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CompletedNCT02309827Updated Sep 19, 2016

Safety and Pharmacokinetic Study of PF-06651600 in Healthy Volunteers

A Phase 1 interventional study of PF-06651600 or Placebo in Healthy, sponsored by Pfizer. Completed at 1 site in Belgium. Open to participants aged 18 Years to 55 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2016-09-19.

Sponsored by Pfizer · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
80
Allocation
Randomized
Ages
18 Years to 55 Years
Sex
All
01

Study summary

This study is a first in human study of PF-06651600. PF-06651600 is being developed for treatment of inflammatory bowel disease. This study will test single and multiple doses of PF-06651600. The goal of the study is to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of PF-06651600 in healthy volunteers.

02

Conditions studied

  • Healthy

Keywords

  • Inflammatory bowel disease
03

In context

Lead sponsor

Pfizer is the lead sponsor of 3,244 studies on the registry; 139 are open to participants now.

Of its 582 completed or terminated interventional studies of FDA-regulated products, 381 (65%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 55 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  • Healthy male/female subjects between 18 and 55 years old, inclusive. Females must be of non-child bearing potential.
  • BMI of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lbs).
  • Evidence of personally signed and dated informed consent document.
  • Willing and able to comply with scheduled visits, treatment plan, lab tests and other study procedures.
  • Subjects must avoid high intensity UV light exposure (eg, active sunbathing, tanning beds/booths or sunlamps) from the first dose of study drug and for the duration of the study.

Exclusion criteria

Exclusion Criteria:

  • Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, GI, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease.
  • Use of tobacco/nicotine containing products in excess of 5 cigarettes/day.
  • History of regular alcohol consumption exceeding 14 drinks/week for females or 21 drinks/week for males.
  • Screening blood pressure >140/90 mm Hg.
  • Screening laboratory abnormalities as defined by the protocol.
  • Unwilling or unable to comply with the Lifestyle Guidelines as defined by the protocol.
05

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Randomized
Masking
Double (Participant, Investigator)
Enrollment
80 participants (actual)

Study arms

  • Experimental
    Cohort 1: PF-06651600 or Placebo

    Single ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 2: PF-06651600 or Placebo

    Single ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 3: PF-06651600 or Placebo

    Single ascending doses and multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 4: PF-06651600 or Placebo

    Single ascending doses and multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 5: PF-06651600 or Placebo

    Single ascending doses and multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 6: PF-06651600 or Placebo

    Single ascending doses and multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 7: PF-06651600 or Placebo

    Single ascending doses and multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 8: PF-06651600 or Placebo

    Single ascending doses and multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

  • Experimental
    Cohort 9: PF-06651600 or Placebo

    Multiple ascending doses of PF-06651600 or placebo to evaluate safety, tolerability and PK.

    Drug: PF-06651600 or Placebo

Interventions

  • DrugPF-06651600 or Placebo

    PF-06651600 or placebo will be administered as an extemporaneously prepared solution in each cohort.

06

What researchers measure

Primary outcomes

  1. 24 hour creatinine clearance (Single Dose)

    24 hour urine creatinine clearance in healthy subjects participating in the single dose periods. For the single dose period, assessment occurs on Study Days 0 and 1.

    Time frame: Single dose period, Day 0 (baseline) and 24 hours post dose Day 1.

  2. 24 hour creatinine clearance (Multiple Dose)

    24 hour urine creatinine clearance in healthy subjects participating in the multiple dose period. For the multiple ascending dose period assessments occur on Study Days 7 and 14.

    Time frame: Multiple dose period, Days 0 (baseline), 7 and 14.

  3. Change from baseline in urine volume (Single Dose)

    For the single dose period, assessment occurs on Study Days 0 and 1.

    Time frame: Single dose period, Day 0 (baseline) and 24 hours post dose Day 1.

  4. Change from baseline in urine electrolytes (Single Dose)

    For the single dose period, assessment occurs on Study Days 0 and 1.

    Time frame: Single dose period, Day 0 (baseline) and 24 hours post dose Day 1.

  5. Change from baseline in urine osmolality (Single Dose)

    For the single dose period, assessment occurs on Study Days 0 and 1.

    Time frame: Single dose period, Day 0 (baseline) and 24 hours post dose Day 1.

  6. Change from baseline of urine volume (Multiple Dose)

    For the multiple ascending dose period assessments occur on Study Days 7 and 14.

    Time frame: Multiple dose period, Days 0 (baseline), 7 and 14.

  7. Change from baseline of urine electrolytes (Multiple Dose)

    For the multiple ascending dose period assessments occur on Study Days 7 and 14.

    Time frame: Multiple dose period, Days 0 (baseline), 7 and 14.

  8. Change from baseline in urine osmolality (Multiple Dose)

    For the multiple ascending dose period assessments occur on Study Days 7 and 14.

    Time frame: Multiple dose period, Days 0 (baseline), 7 and 14.

Secondary outcomes

  1. Maximum Observed Plasma Concentration (Cmax) for PF-06651600 (Single Dose)

    Maximum Observed Plasma Concentration (Cmax)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  2. Maximum Observed Plasma Concentration (Cmax) for PF-06651600 (Multiple Dose)

    Maximum Observed Plasma Concentration (Cmax)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  3. Time to Reach Maximum Observed Plasma Concentration (Cmax) for PF-06651600 (Single Dose)

    Time to Reach Maximum Observed Plasma Concentration (Cmax)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  4. Time to Reach Maximum Observed Plasma Concentration (Cmax) for PF-06651600 (Multiple Dose)

    Time to Reach Maximum Observed Plasma Concentration (Cmax)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  5. Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) for PF-06651600 (Single Dose)

    Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  6. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for PF-06651600 (Single Dose)

    Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  7. Dose Normalized Maximum Observed Plasma Concentration (Cmaxdn) for PF-06651600 (Single Dose)

    Dose Normalized Maximum Observed Plasma Concentration (Cmaxdn)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  8. Dose Normalized Maximum Observed Plasma Concentration (Cmaxdn) for PF-06651600 (Multiple Dose)

    Dose Normalized Maximum Observed Plasma Concentration (Cmaxdn)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  9. Dose Normalized Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinfdn) for PF-06651600 (Single Dose)

    Dose Normalized Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinfdn)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  10. Dose Normalized Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClastdn) for PF-06651600 (Single Dose)

    Dose Normalized Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClastdn)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  11. Plasma Decay Half-Life (t1/2) for PF-06651600 (Single Dose)

    Plasma Decay Half-Life (t1/2)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  12. Plasma Decay Half-Life (t1/2) for PF-06651600 (Multiple Dose)

    Plasma Decay Half-Life (t1/2)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  13. Mean Resonance Time (MRT) for PF-06651600 (Single Dose)

    Mean Resonance Time (MRT)

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  14. Mean Resonance Time (MRT) for PF-06651600 (Multiple Dose)

    Mean Resonance Time (MRT)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  15. Apparent Volume of Distribution (Vz/F) for PF-06651600 (Single Dose)

    Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  16. Apparent Volume of Distribution (Vz/F) for PF-06651600 (Multiple Dose)

    Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed.

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  17. Apparent Total Body Clearance (CL/F) for PF-06651600 (Single Dose)

    Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Apparent total body clearance (CL/F) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.

    Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, 48 hours post dose

  18. Apparent Total Body Clearance (CL/F) for PF-06651600 (Multiple Dose)

    Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Apparent total body clearance (CL/F) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood.

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  19. Minimum Observed Plasma Concentration (Cmin) for PF-06651600 (Multiple Dose)

    Minimum Observed Plasma Concentration (Cmin)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  20. Average Concentration for Dosing Interval (12 or 24 hours) (Cav) for PF-06651600 (Multiple Dose)

    Average Concentration for Dosing Interval (12 or 24 hours) (Cav)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  21. Area Under the Curve for Dosing Interval (12 or 24 hours) for PF-06651600 (Multiple Dose)

    Area Under the Curve for Dosing Interval (12 or 24 hours)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  22. Dose Normalized Area Under the Curve for Dosing Interval (12 or 24 hours) for PF-06651600 (Multiple Dose)

    Dose Normalized Area Under the Curve for Dosing Interval (12 or 24 hours)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  23. Peak to Trough Fluctuation (PTF) for PF-06651600 (Multiple Dose)

    Peak to Trough Fluctuation (PTF)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  24. Observed Accumulation Ratio (Rac) for PF-06651600 (Multiple Dose)

    Observed Accumulation Ratio (Rac)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  25. Observed Accumulation Ratio for Cmax (RacCmax) for PF-06651600 (Multiple Dose)

    Observed Accumulation Ratio for Cmax (RacCmax)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  26. Steady State Accumulation Ratio (Rss) for PF-06651600 (Multiple Dose)

    Steady State Accumulation Ratio (Rss)

    Time frame: Days 1, 4, 6, 8, 10, 12 and 14 (0, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 48 hours post dose)

  27. Amount of PF-066561600 Excreted Unchanged (Multiple Dose)

    Concentration in urine.

    Time frame: Day 14 (12, 24 hours post dose)

  28. Change from baseline of BCL2 gene expression in whole blood (Single Dose)

    Time frame: Days -1 and 1 (0, 1, 2, 4, 8, 12 and 24 hours post dose)

  29. Change from baseline of BCL2 gene expression in whole blood (Multiple Dose)

    Time frame: Days 1, 5, 10, 14 (0, 1, 2, 4, 8, 12 and 24 hours post dose), 16, and 28

  30. Change from baseline of IP-10 protein concentration in serum (Multiple Dose)

    Time frame: Days 0, 2, 7, 14 (0, and 16 hours post dose) and 16

  31. Change from baseline of hsCRP protein concentration in serum (Multiple Dose)

    Time frame: Days 0, 2, 7, 14 (0, and 16 hours post dose) and 16

  32. Change from baseline of reticulocyte counts in whole blood (Single Dose)

    Time frame: Days 0, 2, 3, and 7

  33. Change from baseline of neutrophil counts in whole blood (Single Dose)

    Time frame: Days 0, 2, 3, and 7

  34. Change from baseline of hemoglobin level whole blood (Single Dose)

    Time frame: Days 0, 2, 3, and 7

  35. Change from baseline of reticulocyte counts in whole blood (Multiple Dose)

    Time frame: Days 0, 4, 8, 12, 14 (pre-dose) 15, and 28

  36. Change from baseline of neutrophil counts in whole blood (Multiple Dose)

    Time frame: Days 0, 4, 8, 12, 14 (pre-dose) 15, and 28

  37. Change from baseline of hemoglobin level in whole blood (Multiple Dose)

    Time frame: Days 0, 4, 8, 12, 14 (pre-dose) 15, and 28

  38. Renal Clearance (Multiple Dose)

    Time frame: Day 1, Day 14 (12, 24 hours post dose)

  39. Percentage of PF-066561600 Excreted Unchanged (Multiple Dose)

    Concentration in urine.

    Time frame: Day 14 (12, 24 hours post dose)

  40. Change from baseline of IP-10 gene expression in blood (Multiple Dose)

    Time frame: Days 0, 5, 10, 14 (0, 1, 2, 4, 8 and 12 hours post dose) and 16

  41. Change from baseline of IP-10 gene expression in blood (Single Dose)

    Time frame: Days 0, 1 (0, 1, 2, 4, 8 and 12 hours post dose) and 16

07

Study locations

1 site
  • Pfizer Clinical Research Unit
    Brussels, B-1070, Belgium
08

References and documents

Publications

  • Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. doi: 10.1021/acschembio.6b00677. Epub 2016 Nov 10. PubMed 27791347 ↗
09

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Sep 19, 2016, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
10

Registry details

Key details

Study ID
NCT02309827
Lead sponsor
Pfizer
Responsible party
Sponsor
First posted
Dec 5, 2014
Start date
Dec 2014
Primary completion
Apr 2016
Completion
Apr 2016
Last update
Sep 19, 2016

Study contacts

Pfizer CT.gov Call Center
study director · Pfizer

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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