Table 2. Description of the 17 Phase 1 studies and the one Phase 2 study.
| Study description | Design | Subjects | Samples* | Doses/formulations |
|---|---|---|---|---|
| Single oral dose escalation | XO | 14♂HV | 7/0 | 1–20 mg SOL |
| SOL-IR, young-elderly | XO | 20♂/7♀HV | 15/16 | 10 mg IR/SOL |
| IV dose escalation | XO | 8♂HV | 49/46 | 0.6, 2, 6 mg IV |
| Effect of food | XO | 22♂HV | 30/34 | 30 mg CR |
| Multiple-dose IR-CR | XO | 13♂HV | 71/71 | 7.5 mg IR TID, 20 mg CRS, CRM, CRF OD |
| Dose escalation IR-CR | XO | 26♂HV | 48/48 | 7.5, 15, 30 mg CR OD 2.5, 5, 10 mg IR TID |
| One tablet CR vs. 2 tablets CR | XO | 23♂HV | 22/22 | 45 mg, 15 + 30 mg CR |
| Relative F IR and CR | XO | 24♂HV | 62/65 | 4 mg IV, 10 mg IR TID, 30 mg CR OD |
| Ketoconazole interaction | PG | 16♂HV | 22/22 | 30 mg CR OD 0, 400 mg ketoconazole |
| Erythromycin interaction | PG | 29♂HV | 21/21 | 30 mg CR OD 0, 400 mg erythromycin |
| Multiple dose SOL | PG | 11♂HV | 55/0 | 10 mg SOL TID |
| Oral contraceptive interaction | XO | 21♀HV | 5/5 | 10 mg IR TID |
| Multiple-dose IR | XO | 16♂HV | 36/36 | 2.5, 5, 10 mg IR TID |
| IR-CR in patients | XO | 29♂/16CPTS | 7/7 | 2.5 mg IR TID, 15, 30 mg CR OD |
| IR-CR in Japanese | XO | 16♂HV | 34/43 | 5, 7.5, 15, 20 mg CR OD, 5, 7.5 mg IR OD |
| Effect of food in Japanese | XO | 8♂HV | 17/19 | 15 mg CR |
| Single-dose CR in Japanese | PG | 6♂HV | 10/11 | 30 mg CR |
| Multiple-dose CR in Japanese | PG | 12♂HV | 32/33 | 15, 30 mg CR |
*
Samples = median number of darifenacin/metabolite samples per subject. XO, Cross-over; PG, parallel group; HV, healthy volunteer; PTS, patient; SOL, solution; IR, immediate release; CR, (continuous) extended release; CRS, CR; CRM, medium CR; CRF, fast CR; OD, once daily; TID, 3×/day.