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Clinical trial information and results are updated daily from ClinicalTrials.gov. The latest data update was conducted on 01/23/2021.

A Study to Assess Pharmacokinetics of PF-04965842 and Its Metabolites and Effect of Probenecid in Healthy Participants

Clinicaltrials.gov identifier NCT03937258

Recruitment Status Completed

First Posted May 3, 2019

Last update posted October 18, 2019

Study Description

Brief summary:

A total of approximately 12 healthy male or female participants will be enrolled in the study so that at least 10 participants will complete the study. Participants will be screened within 28 days of the first dose of study medication. The single fixed-sequence will consist of 3 periods. Participants will report to the clinical research unit (CRU) at least 12 hours prior to Day 1 dosing in Period 1 and will be required to stay in the CRU for 12 days and 11 nights. Genotyping samples for cytochrome P450 (CYP) 2C19 and CYP2C9 will be collected pre dose in Period 1 only. In Period 1, participants will be administered a single oral 200 mg dose of PF-04965842 in the morning on Day 1 under fasted conditions (overnight fasting for at least 10 hours). No food will be allowed for at least 4 hours postdose and undergo serial blood sample collection for 48 hours postdose. In Period 2, participants will receive oral 200 mg dose of PF-04965842 once daily (QD) in the morning of Day 1 to Day 4 under fasted conditions (overnight fasting for at least 10 hours). No food will be allowed for at least 4 hours postdose and undergo serial blood sample collection for 48 hours postdose on Day 4. In Period 3, participants will receive probenecid 1000 mg twice daily (BID) in the mornings and evenings of Day 1 to Day 3. On the morning of Period 3 Day 2, after an overnight fast of approximately 8 hours, participants will be administered probenecid 1000 mg. A single 200 mg oral dose of PF 04965842 will be administered approximately 2 hours after the probenecid dose. Participants will remain in a fasted state for 4 hours after dosing with PF 04965842 and undergo serial blood sample collection for 48 hours post PF 04965842 dosing. Participants will be discharged from the CRU on Day 4 after all study procedures are completed. The participant will be required to have a Follow-up phone contact 28-35 days after the last dose of investigational product.

  • Condition or Disease:Healthy
  • Intervention/Treatment: Drug: PF-04965842
    Drug: Probenecid
  • Phase: Phase 1
Detailed Description

N/A

Study Design
  • Study Type: Interventional
  • Actual Enrollment: 12 participants
  • Allocation: Randomized
  • Intervention Model: Sequential Assignment
  • Masking: None (Open Label) ()
  • Primary Purpose: Other
  • Official Title: A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO ASSESS SINGLE DOSE AND MULTIPLE DOSE PHARMACOKINETICS OF PF-04965842 AND ITS METABOLITES, AND THE EFFECT OF REPEAT-DOSE PROBENECID ON THE SINGLE DOSE PHARMACOKINETICS OF PF-04965842 AND ITS METABOLITES IN HEALTHY PARTICIPANTS
  • Actual Study Start Date: May 2019
  • Actual Primary Completion Date: July 2019
  • Actual Study Completion Date: July 2019
Arms and interventions
Arm Intervention/treatment
Other: PF-04965842 multiple doses
In Period 2, participants will receive oral 200 mg dose of PF-04965842 once daily (QD) in the morning of Day 1 to Day 4 under fasted conditions.
Drug: PF-04965842
Participants will be administered a single oral 200 mg dose of PF-04965842 in the morning on Period 1 Day 1 and Period 3 Day 2 under fasted conditions. In Period 2, participants will receive oral 200 mg dose of PF-04965842 once daily (QD) in the morning of Day 1 to Day 4 under fasted conditions
Other: PF-04965842 single dose
In Period 1, subjects will be administered a single oral 200 mg dose of PF 04965842 in the morning on Day 1 under fasted conditions.
Drug: PF-04965842
Participants will be administered a single oral 200 mg dose of PF-04965842 in the morning on Period 1 Day 1 and Period 3 Day 2 under fasted conditions. In Period 2, participants will receive oral 200 mg dose of PF-04965842 once daily (QD) in the morning of Day 1 to Day 4 under fasted conditions
Other: Probenecid and PF-04965842
In Period 3, participants will receive probenecid 1000 mg twice daily (BID) in the mornings and evenings of Day 1 to Day 3. On the morning of Period 3 Day 2, after an overnight fast of approximately 8 hours, participants will be administered probenecid 1000 mg. A single 200 mg oral dose of PF 04965842 will be administered approximately 2 hours after the probenecid dose.
Drug: PF-04965842
Participants will be administered a single oral 200 mg dose of PF-04965842 in the morning on Period 1 Day 1 and Period 3 Day 2 under fasted conditions. In Period 2, participants will receive oral 200 mg dose of PF-04965842 once daily (QD) in the morning of Day 1 to Day 4 under fasted conditions

