A Study to Assess the Safety and Pharmacokinetics of Lucerastat (OGT 923) in Healthy Subjects

Phase 1

Completed

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

• Registration Number: NCT02944487
• Lead Sponsor: Actelion

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.

Study Timeline

• Study Start: 2002-10
• Primary Completion: 2002-12
• Study Completion: 2002-12
• Status Verified: 2016-10
• Study First Submitted: 2016-10-24
• Study First Submitted QC: 2016-10-24
• Last Update Submitted: 2016-10-24
• Study First Posted: 2016-10-26
• Last Update Posted: 2016-10-26

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 39

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.

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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.

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Placebo for singe ascending doses	Placebo	These subjects received matching placebo administered orally in the morning of Day 1
Placebo for b.i.d.Group	Placebo	These subjects received matching placebo administered orally in the morning and in the evening of Day 1
B.i.d. Dose Group	Lucerastat	Subjects received two doses of lucerastat (2 x 1 g) 12 hours apart on Day 1
Single ascending doses of lucerastat	Lucerastat	Subjects were enrolled sequentially in 4 groups and received a single oral dose of lucerastat from 100 mg to 1000 mg in the morning of Day 1

Primary Outcome Measures

Name	Time	Method
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.
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.
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 subjectsreceiving a single dose.
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
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

Secondary Outcome Measures

Name	Time	Method
Change from baseline in heart rate	Up to 24 hours post administration
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

Trial Locations

Locations (1)

Investigator Site; 🇬🇧 Tranent, United Kingdom