Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Palbociclib alone · 4 trials · 1 indication
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...
Palbociclib alone refers to the small molecule CDK4 and CDK6 inhibitor developed by Pfizer, studied as a single agent in Phase 1 pharmacokinetic and drug interaction trials. The trials listed here enrolled healthy volunteers rather than patients with a disclosed disease, and all four studies have been completed.
Palbociclib alone targets CDK4, CDK6, and CCND1. It is an inhibitor of these cyclin-dependent kinases and cyclin D1, which regulate progression through the cell cycle. The trials described here were designed to measure drug exposure and interactions rather than to test efficacy against a specific tumor type.
Pfizer, Inc. develops palbociclib alone. The company trades under the ticker PFE. Pfizer sponsored the Phase 1 studies of the compound as a single agent, including the bioavailability and drug interaction trials listed in the clinical trial registry.
Palbociclib alone is in Phase 1 development. All four registered studies of the single agent are Phase 1 trials, and all four are completed. No active trials of palbociclib alone are currently listed, and the studies enrolled a total of 112 participants.
Four completed Phase 1 trials studied palbociclib alone: NCT02311946 examined antacid effects on bioavailability, NCT02222441 examined modafinil and pioglitazone effects on pharmacokinetics, NCT02131298 examined itraconazole effects, and NCT01918176 examined proton pump inhibitor effects. All enrolled healthy volunteers in the United States.
Yes, palbociclib alone is the same compound as PD-0332991. The code PD-0332991 appears in the titles of the Phase 1 pharmacokinetic studies, including the modafinil and pioglitazone interaction trial and the proton pump inhibitor interaction trial, confirming the two names refer to the same agent.