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A Study Of CP-690,550 In Stable Kidney Transplant Patients

Phase 1, Placebo-controlled, Randomized, Sequential, Parallel-group, Dose Escalation Study to Evaluate 28-day Multiple Dose Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of CP-690,550 in Stable Renal Allograft Recipients

Status
Completed
Phases
Phase 1
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT01710033
Enrollment
28
Registered
2012-10-18
Start date
2003-09-30
Completion date
2005-04-30
Last updated
2012-12-26

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Kidney Transplant

Keywords

CP-690,550, kidney transplant

Brief summary

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.

Interventions

DRUGPlacebo

Placebo tables twice daily (BID) for 28 days

DRUGCP-690,550 5 mg BID

CP-690,550 5 mg BID for 28 days

DRUGCP-690,550 15 mg BID

CP-690,550 15 mg BID for 28 days

DRUGCP-690,550 30 mg BID

CP-690,550 30 mg BID for 28 days

Sponsors

Pfizer
Lead SponsorINDUSTRY

Study design

Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
BASIC_SCIENCE
Masking
DOUBLE (Subject, Investigator)

Eligibility

Sex/Gender
ALL
Age
18 Years to 70 Years
Healthy volunteers
No

Inclusion criteria

* Medically stable kidney transplant patients 6 or more months after transplantation. * Subjects must be on mycophenolate mofetil 1-2 gm daily * In Cohort 3 (and 4, if conducted) in Stage 1 and the expanded cohort in Stage 2, subjects must be on a calcineurin inhibitor-free regimen.

Exclusion criteria

* Any rejection episodes in the preceding 3 months. * Treated with Thymoglobulin or OKT3 for acute rejection in the past 6 months.

Design outcomes

Primary

MeasureTime frameDescription
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) For CP-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast).
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) at Steady State For CP-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) at steady state.
Area Under the Curve From Time Zero to 12 Hour Concentration [AUC(0-12)] at Steady State For CP-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 29Area under the plasma concentration time-curve from zero to 12 hour concentration \[AUC(0-12)\] at steady state.
Maximum Observed Plasma Concentration (Cmax) For CP-690,5500 (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-690,5500 (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-690,5500 (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-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29—
Accumulation Ratio (Rac) For CP-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1 and 29Rac obtained from AUC(0-12) (Day 29) divided by AUC(0-12) (Day 1).
Plasma Decay Half-Life (t1/2) For CP-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12 hours post-dose on Day 1Plasma decay half-life is the time measured for the plasma concentration to decrease by one half.
Plasma Decay Half-Life (t1/2) at Steady State For CP-690,5500 (pre-dose), 0.5, 1, 2, 4, 8, 10, 12, 24 hours post-dose on Day 29Plasma decay half-life is the time measured for the plasma concentration to decrease by one half at steady state.
Mycophenolic Acid (MPA) Plasma Trough Concentration at BaselineScreening, 0 hour (pre-dose) on Day 1Pro-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.
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 80 hour (pre-dose) on Day 8Pro-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.
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 150 hour (pre-dose) on Day 15Pro-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.
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 290 hour (pre-dose) on Day 29Pro-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.
Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 570 hour (pre-dose) on Day 57Pro-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.
Cyclosporine (CsA) Plasma Trough Concentration at BaselineScreening, 0 hour (pre-dose) on Day 1The 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.
Cyclosporine (CsA) Plasma Trough Concentration at Day 80 hour (pre-dose) on Day 8CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Cyclosporine (CsA) Plasma Trough Concentration at Day 150 hour (pre-dose) on Day 15CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Cyclosporine (CsA) Plasma Trough Concentration at Day 290 hour (pre-dose) on Day 29CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Cyclosporine (CsA) Plasma Trough Concentration at Day 570 hour (pre-dose) on Day 57CsA levels were assessed at different visits to assess change in CsA trough levels due to CP-690,550 exposure.
Tacrolimus (TAC) Plasma Trough Concentration at BaselineScreening, 0 hour (pre-dose) on Day 1The 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.
Tacrolimus (TAC) Plasma Trough Concentration at Day 80 hour (pre-dose) on Day 8TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Tacrolimus (TAC) Plasma Trough Concentration at Day 150 hour (pre-dose) on Day 15TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Tacrolimus (TAC) Plasma Trough Concentration at Day 290 hour (pre-dose) on Day 29TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.
Tacrolimus (TAC) Plasma Trough Concentration at Day 570 hour (pre-dose) on Day 57TAC levels were assessed at different visits to assess change in TAC trough levels due to CP-690,550 exposure.

