A Pilot Study To Investigate The Effect Of Concurrent Antacid Administration On The Bioavailability Of Six Experimental Formulations Of Palbociclib

Pfizer

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Palbociclib Alone; Drug: Palbociclib + Rabeprazole

Study type: Interventional

Funder types: Industry

Identifiers

NCT02311946

A5481041

Details and patient eligibility

About

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.

Full 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.

Enrollment: 60 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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 test
• A known history of hypersensitivity to palbociclib
• A supine systolic blood pressure >140 mmHg, or a QTc >450 msec.

Trial design

Primary purpose: Basic Science

Allocation: Non-Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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60 participants in 6 patient groups

Cohort 1

Experimental group

Description:

Cohort 1 will receive a 125 mg round yellow palbociclib tablet containing succinic acid

Treatment:

Drug: Palbociclib + Rabeprazole

Drug: Palbociclib Alone

Cohort 2

Experimental group

Description:

Cohort 2 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet containing HMPC E3

Treatment:

Drug: Palbociclib + Rabeprazole

Drug: Palbociclib Alone

Cohort 3

Experimental group

Description:

Cohort 3 will receive a 125 mg oval yellow palbociclib spray-dried dispersion tablet with HMPC E3 and succinic acid.

Treatment:

Drug: Palbociclib + Rabeprazole

Drug: Palbociclib Alone

Cohort 4

Experimental group

Description:

Cohort 4 will receive a 125 mg oval white/yellow palbociclib bilayer tablet with tartaric and succinic acid.

Treatment:

Drug: Palbociclib + Rabeprazole

Drug: Palbociclib Alone

Cohort 5

Experimental group

Description:

Cohort 5 will receive a 125 mg oval yellow palbociclib fluid bed granulation tablet with succinic acid.

Treatment:

Drug: Palbociclib + Rabeprazole

Drug: Palbociclib Alone

Cohort 6

Experimental group

Description:

Cohort 6 will receive a 125 mg palbociclib oral solution

Treatment:

Drug: Palbociclib + Rabeprazole

Drug: Palbociclib Alone