Leucettinib-21 First-in-Human Phase 1 in Healthy Volunteers and Subjects With Down Syndrome and Alzheimer's Disease
- Conditions
- Healthy VolunteersDown SyndromeAlzheimer's Disease
- Interventions
- Registration Number
- NCT06206824
- Lead Sponsor
- Perha Pharmaceuticals
- Brief Summary
Leucettinib-21 First-in-Human Phase 1 Study in 4 Parts: Single (Part 1) and Multiple (Part 3) Ascending Doses, and Food-Effect (Part 2) in Healthy Subjects, and Single Dose (Part 4) in People with Down Syndrome (DS) and Alzheimer's Disease (AD).
For Parts 1, 3 and 4, safety and tolerability of an oral administration of Leucettinib-21 will be assessed as primary objectives. Pharmacokinetics and pharmacodynamic biomarkers will be investigated as secondary objectives.
For Part 2, the effect of high fat meal will be evaluated on the pharmacokinetics parameters after an oral administration of Leucettinib-21.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- RECRUITING
- Sex
- Male
- Target Recruitment
- 120
Not provided
Not provided
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SEQUENTIAL
- Arm && Interventions
Group Intervention Description Part 2 : Food-Effect in Healthy Volunteers Leucettinib-21 A total of 12 healthy male volunteers will be randomly assigned to one of two sequences in this cross over study part. All subjects will receive the same one dose of Leucettinib-21 in each sequence. Part 1 : Single Ascending Doses in Healthy Volunteers Leucettinib-21 A total of 48 healthy male volunteers will be randomized into six consecutive single ascending dose cohorts of 8 subjects, 6 receiving one dose of Leucettinib-21 and 2 receiving placebo. Part 3 : Multiple Ascending Doses over 14 days in Healthy Volunteers Leucettinib-21 A total of 36 healthy male volunteers will be randomized into three consecutive multiple ascending doses cohorts of 12 subjects, 9 receiving one dose of Leucettinib-21 and 3 receiving placebo everyday for 14 days. Part 4 : Single Dose in People with Down Syndrome and Alzheimer's Disease Leucettinib-21 A total of 12 people with Down Syndrome and 12 people with Alzheimer's Disease will receive the same one dose of Leucettinib-21.
- Primary Outcome Measures
Name Time Method Part 1 : Safety and tolerability of Leucettinib-21 after single administration at 6 increasing doses in healthy male subjects. Part 1 : Up to 8 days following administration Assessment of systemic tolerability and safety:
Part 2 : Effect of food on the PK parameters after an oral administration of Leucettinib-21 in healthy male subjects in high fat breakfast condition vs. under fasted conditions. Part 2 : Up to 8 days following administration Plasma PK assessments
Part 3 : Safety and tolerability of Leucettinib-21 after multiple administration at 3 increasing doses in healthy male subjects Part 3 : Up to 21 days following administration Assessment of systemic tolerability and safety
Part 4 : Safety and tolerability of Leucettinib-21 after single administration at 1 dose in Down Syndrome individuals and patients with Alzheimer's disease Part 4 : Up to 8 days following administration Assessment of systemic tolerability and safety
- Secondary Outcome Measures
Name Time Method PK of Leucettinib-21 Up to 24 hours following Leucettinib-21 administration Assessment of the plasmatic PK of Leucettinib-21
PD of Leucettinib-21 Up to 4 hours following Leucettinib-21 administration Change in the proteome following Leucettinib-21 administration assessed by phosphoproteomics
Activity of DYRK1A Up to 8 hours following Leucettinib-21 administration Change in DYRK1A activity following Leucettinib-21 administration assessed in Peripheral Blood Mononuclear Cells
Trial Locations
- Locations (1)
Eurofins Optimed
🇫🇷Gières, France