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Absorption, Metabolism, Excretion and Absolute Bioavailability

Last updated on August 9, 2018

FOR MORE INFORMATION
Study Location
PRA Health Sciences
Groningen, , 9713 GZ Netherlands
Contact
1-800-718-1021
Eligibility criteria
Condition
The disease, disorder, syndrome, illness, or injury that is being studied.
Healthy
Sex
Male
Age
Pediatric Trials: 0-17 Years
Adult Trials: 18+ Years
18-55 years
Inclusion criteria
The factors, or reasons, that allow a person to participate in a clinical study.
Show details

1. Healthy male subjects who, at the time of screening, are between the ages of 18 and 55
years, 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 electrocardiogram (ECG), or clinical
laboratory tests.

2. Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).

3. Evidence of a personally signed and dated informed consent document indicating that
the subject has been informed of all pertinent aspects of the study.

4. Subjects who are willing and able to comply with study confinement period, scheduled
visits, treatment plan, laboratory tests, contraceptive requirements and other study
procedures.

Exclusion criteria
The factors, or reasons, that prevent a person from participating in a clinical study.
Show details

Subjects with any of the following characteristics/conditions will not be included in the
study:

1. 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).

2. Any clinically significant malabsorption condition (eg, gastrectomy, bowel resection).

3. A positive urine drug screen for drugs of abuse or recreational drugs.

4. 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).

5. History of abuse of alcohol 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
or more alcoholic drinks (male) in about 2 hours. As a general rule, alcohol intake
should not exceed 21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit or a
125 mL glass of wine).

6. Use of tobacco/nicotine containing products in excess of 5 cigarettes/day.

7. Treatment with an investigational drug within 60 days.

8. Total 14C radioactivity measured in plasma exceeding 11 mBq/mL.

9. Screening supine blood pressure >=140 mm Hg (systolic) or >=90 mm Hg (diastolic),
following at least 5 minutes of supine rest. If blood pressure is >=140 mm Hg
(systolic) or >=90 mm Hg (diastolic), the blood pressure measurement should be
repeated two more times and the average of the three measurements should be used to
assess the subject's eligibility.

10. Supine 12 lead ECG demonstrating QTcF >450 msec or a QRS interval >120 msec at
screening. If QTcF exceeds 450 msec, or QRS exceeds 120 msec, the ECG should be
repeated two more times and the average of the three QTcF or QRS values should be used
to determine the subject's eligibility.

11. Use of prescription or nonprescription drugs (including vitamins and dietary
supplements) within 7 days or 5 half lives (whichever is longer) prior to the first
dose of study medication. As an exception, acetaminophen may be used at doses of = g/day. Limited use of non prescription medications that are not believed to affect
subject safety or the overall results of the study may be permitted on a case by case
basis following approval by Pfizer.

12. Use of herbal supplements within 28 days prior to the first dose of study medication.

13. Blood donation (excluding plasma donations) of no more than 100 mL or more within 56
days prior to dosing.

14. An estimated glomerular filtration rate of variable Modification of Diet in Renal Disease (MDRD) equation.

15. History of tuberculosis or active or latent or inadequately treated infection,
positive QuantiFERON TB Gold test.

16. Any medical history of disease (ie, Gilbert's disease) that has the potential to cause
a rise in total bilirubin over the upper limit of normal (ULN).

17. Subjects 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, if deemed necessary:

- Serum aspartate aminotransferase (AST) or alanine aminotransferase (ALT) >=1.5 ×
ULN, total serum bilirubin >= 25.6 micromol/L;

- Hemoglobin =

18. Known participation in a clinical trial for PF 04965842 within 60 days prior to the
first dose of study medication.

19. Serious adverse reaction or serious hypersensitivity to any drug or the formulation
excipients.

20. Unwilling or unable to comply with the Lifestyle Requirements described in this
protocol.

21. Subjects who are investigational site staff members directly involved in the conduct
of the study and their family members, site staff members otherwise supervised by the
Investigator, or subjects who are Pfizer employees, including their family members,
directly involved in the conduct of the study.

