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 |
|---|---|---|---|---|---|---|---|---|---|---|---|
| NCT02311946 | A Pilot Study To Investigate The Effect Of Concurrent Antacid Administration On The Bioavailability Of Six Experimental Formulations Of Palbociclib | PHASE1 | COMPLETED | 60 | — | — | Jan 1, 2015 | Apr 1, 2015 | May 28, 2015 | 3 | United States |
| NCT02222441 | Effect Of Modafinil And Pioglitazone On The Pharmacokinetics Of Palbociclib (PD-0332991) | PHASE1 | COMPLETED | 14 | — | — | Oct 1, 2014 | Dec 1, 2014 | Feb 20, 2015 | 1 | United States |
| NCT02131298 | Effect Of Itraconazole On The Pharmacokinetics Of Palbociclib | PHASE1 | COMPLETED | 12 | — | — | May 1, 2014 | Jun 1, 2014 | Jun 30, 2014 | 1 | United States |
| NCT01918176 | Drug Interaction Study To Investigate The Potential Effect Of Proton Pump Inhibitor On The Pharmacokinetics Of Palbociclib (PD-0332991) | PHASE1 | COMPLETED | 26 | — | — | Sep 1, 2013 | Dec 1, 2013 | Oct 8, 2015 | 1 | United States |
Area under the concentration-time curve from time zero to infinity.
Maximum observed plasma concentration
AUC (0 - 8)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - 8). It is obtained from AUC (0 - t) plus AUC (t - 8).
| Arm | Type | Description |
|---|---|---|
| Cohort 1 | EXPERIMENTAL | Cohort 1 will receive a 125 mg round yellow palbociclib tablet containing succinic acid |
| Cohort 2 | EXPERIMENTAL | Cohort 2 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet containing HMPC E3 |
| Cohort 3 | EXPERIMENTAL | Cohort 3 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet with HMPC E3 and succinic acid. |
| Cohort 4 | EXPERIMENTAL | Cohort 4 will receive a 125 mg oval white/yellow palbociclib bilayer tablet with tartaric and succinic acid. |
| Cohort 5 | EXPERIMENTAL | Cohort 5 will receive a 125 mg oval yellow palbociclib fluid bed granulation tablet with succinic acid. |
| Cohort 6 | EXPERIMENTAL | Cohort 6 will receive a 125 mg palbociclib oral solution |
| Fixed sequence modafinil DDI arm (Cohort 1) | EXPERIMENTAL | Fixed sequence study with treatment A of palbociclib alone, followed by treatment B of palbociclib with modafinil in Cohort 1. |
| Fixed sequence pioglitazone DDI arm (Cohort 2) | EXPERIMENTAL | For Cohort 2, fixed sequence study with treatment A of palbociclib alone, followed by treatment C of palbociclib with pioglitazone. |
| Fixed sequence | OTHER | Fixed sequence study with treatment A of palbociclib alone, followed by treatment B (palbociclib with itraconazole) |
| Fixed sequence crossover | EXPERIMENTAL | All the subjects will undergo the treatment of Palbociclib alone first and then treatment of Palbociclib and Rabeprazole. |
| Name | Type | Description |
|---|---|---|
| Palbociclib Alone | DRUG | In Period 1 of each Cohort, a single 125 mg dose of palbociclib will be administered alone in a fasted state, and subjects will undergo serial pharmacokinetic blood sampling for up to 120 hours post-dose. |
| Palbociclib + Rabeprazole | DRUG | In Period 2 of each Cohort, subjects will receive daily 40 mg oral doses of the proton pump inhibitor rabeprazole on 7 consecutive days. Approximately 4 hours after the last rabeprazole dose a single 125 mg dose of palbociclib will be administered alone in a fasted state, and subjects will undergo serial pharmacokinetic blood sampling for up to 120 hours post-dose. |
| Palbociclib plus Modafinil | DRUG | For Cohort 1, modafinil 200 mg once daily for 7 days, followed by 400 mg once daily for 25 days; on Day 28, a single oral 125 mg dose of palbociclib will be given with modafinil after a meal, followed by 120 hours of PK sample collection. |
| Palbociclib plus pioglitazone | DRUG | For Cohort 2, pioglitazone 45 mg once daily for a total of 19 days; On Day 15, a single oral 125 mg dose of palbociclib will be given with pioglitazone after a meal, followed by 120 hours of PK sample collection. |
| Palbociclib plus itraconazole | DRUG | Itraconazole 200 mg once daily with food for a total of 11 days; on Day 5, a single oral 125 mg dose of palbociclib will be given with itraconazole after a meal, followed by 168 hours of PK sample collection. |
Inclusion Criteria: * Healthy Male or Female of non-childbearing potential, * Having a body weight \>50 kg * Having a bopy mass index (BMI) between 17.5 and 30.5 kg/m2. Exclusion Criteria: * Any condition possibly affecting drug absorption (eg, gastrectomy) * A positive urine drug or cotinine tes...