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This randomized, single-center, open-label, one-sequence, two-period crossover study in three parts will assess the effects of multiple doses of ketoconazole, rifampicin and ritonavir-boosted atazanavir on the pharmacokinetics of a single dose of RO5093151 in healthy male and female volunteers. In Period 1, subjects will receive a single oral dose of RO5093151. In Period 2, subjects will receive a single oral dose of RO5093151 and multiple oral doses of either ketoconazole, rifampicin or ritonavir-boosted atazanavir. Anticipated time on study is up to 8.5 weeks.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| 1 Ketoconazole DDI | Experimental |
| |
| 2 Rifampicin DDI | Experimental |
| |
| 3 ATZ/r DDI | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| RO5093151 | Drug | Single oral dose |
|
| Measure | Description | Time Frame |
|---|---|---|
| Part 1: Effect of multiple doses of ketoconazole on single-dose pharmacokinetics of RO5093151 and metabolites: Area under the concentration-time curve (AUC) | Pre-dose and up to 72 hours post-dose | |
| Part 2: Effect of multiple doses of rifampicin on single-dose pharmacokinetics of RO5093151 and metabolites: Area under the concentration-time curve (AUC) | Pre-dose and up to 72 hours post-dose | |
| Part 3: Effect of multiple doses of ritonavir-boosted atazanavir on single-dose pharmacokinetics of RO5093151 and metabolites: Area under the concentration-time curve (AUC) | Pre-dose and up to 72 hours post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| Safety: Incidence of adverse events | approximately 6 month | |
| RO5093151 metabolites: Plasma/urine concentrations | Pre-dose and up to 72 hours post-dose | |
| Pharmacodynamics: Area under the effect curve (AUEC) for plasma cortisol/cortisone (Part 1 only) |
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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 |
|---|---|---|---|---|---|---|
| Merritt Island | Florida | 32953 | United States |
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| atazanavir | Drug | Multiple oral doses |
|
| ketoconazole | Drug | Multiple oral doses |
|
| rifampicin | Drug | Multiple oral doses |
|
| ritonavir | Drug | Multiple oral doses |
|
| Pre-dose and up to 24 hours post-dose |
| ID | Term |
|---|---|
| D000069446 | Atazanavir Sulfate |
| D007654 | Ketoconazole |
| D012293 | Rifampin |
| D019438 | Ritonavir |
| ID | Term |
|---|---|
| D011725 | Pyridines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D009842 | Oligopeptides |
| D010455 | Peptides |
| D000602 | Amino Acids, Peptides, and Proteins |
| D010879 | Piperazines |
| D012294 | Rifamycins |
| D006576 | Heterocyclic Compounds, 4 or More Rings |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D047029 | Lactams, Macrocyclic |
| D047028 | Macrocyclic Compounds |
| D011083 | Polycyclic Compounds |
| D013844 | Thiazoles |
| D013457 | Sulfur Compounds |
| D009930 | Organic Chemicals |
| D001393 | Azoles |
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