Countries

United States

Participant flow

Participants by arm

ArmCount
Placebo, Stage 1
Placebo matched to CP-690,550 tablet orally twice daily up to Day 28 followed by single oral dose on Day 29 in stable renal transplant recipients, receiving maintenance immunosuppression therapy (MMF) with or without calcineurin inhibitor (CsA or TAC) as per local clinical practice in Stage 1.
6
CP-690,550 5 mg, Stage 1
CP-690,550 5 milligram (mg) tablet orally twice daily up to Day 28 followed by single oral dose on Day 29 in stable renal transplant recipients, receiving maintenance immunosuppression therapy (MMF), calcineurin inhibitor (CsA) as per local clinical practice in Stage 1.
6
CP-690,550 15 mg, Stage 1
CP-690,550 15 mg tablet orally twice daily up to Day 28 followed by single oral dose on Day 29 in stable renal transplant recipients, receiving maintenance immunosuppression therapy (MMF), calcineurin inhibitor (CsA or TAC) as per local clinical practice in Stage 1.
6
CP-690,550 30 mg, Stage 1 And 2
CP-690,550 30 mg tablet orally twice daily up to Day 28 followed by single oral dose on Day 29 in stable renal transplant recipients, receiving maintenance immunosuppression therapy (MMF) as per local clinical practice in Stage 1 and 2.
10
Total28

Withdrawals & dropouts

PeriodReasonFG000FG001FG002FG003FG004
Stage 2Adverse Event00001

Baseline characteristics

CharacteristicPlacebo, Stage 1CP-690,550 5 mg, Stage 1CP-690,550 15 mg, Stage 1CP-690,550 30 mg, Stage 1 And 2Total
Age Continuous54.5 years
STANDARD_DEVIATION 15
53.0 years
STANDARD_DEVIATION 15.5
46.0 years
STANDARD_DEVIATION 17.8
54.2 years
STANDARD_DEVIATION 14.3
52.3 years
STANDARD_DEVIATION 15
Sex: Female, Male
Female
2 Participants1 Participants3 Participants2 Participants8 Participants
Sex: Female, Male
Male
4 Participants5 Participants3 Participants8 Participants20 Participants

Adverse events

Event typeEG000
affected / at risk
EG001
affected / at risk
EG002
affected / at risk
EG003
affected / at risk
deaths
Total, all-cause mortality
— / —— / —— / —— / —
other
Total, other adverse events
5 / 65 / 65 / 68 / 10
serious
Total, serious adverse events
1 / 60 / 62 / 61 / 10

