the plasma concentration-time curves (AUC) of lucerastat after single ascending doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 24 hours post administration | AUC was calculated from time zero to time t (last PK blood sample in which drug was detected) and extrapolated to infinity for subjects receiving a single dose. |
| Area under the plasma concentration-time curves (AUC) of lucerastat after two daily doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 48 hours after the first administration | AUC was calculated from time zero to time t (last PK blood sample in which drug was detected) and extrapolated to infinity for subjects receiving lucerastat twice daily |
| Terminal elimination half-life (t1/2) of lucerastat after single ascending doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 24 hours post administration | t1/2 was calculated from the corresponding plasma concentrations-time curves for subjects receiving a single dose |
| Maximum plasma concentration (Cmax) of lucerastat after two daily doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 48 hours after the first administration | Cmax was determined directly from the observed plasma concentration-time curves of lucerastat in subjects receiving lucerastat twice daily. |
| Number of participants with Adverse Events (AEs) | From baseline up to 7 days post-administration | An AE was defined as any untoward medical occurrence in a clinical investigation subject, which did not necessarily have a causal relationship with the treatment. |
| Maximum plasma concentration (Cmax) of lucerastat after single ascending doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 24 hours post administration | Cmax was determined directly from the observed plasma concentration-time curves of lucerastat in subjects receiving a single dose. |
| Time to reach Cmax (tmax) of lucerastat after single ascending doses of lucerastat | PK Blood samples were collected at pre-dose and at scheduled time points up to 24 hours post administration | tmax was determined directly from the observed plasma concentration-time curves of lucerastat in subjects receiving a single dose. |
Secondary
| Measure | Time frame |
|---|---|
| Change from baseline in blood pressure | Up to 24 hours post administration |
| Change from baseline in electrocardiogram (ECG) variables | Up to 24 hours post administration |
| Change from baseline in laboratory tests | Up to 24 hours post administration |
| Change from baseline in heart rate | Up to 24 hours post administration |
Countries
United Kingdom
Outcome results
None listed