Drug: Probenecid
In Period 3, participants will receive probenecid 1000 mg twice daily (BID) in the mornings and evenings of Day 1 to Day 3. On the morning of Period 3 Day 2, after an overnight fast of approximately 8 hours, participants will be administered probenecid 1000 mg. A single 200 mg oral dose of PF 04965842 will be administered approximately 2 hours after the probenecid dose.
Outcome Measures
  • Primary Outcome Measures: 1. Maximum observed plasma concentration (Cmax) of PF-04965842 [ Time Frame: Period 1 Day 1, and Period 3 Day 2. ]
  • 2. Area under the curve from time zero to extrapolated infinite time (AUCinf) of PF-04965842 [ Time Frame: Period 1 Day 1 and Period 3 Day 2 ]
  • 3. AUC from time 0 to the time of the last quantifiable concentration (AUClast) of PF-04965842 [ Time Frame: Period 1 Day 1 and Period 3 Day 2 ]
  • 4. Area under the plasma concentration-time profile from time 0-24hr (AUCtau) of PF-04965842 [ Time Frame: Period 1 Day 1 ]
  • Secondary Outcome Measures: 1. Number of subjects with clinically significant abnormal vital signs [ Time Frame: Screenig up to Period 3 Day 4 ]
    Number of subjects with clinically significant abnormal vital signs
  • 2. Number of subjects with laboratory tests findings of potential clinical importance [ Time Frame: Screening up to Period 3 Day 4 ]
    Number of subjects with laboratory tests findings of potential clinical importance
  • 3. Number of subjects with adverse events (AEs). [ Time Frame: Screening up to 28-35 days after the last dose of PF 04965842 in period 3 ]
    Number of subjects with adverse events (AEs).
  • 4. Number of subjects with clinically significant abnormal Electrocardiograms (ECGs) [ Time Frame: Screening up to Period 3 Day 4 ]
    Number of subjects with clinically significant abnormal Electrocardiograms (ECGs).
Eligibility Criteria
  • Ages Eligible for Study: 18 to 55 Years (Adult)
  • Sexes Eligible for Study: All
  • Accepts Healthy Volunteers: Yes
Criteria

Inclusion Criteria:

1. Male and female participants must be 18 to 55 years of age, inclusive, at the time of
signing the informed consent document (ICD).

2. Male and female participants who are overtly healthy as determined by medical
evaluation including detailed medical history, full physical examination, including
blood pressure (BP) and pulse rate measurement, 12-lead ECG, and clinical laboratory
tests.

3. Participants who are willing and able to comply with all scheduled visits, treatment
plan, laboratory tests, lifestyle considerations, and other study procedures.

4. Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).

5. Capable of giving signed informed consent , which includes compliance with the
requirements and restrictions listed in the informed consent document (ICD) and in
this protocol.

Exclusion Criteria:

1. Evidence or history of clinically significant hematological, renal, endocrine,
pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or
allergic disease (including drug allergies, but excluding untreated, asymptomatic,
seasonal allergies at the time of dosing). Evidence of acute exacerbation of
dermatological condition (eg, AD, eczema or psoriasis) or visible rash present during
physical examination. Participants with history of psoriasis, AD or eczema can be
included in the study.

2. Participants, who according to the product label for probenecid, would be at increased
risk if dosed with probenecid, including participants with known blood dyscrasias,
uric acid kidney stones, gout, or gouty arthritis.

3. Any condition possibly affecting drug absorption (eg, gastrectomy).

4. Known relevant history or current elevations of liver function tests (LFTs) or
impaired liver function.

5. History of active or latent or inadequately treated tuberculosis (TB) infection, or a
positive QuantiFERON- TB Gold test.

6. Any history of chronic infections, any history of recurrent infections, any history of
latent infections, or any acute infection within 2 weeks of screening. History of
disseminated herpes zoster, or disseminated herpes simplex, or recurrent localized
multi-dermatomal herpes zoster.