Outcome results

Primary

Accumulation Ratio (Rac) For CP-690,550

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Accumulation Ratio (Rac) For CP-690,5501.48 ratioStandard Deviation 0.467
CP-690,550 15 mg, Stage 1Accumulation Ratio (Rac) For CP-690,5501.39 ratioStandard Deviation 0.245
CP-690,550 30 mg, Stage 1 And 2Accumulation Ratio (Rac) For CP-690,5501.22 ratioStandard Deviation 0.182
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Area Under the Curve From Time Zero to 12 Hour Concentration [AUC(0-12)] at Steady State For CP-690,550273 ng*hr/mLStandard Deviation 132
CP-690,550 15 mg, Stage 1Area Under the Curve From Time Zero to 12 Hour Concentration [AUC(0-12)] at Steady State For CP-690,5501090 ng*hr/mLStandard Deviation 150
CP-690,550 30 mg, Stage 1 And 2Area Under the Curve From Time Zero to 12 Hour Concentration [AUC(0-12)] at Steady State For CP-690,5501420 ng*hr/mLStandard Deviation 253
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) at Steady State For CP-690,550319 ng*hr/mLStandard Deviation 175
CP-690,550 15 mg, Stage 1Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) at Steady State For CP-690,5501300 ng*hr/mLStandard Deviation 241
CP-690,550 30 mg, Stage 1 And 2Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) at Steady State For CP-690,5501560 ng*hr/mLStandard Deviation 311
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) For CP-690,550183 nanogram*hour per milliliter (ng*hr/mL)Standard Deviation 75.3
CP-690,550 15 mg, Stage 1Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) For CP-690,550754 nanogram*hour per milliliter (ng*hr/mL)Standard Deviation 182
CP-690,550 30 mg, Stage 1 And 2Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) For CP-690,5501200 nanogram*hour per milliliter (ng*hr/mL)Standard Deviation 266
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Baseline249.50 ng/mL—
CP-690,550 15 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Baseline81.00 ng/mLStandard Deviation 41.99
CP-690,550 30 mg, Stage 1 And 2Cyclosporine (CsA) Plasma Trough Concentration at Baseline173.00 ng/mLStandard Deviation 51.11
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 15207.00 ng/mL—
CP-690,550 15 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 1586.60 ng/mLStandard Deviation 43.71
CP-690,550 30 mg, Stage 1 And 2Cyclosporine (CsA) Plasma Trough Concentration at Day 15160.33 ng/mLStandard Deviation 24.58
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 29226.00 ng/mL—
CP-690,550 15 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 2996.00 ng/mLStandard Deviation 53.43
CP-690,550 30 mg, Stage 1 And 2Cyclosporine (CsA) Plasma Trough Concentration at Day 29125.00 ng/mLStandard Deviation 22.34
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 57292.00 ng/mL—
CP-690,550 15 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 5791.20 ng/mLStandard Deviation 72.71
CP-690,550 30 mg, Stage 1 And 2Cyclosporine (CsA) Plasma Trough Concentration at Day 57152.00 ng/mLStandard Deviation 43.28
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 8137.00 ng/mL—
CP-690,550 15 mg, Stage 1Cyclosporine (CsA) Plasma Trough Concentration at Day 877.25 ng/mLStandard Deviation 47.28
CP-690,550 30 mg, Stage 1 And 2Cyclosporine (CsA) Plasma Trough Concentration at Day 8134.00 ng/mLStandard Deviation 17.78
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Maximum Observed Plasma Concentration (Cmax) at Steady State For CP-690,55052.2 ng/mLStandard Deviation 15.2
CP-690,550 15 mg, Stage 1Maximum Observed Plasma Concentration (Cmax) at Steady State For CP-690,550220 ng/mLStandard Deviation 39.4
CP-690,550 30 mg, Stage 1 And 2Maximum Observed Plasma Concentration (Cmax) at Steady State For CP-690,550351 ng/mLStandard Deviation 46.3
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Maximum Observed Plasma Concentration (Cmax) For CP-690,55041.0 nanogram per milliliter (ng/mL)Standard Deviation 14.9
CP-690,550 15 mg, Stage 1Maximum Observed Plasma Concentration (Cmax) For CP-690,550140 nanogram per milliliter (ng/mL)Standard Deviation 34.5
CP-690,550 30 mg, Stage 1 And 2Maximum Observed Plasma Concentration (Cmax) For CP-690,550325 nanogram per milliliter (ng/mL)Standard Deviation 113
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Baseline2.73 Milligram per Liter (mg/L)Standard Deviation 1.23
CP-690,550 15 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Baseline2.18 Milligram per Liter (mg/L)Standard Deviation 1.8
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Baseline1.84 Milligram per Liter (mg/L)Standard Deviation 1.13