22. Systemic therapy with any of the following medications that are CYP3A4 inhibitors
within 7 days or 5 half lives (whichever is longer) or CYP3A inducers within 28 days
prior to the first dose of the trial medication, or during the trial (Section 5.7).

23. History of sensitivity to heparin or heparin induced thrombocytopenia.

24. 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 subject inappropriate for entry into this
study.

25. Subjects with conditions that affect their ability to taste ie, dysgeusia, respiratory
infection, cold, etc.

26. Male subjects 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 90 days after the last dose of investigational product.

NCT03250039
Pfizer
Completed
Absorption, Metabolism, Excretion and Absolute Bioavailability

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Absorption, Metabolism, Excretion and Absolute Bioavailability
A Phase 1, Open-label, Non-randomized, 2-period, Fixed Sequence Study To Investigate The Absorption, Metabolism And Excretion Of [14c-pf-04965842] And To Assess The Absolute Bioavailability And Fraction Absorbed Of Pf-04965842 In Healthy Male Subjects Using A 14c-microtracer Approach
This study will investigate the absorption, metabolism and excretion of 14C-PF 04965842 and characterize plasma, fecal and urinary radioactivity and identify any metabolites, if possible, of 14C PF-04965842 in humans. In addition, this study will provide a better understanding of the pharmacokinetic disposition of PF-04965842 by obtaining intravenous (IV) clearance and delineating the extent of oral absorption (absolute bioavailability (F) and fraction absorbed (Fa)).
Not Provided
Interventional
Phase 1
Allocation: Non-Randomized
Intervention Model: Crossover Assignment
Intervention Model Description:
This study will be an open label, non randomized, 2 period, fixed sequence, single dose study to characterize the absorption, metabolism and excretion of 14C- PF-04965842 and to evaluate the absolute oral bioavailability (F) and fraction absorbed (Fa) of PF-04965842 following oral administration of unlabeled PF-04965842 and IV and oral administration of 14C-PF-04965842 to healthy male subjects.

Masking: None (Open Label)
Primary Purpose: Other

Healthy
  • Drug: PF-04965842
    14C labeled PF-04965842
  • Drug: Absolute Bioavailability
    Oral dose of unlabeled PF-04965842 and an IV dose of 14C labeled PF- 04965842
  • Experimental: Mass Balance
    Cumulative recovery of radioactivity in urine and feces
    Intervention: Drug: PF-04965842
  • Experimental: Absolute Bioavailability
    Oral absolute bioavailability
    Intervention: Drug: Absolute Bioavailability
Not Provided


*   Includes publications given by the data provider as well as publications
identified by ClinicalTrials.gov Identifier (NCT Number) in Medline.
 
Completed
6
September 15, 2017
September 15, 2017   (Final data collection date for primary outcome measure)

Inclusion Criteria:

  1. Healthy male subjects who, at the time of screening, are between the ages of 18 and 55 years, 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 electrocardiogram (ECG), or clinical laboratory tests.
  2. Body Mass Index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
  3. Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study.
  4. Subjects who are willing and able to comply with study confinement period, scheduled visits, treatment plan, laboratory tests, contraceptive requirements and other study procedures.

Exclusion Criteria

Subjects with any of the following characteristics/conditions will not be included in the study:

