A Pilot Study To Investigate The Effect Of Concurrent Antacid Administration On The Bioavailability Of Six Experimental Formulations Of Palbociclib
- Conditions
- Healthy
- Interventions
- Registration Number
- NCT02311946
- Lead Sponsor
- Pfizer
- Brief Summary
This study will investigate whether concurrent administration of rabeprazole, an antacid known as a proton pump inhibitor, alters the absorption of the drug palbociclib when given as one of six experimental formulations.
- Detailed Description
This will be a 6 cohort study investigating one experimental formulation of palbociclib in each of the six cohorts of 10 healthy subjects. Each cohort will receive two treatments in a fixed-sequence. In Period 1, all subjects will receive a single 125mg dose of palbociclib alone and undergo serial pharmacokinetic blood sampling for up to 120 hours post-dose. In Period 2, all subjects will receive daily 40mg doses of Rabeprazole for 7 consecutive days, and approximately 4 hours after the Day 7 rabeprazole dose each subject will receive a single 125mg dose of palbociclib. Subjects will undergo serial pharmacokinetic blood sampling up to 120 hours post-dose.
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 60
- 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.
- Any condition possibly affecting drug absorption (eg, gastrectomy)
- A positive urine drug or cotinine test
- A known history of hypersensitivity to palbociclib
- A supine systolic blood pressure >140 mmHg, or a QTc >450 msec.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Cohort 2 Palbociclib + Rabeprazole Cohort 2 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet containing HMPC E3 Cohort 4 Palbociclib + Rabeprazole Cohort 4 will receive a 125 mg oval white/yellow palbociclib bilayer tablet with tartaric and succinic acid. Cohort 5 Palbociclib Alone Cohort 5 will receive a 125 mg oval yellow palbociclib fluid bed granulation tablet with succinic acid. Cohort 3 Palbociclib Alone Cohort 3 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet with HMPC E3 and succinic acid. Cohort 4 Palbociclib Alone Cohort 4 will receive a 125 mg oval white/yellow palbociclib bilayer tablet with tartaric and succinic acid. Cohort 1 Palbociclib + Rabeprazole Cohort 1 will receive a 125 mg round yellow palbociclib tablet containing succinic acid Cohort 3 Palbociclib + Rabeprazole Cohort 3 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet with HMPC E3 and succinic acid. Cohort 5 Palbociclib + Rabeprazole Cohort 5 will receive a 125 mg oval yellow palbociclib fluid bed granulation tablet with succinic acid. Cohort 6 Palbociclib Alone Cohort 6 will receive a 125 mg palbociclib oral solution Cohort 2 Palbociclib Alone Cohort 2 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet containing HMPC E3 Cohort 1 Palbociclib Alone Cohort 1 will receive a 125 mg round yellow palbociclib tablet containing succinic acid Cohort 6 Palbociclib + Rabeprazole Cohort 6 will receive a 125 mg palbociclib oral solution
- Primary Outcome Measures
Name Time Method AUCinf Pre-dose to 120 hours post-dose Area under the concentration-time curve from time zero to infinity.
Cmax Pre-dose to 120 hours post-dose Maximum observed plasma concentration
- Secondary Outcome Measures
Name Time Method CL/F Pre-dose to 120 hours post-dose Apparent oral clearance from plasma
Vz/F Pre-dose to 120 hours post-dose Apparent volume of distribution
t1/2 Pre-dose to 120 hours post-dose Terminal phase half-life
AUClast Pre-dose to 120 hours post-dose Area under the concentration-time curve from time zero to the time of the last quantifiable concentration.
Tmax Pre-dose to 120 hours post-dose Time of the maximum observed concentration post-dose.
Trial Locations
- Locations (3)
MRA Clinical Research - Phase 1
🇺🇸Miami, Florida, United States
Miami Research Associates, LLC
🇺🇸South Miami, Florida, United States
MRA Clinical Research, LLC
🇺🇸South Miami, Florida, United States