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This randomized, double-blind, placebo-controlled, single ascending dose study will assess the safety, pharmacokinetics, and pharmacodynamics of RO6864018 in healthy, male, Asian and Caucasian participants. Participants will be enrolled in cohorts and randomized 8:2 to receive a single oral administration of RO6864018 or placebo. Total study duration for each participant is up to 9 weeks.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| RO6864018 | Experimental | Asian participants will receive a single oral dose of RO6864018 capsule on Day 1. The first dose escalation cohort will receive a single 400 mg oral dose. Dose will be escalated in subsequent cohorts (up to Cohort 4) up to a maximum of 1600 mg, based on safety, pharmacokinetic, and pharmacodynamic data available from lower dose cohorts. The Cohort 5 will include Caucasian participants who will receive a single 1200 mg (or the highest dose well-tolerated by Asian participants, if lower than 1200 mg) oral dose of RO6864018 capsules on Day 1. |
|
| Placebo | Placebo Comparator | Participants will receive a single oral dose of placebo matching to RO6864018. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| RO6864018 | Drug | A single oral ascending dose of RO6864018 capsules on Day 1. |
| |
| Measure | Description | Time Frame |
|---|---|---|
| Number of Participants With Adverse Events | Baseline up to Day 29 |
| Measure | Description | Time Frame |
|---|---|---|
| Area Under the Plasma Concentration Time Curve From Time Zero to Infinity (AUC0-inf) of RO6864018 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose | |
| AUC0-inf of Active Metabolite RO6871765 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Clinical Trials | Hoffmann-La Roche | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Changi General Hospital; Clinical Trial & Research unit | Singapore | 529889 | Singapore | |||
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| Placebo |
| Drug |
A single oral dose of placebo matching RO6864018 capsules on Day 1. |
|
| AUC0-inf of Prodrug Metabolite RO6870868 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| AUC0-inf of Minor Metabolite RO6872373 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Area Under the Plasma Concentration Time Curve From Time Zero to Last Measurable Concentration (AUClast) of RO6864018 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| AUClast of Active Metabolite RO6871765 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| AUClast of Prodrug Metabolite RO6870868 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| AUClast of Minor Metabolite RO6872373 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Maximum Observed Plasma Concentration (Cmax) of RO6864018 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Cmax of Active Metabolite RO6871765 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Cmax of Prodrug Metabolite RO6870868 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Cmax of Minor Metabolite RO6872373 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Time to Maximum Plasma Concentration (Tmax) of RO6864018 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Tmax of Active Metabolite RO6871765 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Tmax of Minor Metabolite RO6872373 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| RO6864018 Urine Concentration | Pre-dose (0-4 hours before dosing), 0-4, 4-8, 8-12, 12-24, 24-36, and 36-48 hours post-Day 1 dose |
| Active Metabolite RO6871765 Urine Concentration | Pre-dose (0-4 hours before dosing), 0-4, 4-8, 8-12, 12-24, 24-36, and 36-48 hours post-Day 1 dose |
| Prodrug Metabolite RO6870868 Urine Concentration | Pre-dose (0-4 hours before dosing), 0-4, 4-8, 8-12, 12-24, 24-36, and 36-48 hours post-Day 1 dose |
| Minor Metabolite RO6872373 Urine Concentration | Pre-dose (0-4 hours before dosing), 0-4, 4-8, 8-12, 12-24, 24-36, and 36-48 hours post-Day 1 dose |
| Apparent Terminal Elimination Half-Life (T1/2) of RO6864018 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| T1/2 of Active Metabolite RO6871765 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| T1/2 of Prodrug Metabolite RO6870868 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| T1/2 of Minor Metabolite RO6872373 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Serum Interferon alpha Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Serum Interferon-Gamma-Inducible Protein-10 (IP-10) Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Serum Interleukin (IL)-6 Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Serum IL-10 Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Serum IL-12 Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Serum Neopterin Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Serum p40 (IL-12B) Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Interferon-Stimulated Gene-15 (ISG-15) Messenger Ribonucleic Acid (mRNA) Levels in Whole Blood | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Myxovirus Resistance 1 (MX-1) Gene mRNA Levels in Whole Blood | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Oligoadenylate Synthetase 1 (OAS 1) Gene mRNA Levels in Whole Blood | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Toll-Like Receptor 7 (TLR7) Gene mRNA Levels in Whole Blood | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Tmax of Prodrug Metabolite RO6870868 | Pre-dose (0 hour), 0.25, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 18, 24, 36 and 48 hours post-Day 1 dose |
| Serum Tumor Necrosis Factor Alpha Levels | Pre-dose (0 hours), 3, 6, 12, 18, 24, 36, and 48 hours post-Day 1 dose |
| Singapore |
| 529889 |
| Singapore |