  1. 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).
  2. Any clinically significant malabsorption condition (eg, gastrectomy, bowel resection).
  3. A positive urine drug screen for drugs of abuse or recreational drugs.
  4. 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).
  5. History of abuse of alcohol 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 or more alcoholic drinks (male) in about 2 hours. As a general rule, alcohol intake should not exceed 21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit or a 125 mL glass of wine).
  6. Use of tobacco/nicotine containing products in excess of 5 cigarettes/day.
  7. Treatment with an investigational drug within 60 days.
  8. Total 14C radioactivity measured in plasma exceeding 11 mBq/mL.
  9. Screening supine blood pressure >=140 mm Hg (systolic) or >=90 mm Hg (diastolic), following at least 5 minutes of supine rest. If blood pressure is >=140 mm Hg (systolic) or >=90 mm Hg (diastolic), the blood pressure measurement should be repeated two more times and the average of the three measurements should be used to assess the subject's eligibility.
  10. Supine 12 lead ECG demonstrating QTcF >450 msec or a QRS interval >120 msec at screening. If QTcF exceeds 450 msec, or QRS exceeds 120 msec, the ECG should be repeated two more times and the average of the three QTcF or QRS values should be used to determine the subject's eligibility.
  11. Use of prescription or nonprescription drugs (including vitamins and dietary supplements) within 7 days or 5 half lives (whichever is longer) prior to the first dose of study medication. As an exception, acetaminophen may be used at doses of =<1 g/day. Limited use of non prescription medications that are not believed to affect subject safety or the overall results of the study may be permitted on a case by case basis following approval by Pfizer.
  12. Use of herbal supplements within 28 days prior to the first dose of study medication.
  13. Blood donation (excluding plasma donations) of no more than 100 mL or more within 56 days prior to dosing.
  14. An estimated glomerular filtration rate of <90 mL/min/1.73 m2 based on the four variable Modification of Diet in Renal Disease (MDRD) equation.
  15. History of tuberculosis or active or latent or inadequately treated infection, positive QuantiFERON TB Gold test.
  16. Any medical history of disease (ie, Gilbert's disease) that has the potential to cause a rise in total bilirubin over the upper limit of normal (ULN).
  17. Subjects 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, if deemed necessary:

    • Serum aspartate aminotransferase (AST) or alanine aminotransferase (ALT) >=1.5 × ULN, total serum bilirubin >= 25.6 micromol/L;
    • Hemoglobin =<2.17 mmol/L (males).
  18. Known participation in a clinical trial for PF 04965842 within 60 days prior to the first dose of study medication.
  19. Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients.
  20. Unwilling or unable to comply with the Lifestyle Requirements described in this protocol.
  21. Subjects who are investigational site staff members directly involved in the conduct of the study and their family members, site staff members otherwise supervised by the Investigator, or subjects who are Pfizer employees, including their family members, directly involved in the conduct of the study.
  22. Systemic therapy with any of the following medications that are CYP3A4 inhibitors within 7 days or 5 half lives (whichever is longer) or CYP3A inducers within 28 days prior to the first dose of the trial medication, or during the trial (Section 5.7).
  23. History of sensitivity to heparin or heparin induced thrombocytopenia.
  24. 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 subject inappropriate for entry into this study.
  25. Subjects with conditions that affect their ability to taste ie, dysgeusia, respiratory infection, cold, etc.
  26. Male subjects 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 90 days after the last dose of investigational product.
Sexes Eligible for Study: Male
Gender Based Eligibility: Yes
18 Years to 55 Years   (Adult)
Yes
Contact information is only displayed when the study is recruiting subjects
Netherlands
 
 
NCT03250039
B7451008
2017-000461-73 ( EudraCT Number )
No
Studies a U.S. FDA-regulated Drug Product: No
Studies a U.S. FDA-regulated Device Product: No
Plan to Share IPD: No
Plan Description: Information relating to our policy on data sharing and the process for requesting data can be found at the following link: http://www.pfizer.com/research/clinical_trials/trial_data_and_results/da...
Pfizer
Pfizer
Not Provided
Study Director: Pfizer CT.gov Call Center Pfizer
Pfizer
November 2017

ICMJE     Data element required by the

International Committee of Medical Journal Editors
and the
World Health Organization ICTRP

FOR MORE INFORMATION

Contact a representative by phone, email, or visiting thte study website. To get updates and notications about this trail, sign up using the form below.

BY PHONE

Pfizer Clinical Trials Contact Center

1-800-718-1021

BY EMAIL

Contact

[email protected]



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