7. History of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C;
positive testing for HIV, hepatitis B surface antigen (HBsAg), hepatitis B core
antibody (HBcAb) or hepatitis C virus antibody (HCVAb). Hepatitis B vaccination is
allowed.

8. History or evidence of any malignancies with the exception of adequately treated or
excised non-metastatic basal cell or squamous cell cancer of the skin, or cervical
carcinoma in situ.

9. Other acute or chronic medical or psychiatric condition including recent (within the
past year) or active suicidal ideation or behavior or laboratory abnormality that may
increase the risk associated with study participation or investigational product
administration or may interfere with the interpretation of study results and, in the
judgment of the investigator, would make the participant inappropriate for entry into
this study.

10. Use of prescription or nonprescription drugs and dietary and herbal supplements within
7 days or 5 half-lives (whichever is longer) prior to the first dose of
investigational product.

11. 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).

12. A positive urine drug test.

13. Screening supine systolic blood pressure (BP) <= 140 mm Hg or <90 mm Hg, following at least 5 minutes of supine rest OR Screening supine diastolic BP = 90 mm
Hg following at least 5 minutes of supine rest. If a participant meets any of these
criteria, the BP should be repeated 2 more times and the average of the 3 BP values
should be used to determine the participant's eligibility.

14. Screening supine 12-lead ECG demonstrating a corrected QT (QTc) interval >450 msec or
a QRS interval >120 msec. If QTc exceeds 450 msec, or QRS exceeds 120 msec, the ECG
should be repeated 2 more times and the average of the 3 QTc or QRS values should be
used to determine the participant's eligibility.

15. Participants with ANY of the following abnormalities in clinical laboratory tests at
screening, as assessed by the study-specific laboratory and confirmed by a single
repeat test, if deemed necessary:

1. Absolute neutrophil count of <1200/mm3; 2. Hemoglobin <10.0 g/dL or hematocrit <30%; 3. Absolute lymphocyte count = 2 *
upper limit of normal (ULN);

5. Total bilirubin level >1 * ULN; participants with a history of Gilbert's syndrome
may have direct bilirubin measured and would be eligible for this study provided
the direct bilirubin level is <= ULN; 6. Uric acid not within the normal reference range; 7. Platelet count of <150,000/mm3; 8. Estimated creatinine clearance 1.5 times the ULN.

16. History of alcohol abuse or binge drinking and/or any other illicit drug use or
dependence within 6 months of Screening. Binge drinking is defined as a pattern of 5
(male) and 4 (female) or more alcoholic drinks in about 2 hours. As a general rule,
alcohol intake should not exceed 14 units per week (1 unit = 8 ounces (240 mL) beer, 1
ounce (30 mL) of 40% spirit or 3 ounces (90 mL) of wine).

17. Use of tobacco or nicotine-containing products in excess of the equivalent of 5
cigarettes per day or 2 chews of tobacco per day.

18. Pregnant female participants; breastfeeding female participants; female participants
of childbearing potential who are unwilling or unable to use 1 highly effective method
of contraception as outlined in this protocol Contraception section for the duration
of the study and for at least 28 days after the last dose of investigational product.

19. Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more
within 60 days prior to dosing.

20. History of sensitivity to heparin or heparin-induced thrombocytopenia.

21. Unwilling or unable to comply with the criteria in the Lifestyle Considerations
section of this protocol.

22. Investigator site staff members directly involved in the conduct of the study and
their family members, site staff members otherwise supervised by the investigator, or
Pfizer employees, including their family members, directly involved in the conduct of
the study.

Contacts and Locations
Contacts
Locations

United States, Connecticut
New Haven Clinical Research Unit
New Haven

Sponsors and Collaborators

Pfizer

Investigators

Study Director: Pfizer CT.gov Call Center Pfizer

More Information
  • Responsible Party: Pfizer
  • ClinicalTrials.gov Identifier: NCT03937258 History of Changes
  • Other Study ID Numbers: B7451043
  • First Posted: May 3, 2019 Key Record Dates
  • Last Update Posted: October 18, 2019
  • Last Verified: October 2019
  • Individual Participant
    Data (IPD) Sharing
    Statement:
  • Plan to Share IPD: No
  • 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.
  • Studies a U.S. FDA-regulated Drug Product: Yes
  • Studies a U.S. FDA-regulated Device Product: No
  • Keywords provided by Pfizer: healthy volunteers