Approval Probability 71%
TA Base Rate26%
Adjusted LOA41%
ML RiskLOW_RISK
| NCT ID | Title | Phase | Status | Enrollment | Velocity | Design | Start | Completion | Last Updated | Sites | Countries |
|---|---|---|---|---|---|---|---|---|---|---|---|
| NCT00964106 | Validation Study of Multiple Probe Compounds for Drug Interaction Evaluation | PHASE1 | COMPLETED | 87 | — | — | Aug 26, 2009 | Aug 29, 2011 | Jan 4, 2018 | 2 | South Korea |
Plasma AUC (0-inf) of probe and metabolite (where applicable) when administered alone, in combination with other probes/inhibitors
| Arm | Type | Description |
|---|---|---|
| Probe drugs | EXPERIMENTAL | Caffeine 100 mg CYP1A2 Pioglitazone 15 mg CYP2C8 Flurbiprofen 40 mg CYP2C9 Omeprazole 20 mg CYP2C19 Dextromethorphan 45 mg CYP2D6 Midazolam 3 mg (Part 1, Part 2 Cohorts B and C) 1 mg (Part 2 Cohort A) CYP3A4/5 Rosuvastatin 10 mg OATP1B1 |
| Default Inhibitors | EXPERIMENTAL | A Ketoconazole 400 mg once-daily Day 1 through Day 9 CYP3A4 B Fluconazole 400 mg x1 dose on Day 1 200 mg once-daily Day 2 through Day 9 CYP2C9 C Rifampin 600 mg x1 dose on Day 1 and Day 8 OATP1B1 |
| Name | Type | Description |
|---|---|---|
| Caffeine | DRUG | Caffeine dosed at 100 mg as probe for CYP1A2 pathway |
| Rosiglitazone | DRUG | Dosed at 4 mg as probe for CYP2C8 pathway |
| Flurbiprofen | DRUG | Dosed at 40 mg, probe for CYP2C9 pathway |
| Omeprazole | DRUG | Dosed at 20 mg, probe for CYP2C19 pathway |
| Dextromethorphan | DRUG | Dosed at 30 mg, probe for CYP2D6 pathway |
| Midazolam | DRUG | Dosed at 3 mg for Part 1, Part 2 cohorts B and C and 1 mg for Part 2 Cohort A, probe drug for CYP3A4/5 pathway |
| Rosuvastatin | DRUG | Dosed at 10 mg, probe drug for OATP1B1 pathway |
| Ketoconazole | DRUG | Dosed at 400 mg once-daily Day 1 through Day 9, inhibitor of CYP3A4 |
| Fluconazole | DRUG | Dosed at 400 mg x 1 dose on day 1, 200 mg once daily on days 2 through 9, inhibitor of CYP2C9 pathway |
| Rifampin | DRUG | Dosed at 600 mg x 1 dose on Day 1 and Day 8, inhibitor of OATP1B1 pathway |
Inclusion Criteria: * Healthy as determined by a responsible physician * Subjects are not poor metabolizers based on genotyping for the major CYP2C9, 2C19, 2D6 alleles * Male or female between 20 and 50 years of age at the time of screening, inclusive. * A female subject is eligible to participate ...