SAD Study First-in-human study MAD Study RBA Study
Design features Two-part, single-centre, double-blind, randomised, placebo-controlled, parallel-group, single-ascending-dose, comparative study Single-centre, double-blind, randomised, placebo-controlled, parallel-group, multiple-ascending-dose study Two-part, randomised, open-label, single-dose, comparative parallel-group study
Study groups 10 cohorts of 8 subjects each; 6 on emodepside, 2 on placebo 3 cohorts of 8 subjects each; 6 on emodepside, 2 on placebo 7 cohorts of 12 subjects each; all on emodepside
Study population Healthy male subjects Healthy male subjects Healthy male subjects
Objectives Cohorts 1 to 8: assess safety, tolerability and PK of single ascending oral doses. Cohort 9: assess food effect on bio-availability of LSF Cohort 10: explore relationship between emodepside and AEs reported in Part 1, in particular ophthalmological events Assess safety, tolerability, PK and PD of multiple ascending oral doses of LSF over 10 days Assess PK (including food effect), safety and tolerability of two new ASD tablet formulations, a GR tablet and a GS tablet, compared to the LSF
Doses studied Cohorts 1 to 8: LSF at 1 mg, 2.5 mg, 5 mg, 10 mg or 20 mg under fasting conditions; IR tablet: 5 mg or 20 mg under fasting conditions; Cohort 9: LSF at 10 mg under fed conditions Cohort 10: 40 mg under fasting conditions Cohort 1: 5 mg once daily for 10 days; Cohort 2: 10 mg once daily for 10 days; Cohort 3: 10 mg twice daily for 10 days (single intake on last day). Once daily dosing: Cohort A: 5 mg LSF, fasting; Cohort B: 5 mg GR tablet, fasting; Cohort C: 5 mg GS tablet, fasting; Cohort D: 5 mg GR tablet, fed; Cohort E: 5 mg GS tablet, fed; Cohort F: 10 mg GR tablet, fasting Cohort G: 10 mg GS tablet, fasting
PK sample collection Pre-dose, at frequent timepoints up to 24 hours post-dose, at regular timepoints up to 168 hours post-dose and at 3 weeks post-dose Pre-dose, at frequent timepoints up to 15 hours post-dose at regular timepoints up to Day 30 post-dose Pre-dose, at frequent timepoints up to 24 hours post-dose and at regular timepoints up to 168 hours post-dose