Clinical Study to Evaluate Blood Concentrations of PF-06700841 After Oral Dose as Different Formulations

A PHASE 1, OPEN-LABEL STUDY IN HEALTHY PARTICIPANTS TO INVESTIGATE THE PHARMACOKINETICS OF PF-06700841 FOLLOWING SINGLE ORAL ADMINISTRATION OF MODIFIED RELEASE TABLETS COMPARED TO IMMEDIATE RELEASE TABLETS UNDER FASTED CONDITIONS

PF-06700841 is a dual Tyrosine kinase 2 (TYK2) Janus kinase 1 (JAK1) inhibitor that is being developed for oral treatment of adult patients with Inflammatory Bowel Disease (IBD).This open-label study will evaluate the pharmacokinetics of PF-06700841 following single oral doses of immediate release (IR) and modified release (MR) tablets in healthy, adult participants under fasted conditions. This is an open label, single dose, randomized, 2 period, 2- sequence crossover study in a single cohort of approximately 8 (minimum 6) healthy participants.

Study Overview

• Status: Completed
• Conditions: Healthy Participants
• Intervention / Treatment: Drug: PF-06700841 Immediate release tablets; Drug: PF-06700841 Modified release tablets

• Study Type: Interventional
• Enrollment (Actual): 8
• Phase: Phase 1

Contacts and Locations

Study Locations

• Belgium
  • Brussels, Belgium, B-1070
    • Pfizer Clinical Research Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Key Inclusion Criteria:

• Healthy male, and female participants between the ages of 18 and 55 years at the time of screening, inclusive (Healthy is defined as no clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12 lead ECG and clinical laboratory tests).
• Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures.
• Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).

Key Exclusion Criteria:

• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
• Any condition possibly affecting drug absorption (eg, gastrectomy).
• Have or have had clinically significant infections within the past 3 months prior to the first dose of investigational product (eg, those requiring hospitalization or parenteral antibiotics, or as judged by the Investigator), evidence of any infection within the past 7 days prior to the first dose of investigational product, herpes simplex within 12 weeks or history of disseminated herpes simplex infection, symptomatic herpes zoster or recurrent (>1 episode) or disseminated herpes zoster.
• History of human immunodeficiency virus (HIV), hepatitis B, or hepatitis C; positive testing for HIV, hepatitis B surface antigen (HepBsAg), hepatitis B core antibody (HepBcAb) or hepatitis C antibody (HCVAb). As an exception, a positive hepatitis B surface antibody (HepBsAb) finding as a result of participant vaccination is permissible.
• History of tuberculosis or active or latent or inadequately treated infection, positive QuantiFERON tuberculosis (TB) Gold test.
• Previous administration with an investigational drug within 30 days (or as determined by the local requirement) or 5 half lives preceding the first dose of investigational product used in this study (whichever is longer).
• Female participants who are pregnant or wish to become pregnant; breastfeeding females.
• Males/Females of childbearing potential who are unwilling or unable to use a highly effective method of contraception as outlined in this protocol for the duration of the study and for at least 28 days after the last dose of investigational product.
• Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more within 56 days prior to dosing.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: PF-06700841: IR followed by MR; Participants receive PF-06700841 Immediate release tablets (IR) followed by PF-06700841 Modified release tablets (MR)	Drug: PF-06700841 Immediate release tablets; Small molecule tablets in immediate release form; Drug: PF-06700841 Modified release tablets; Small molecule tablets in modified release form
Experimental: PF-06700841: MR followed by IR; Participants receive PF-06700841 Modified release tablets (MR) followed by PF-06700841 Immediate release tablets (IR)	Drug: PF-06700841 Immediate release tablets; Small molecule tablets in immediate release form; Drug: PF-06700841 Modified release tablets; Small molecule tablets in modified release form

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum Observed Plasma Concentration (Cmax) of PF-06700841	pre-dose, 1,2,4,6,8,10,12,16,24,28,32,36,48 hour post-dose
Area under the plasma concentration-time curve from time zero to the last measured concentration (AUClast) of PF-06700841	pre-dose, 1,2,4,6,8,10,12,16,24,28,32,36,48 hour post-dose
Time to reach maximum observed plasma concentration (Tmax) of PF-06700841	pre-dose, 1,2,4,6,8,10,12,16,24,28,32,36,48 hour post-dose
Area under the plasma concentration-time curve from time zero to extrapolated infinite time (AUCinf) of PF-06700841 if data permit	pre-dose, 1,2,4,6,8,10,12,16,24,28,32,36,48 hour post-dose

Secondary Outcome Measures

Outcome Measure	Time Frame
Change from baseline in 12-Lead Electrocardiogram (ECG) parameters - PR interval, QRS complex, QT interval and QTC interval	Pre-dose and 48 hours post-dose
Change from baseline in heart rate	Pre-dose and 48 hours post-dose
Change from baseline in blood pressure	Pre-dose and 48 hours post-dose
Change from baseline in pulse rate	Pre-dose and 48 hours post-dose
Change from baseline in oral temperature	Pre-dose and 48 hours post-dose
Number of participants with laboratory abnormalities	Baseline and 48 hours post-dose
Number of participants with Treatment -Emergent Adverse Events (AEs), Serious Adverse Events (SAEs) and Discontinuation Due to AEs	Baseline to 48 hours post-dose

Collaborators and Investigators

• Sponsor: Pfizer

Publications and helpful links

Helpful Links

• To obtain contact information for a study center near you, click here.
• To obtain contact information for a study center near you, click here.

Study record dates

Study Major Dates

• Study Start (Actual): January 7, 2019
• Primary Completion (Actual): April 3, 2019
• Study Completion (Actual): April 3, 2019

Study Registration Dates

• First Submitted: November 28, 2018
• First Submitted That Met QC Criteria: December 4, 2018
• First Posted (Actual): December 5, 2018

Study Record Updates

• Last Update Posted (Actual): May 9, 2019
• Last Update Submitted That Met QC Criteria: May 7, 2019
• Last Verified: May 1, 2019

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protein Kinase Inhibitors; PF-06700841
• Other Study ID Numbers: B7931010; 2018-003512-41 (EudraCT Number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO
• IPD Plan Description: Pfizer will provide access to individual de-identified participant data and related study documents (e.g. protocol, Statistical Analysis Plan (SAP), Clinical Study Report (CSR)) upon request from qualified researchers, and subject to certain criteria, conditions, and exceptions. Further details on Pfizer's data sharing criteria and process for requesting access can be found at: https://www.pfizer.com/science/clinical_trials/trial_data_and_results/data_requests.

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes