This was a Phase 1 dose escalation study to evaluate the safety, tolerability and pharmacokinetics of 28-day treatment of CP-690,550 in stable renal allograft recipients. In Stage 1, ascending doses of CP-690,550 were to be administered sequentially to 3-4 cohorts of subjects. After Stage 1, one dose level was to be selected for dosing in an expanded cohort in Stage 2.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
DOUBLE
Enrollment
28
Placebo tables twice daily (BID) for 28 days
CP-690,550 5 mg BID for 28 days
CP-690,550 15 mg BID for 28 days
Pfizer Investigational Site
Birmingham, Alabama, United States
Pfizer Investigational Site
Birmingham, Alabama, United States
Pfizer Investigational Site
Birmingham, Alabama, United States
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) For CP-690,550
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast).
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) at Steady State For CP-690,550
Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) at steady state.
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29
Area Under the Curve From Time Zero to 12 Hour Concentration [AUC(0-12)] at Steady State For CP-690,550
Area under the plasma concentration time-curve from zero to 12 hour concentration \[AUC(0-12)\] at steady state.
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 29
Maximum Observed Plasma Concentration (Cmax) For CP-690,550
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1
Maximum Observed Plasma Concentration (Cmax) at Steady State For CP-690,550
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29
Time to Reach Maximum Observed Plasma Concentration (Tmax) For CP-690,550
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1
Time to Reach Maximum Observed Plasma Concentration (Tmax) at Steady State For CP-690,550
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29
Accumulation Ratio (Rac) For CP-690,550
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CP-690,550 30 mg BID for 28 days
Pfizer Investigational Site
Los Angeles, California, United States
Pfizer Investigational Site
Indianapolis, Indiana, United States
Pfizer Investigational Site
Minneapolis, Minnesota, United States
Pfizer Investigational Site
St Louis, Missouri, United States
Pfizer Investigational Site
St Louis, Missouri, United States
Pfizer Investigational Site
Livingston, New Jersey, United States
Pfizer Investigational Site
Madison, Wisconsin, United States
...and 1 more locations
Rac obtained from AUC(0-12) (Day 29) divided by AUC(0-12) (Day 1).
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1 and 29
Plasma Decay Half-Life (t1/2) For CP-690,550
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1
Plasma Decay Half-Life (t1/2) at Steady State For CP-690,550
Plasma decay half-life is the time measured for the plasma concentration to decrease by one half at steady state.
Time frame: 0 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29
Mycophenolic Acid (MPA) Plasma Trough Concentration at Baseline
Pro-drug MMF was metabolically converted to active form MPA in the liver. The baseline for MPA trough concentrations was defined as the average of the values obtained at Screening and on Day 1 (pre-dose). MPA levels were assessed at different visits to assess change in MPA trough levels due to CP-690,550 exposure.
Time frame: Screening, 0 hour (pre-dose) on Day 1
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 8
Pro-drug MMF was metabolically converted to active form MPA in the liver. MPA levels were assessed at different visits to assess change in MPA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 8
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 15
Pro-drug MMF was metabolically converted to active form MPA in the liver. MPA levels were assessed at different visits to assess change in MPA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 15
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 29
Pro-drug MMF was metabolically converted to active form MPA in the liver. MPA levels were assessed at different visits to assess change in MPA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 29
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 57
Pro-drug MMF was metabolically converted to active form MPA in the liver. MPA levels were assessed at different visits to assess change in MPA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 57
Cyclosporine (CsA) Plasma Trough Concentration at Baseline
The baseline for CsA trough concentrations was defined as the average of the values obtained at Screening and on Day 1 (pre-dose). CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Time frame: Screening, 0 hour (pre-dose) on Day 1
Cyclosporine (CsA) Plasma Trough Concentration at Day 8
CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 8
Cyclosporine (CsA) Plasma Trough Concentration at Day 15
CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 15
Cyclosporine (CsA) Plasma Trough Concentration at Day 29
CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 29
Cyclosporine (CsA) Plasma Trough Concentration at Day 57
CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 57
Tacrolimus (TAC) Plasma Trough Concentration at Baseline
The baseline for TAC trough concentrations was defined as the average of the values obtained at Screening and on Day 1 (pre-dose). TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Time frame: Screening, 0 hour (pre-dose) on Day 1
Tacrolimus (TAC) Plasma Trough Concentration at Day 8
TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 8
Tacrolimus (TAC) Plasma Trough Concentration at Day 15
TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 15
Tacrolimus (TAC) Plasma Trough Concentration at Day 29
TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 29
Tacrolimus (TAC) Plasma Trough Concentration at Day 57
TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Time frame: 0 hour (pre-dose) on Day 57