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Baseline2.43 Milligram per Liter (mg/L)Standard Deviation 1.8
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 153.15 mg/LStandard Deviation 1.75
CP-690,550 15 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 152.36 mg/LStandard Deviation 2.21
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 151.48 mg/LStandard Deviation 0.63
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 152.74 mg/LStandard Deviation 1.52
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 292.61 mg/LStandard Deviation 1.77
CP-690,550 15 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 292.68 mg/LStandard Deviation 2
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 294.30 mg/LStandard Deviation 3.88
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 293.24 mg/LStandard Deviation 1.71
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 572.60 mg/LStandard Deviation 1.56
CP-690,550 15 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 572.89 mg/LStandard Deviation 2.75
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 571.75 mg/LStandard Deviation 1.1
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 572.67 mg/LStandard Deviation 1.87
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 83.25 mg/LStandard Deviation 2.77
CP-690,550 15 mg, Stage 1Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 82.11 mg/LStandard Deviation 2.01
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 81.29 mg/LStandard Deviation 0.48
CP-690,550 30 mg, Stage 1 And 2Mycophenolic Acid (MPA) Plasma Trough Concentration at Day 82.56 mg/LStandard Deviation 1.62
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Plasma Decay Half-Life (t1/2) at Steady State For CP-690,5505.18 hoursStandard Deviation 2
CP-690,550 15 mg, Stage 1Plasma Decay Half-Life (t1/2) at Steady State For CP-690,5505.15 hoursStandard Deviation 1.12
CP-690,550 30 mg, Stage 1 And 2Plasma Decay Half-Life (t1/2) at Steady State For CP-690,5503.71 hoursStandard Deviation 0.201
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Plasma Decay Half-Life (t1/2) For CP-690,5503.36 hoursStandard Deviation 0.869
CP-690,550 15 mg, Stage 1Plasma Decay Half-Life (t1/2) For CP-690,550NA hours—
CP-690,550 30 mg, Stage 1 And 2Plasma Decay Half-Life (t1/2) For CP-690,5502.94 hoursStandard Deviation 0.62
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Baseline6.75 ng/mLStandard Deviation 2.47
CP-690,550 15 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Baseline7.17 ng/mLStandard Deviation 1.76
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 158.00 ng/mLStandard Deviation 2.83
CP-690,550 15 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 156.67 ng/mLStandard Deviation 2.08
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 297.00 ng/mLStandard Deviation 2.83
CP-690,550 15 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 2912.67 ng/mLStandard Deviation 4.51
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 575.00 ng/mLStandard Deviation 1.41
CP-690,550 15 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 576.33 ng/mLStandard Deviation 0.58
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEAN)Dispersion
CP-690,550 5 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 87.50 ng/mLStandard Deviation 2.12
CP-690,550 15 mg, Stage 1Tacrolimus (TAC) Plasma Trough Concentration at Day 88.00 ng/mLStandard Deviation 1
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEDIAN)
CP-690,550 5 mg, Stage 1Time to Reach Maximum Observed Plasma Concentration (Tmax) at Steady State For CP-690,5500.75 hours
CP-690,550 15 mg, Stage 1Time to Reach Maximum Observed Plasma Concentration (Tmax) at Steady State For CP-690,5500.50 hours
CP-690,550 30 mg, Stage 1 And 2Time to Reach Maximum Observed Plasma Concentration (Tmax) at Steady State For CP-690,5500.50 hours
Primary

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

Population: Analysis population included all randomized participants who received at least 1 dose of study treatment. Here N (Number of Participants Analyzed) signifies participants who were evaluable for this measure.

ArmMeasureValue (MEDIAN)
CP-690,550 5 mg, Stage 1Time to Reach Maximum Observed Plasma Concentration (Tmax) For CP-690,5500.75 hours
CP-690,550 15 mg, Stage 1Time to Reach Maximum Observed Plasma Concentration (Tmax) For CP-690,5501.50 hours
CP-690,550 30 mg, Stage 1 And 2Time to Reach Maximum Observed Plasma Concentration (Tmax) For CP-690,5500.50 hours

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026