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PPI And Food Effect Study For PF-06463922 In Healthy Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Registration Number
NCT02569554
Lead Sponsor
Pfizer
Brief Summary

The current study will be conducted in healthy adult subjects to evaluate the effect of proton pump inhibitor and food on pharmacokinetics of PF-06463922, to evaluate the bioavailability of the oral solution relative to the tablet formulation of PF-06463922.

Detailed Description

PF-06463922 is a selective, ATP competitive small molecule tyrosine kinase inhibitor (TKI) of the Anaplastic Lymphoma Kinase (ALK) positive (ALK+) or ROS oncogene 1 (ROS1) positive (ROS1+) receptor tyrosine kinases (RTK) that also potently inhibits ALK kinase domain mutations responsible for resistance to crizotinib. PF-06463922 is being developed as a novel anticancer agent for the treatment of patients with advanced ALK+ NSCLC or ROS1+ NSCLC.

The current study is a Phase 1, randomized, open label, 4 period, 4 treatment, 4 sequence, crossover study conducted in healthy adult subjects. Each subject will receive four single oral doses of 100 mg PF-06463922 as tablets alone, tablets with food, tablets with rabeprazole, and oral solution after overnight fasting with at least a 10 day washout period between each PF-06463922 dose.

Twenty four (24) subjects will be enrolled to obtain at least 20 evaluable subjects who complete all treatments. Subjects who withdraw will not be replaced unless the total number of completed subjects falls below 20.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
27
Inclusion Criteria
  • Healthy female subjects of non-childbearing potential and/or male subjects
  • Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
  • Evidence of a personally signed and dated informed consent document.
  • Subject must be willing to avoid direct sunlight exposure or any high intensity ultraviolet light exposure
Exclusion Criteria
  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular
  • Any condition possibly affecting drug absorption
  • A positive urine drug screen.
  • Use of tobacco- or nicotine containing products within 90 days of screening or a positive urine cotinine test and history of regular alcohol consumption exceeding 14 drinks/week for females or 21 drinks/week for males within 6 months of Screening.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
PF-06463922rabeprazoleeach subject will receive four single doses of PF-06463922 without food, with food, with rabeprazole (without food), and one of the two new formulations without food.
PF-06463922PF-06463922each subject will receive four single doses of PF-06463922 without food, with food, with rabeprazole (without food), and one of the two new formulations without food.
Primary Outcome Measures
NameTimeMethod
plasma Cmax for PF-064639223 months

observed maximal plasma PF-06463922 concentration

plasma AUCinf for PF-064639223 months

area under plasma concentration-time profile from time 0 extrapolated to infinite time for PF-06463922

Secondary Outcome Measures
NameTimeMethod
plasma Tmax for PF-064639223 months

time to the plasma maximal concentration for PF-06463922

plasma t1/2 for PF-064639223 months

plasma terminal half-life for PF-06463922

plasma AUClast for PF-064639223 months

area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration for PF-06463922

plasma CL/F for PF-064639223 months

apparent clearance for PF-06463922

plasma Vz/F for PF-064639223 months

apparent volume of distribution for PF-06463922

Trial Locations

Locations (1)

Pfizer Clinical Research Unit

🇧🇪

Brussels, Belgium

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