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A Study of the Correlation Between Pharmacokinetic and Pharmacodynamic Parameters of CellCept (Mycophenolate Mofetil).

Phase 2
Completed
Conditions
Kidney Transplantation
Interventions
Drug: antibody induction
Drug: corticosteroid
Registration Number
NCT01292226
Lead Sponsor
Hoffmann-La Roche
Brief Summary

This study will evaluate the correlation between the pharmacokinetic and pharmacodynamic parameters of CellCept in patients undergoing primary kidney transplantation, in order to assess the impact on clinical outcome and the risks of acute rejection. All patients will receive oral CellCept, 1g twice daily, and pharmacokinetic and pharmacodynamic parameters will be measured at weeks 2, 4, 12 and 24. The anticipated time on study treatment is 24 weeks.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
45
Inclusion Criteria
  • Adult patients, 18 to 65 years of age
  • Patients undergoing primary kidney transplantation
Exclusion Criteria
  • Recipients of multiple organ transplants
  • Prior therapy with CellCept
  • Presence or history of malignancies, except for successfully treated basal or squamous cell carcinoma of the skin
  • Active peptic ulcer or active serious digestive system disease that may affect the absorption of CellCept

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Mycophenolate Mofetil Monotherapyantibody inductionParticipants received an initial dose of mycophenolate mofetil (MMF), 1 gram (g), orally (PO), twice per day (BID), within 5 days of transplant for 24 weeks. Participants also received concurrent antibody induction, cyclosporine, and corticosteroids as needed according to center's practice.
Mycophenolate Mofetil MonotherapycorticosteroidParticipants received an initial dose of mycophenolate mofetil (MMF), 1 gram (g), orally (PO), twice per day (BID), within 5 days of transplant for 24 weeks. Participants also received concurrent antibody induction, cyclosporine, and corticosteroids as needed according to center's practice.
Mycophenolate Mofetil Monotherapymycophenolate mofetilParticipants received an initial dose of mycophenolate mofetil (MMF), 1 gram (g), orally (PO), twice per day (BID), within 5 days of transplant for 24 weeks. Participants also received concurrent antibody induction, cyclosporine, and corticosteroids as needed according to center's practice.
Mycophenolate Mofetil MonotherapyCyclosporineParticipants received an initial dose of mycophenolate mofetil (MMF), 1 gram (g), orally (PO), twice per day (BID), within 5 days of transplant for 24 weeks. Participants also received concurrent antibody induction, cyclosporine, and corticosteroids as needed according to center's practice.
Primary Outcome Measures
NameTimeMethod
Percentage of Participants With Acute RejectionDay 1, Weeks 2, 4, 12, 24, and 28

Diagnosis of acute rejection was suspected in any participant with an increase in serum creatinine greater than or equal to (≥) 25 percent (%). All suspected acute rejections were confirmed by biopsy. The start date of acute rejection was identified as the date of biopsy.

Time to RejectionDay 1, Weeks 2, 4, 12, 24, and 28

The mean time, in days, from the date of enrollment to date of biopsy confirming acute rejection.

Percentage of Participants With Biopsy-Proven Acute Rejection (BPAR)Day 1, Weeks 2, 4, 12, 24, and 28

BPAR was defined according to 1997 Banff Criteria as a biopsy Banff grade of IA, IB, IIA, IIB, or III. Grade IA was defined as significant interstitial infiltration with greater than (\>)25% of parenchyma affected, and foci of moderate tubulitis with \>4 mononuclear cells per tubular cross section or group of 10 tubular cells. Grade IB was defined as significant interstitial infiltration with \>25% parenchyma affected, and foci of severe tubulitis with \>10% mononuclear cells per tubular cross section or group of 10 tubular cells. Grade IIA was defined as mild to moderate intimal arteritis. Grade IIB was defined as severe intimal arteritis comprising \>25% of the luminal area. Grade III was defined as transmural arteritis and/or arterial fibrinoid changes and necrosis of medial smooth muscle cells.

Secondary Outcome Measures
NameTimeMethod
Percentage of Participants With Hematologic ToxicityBL and Weeks 2, 4, 12, 24, and 28 (Safety Follow-Up)

Hematological toxicities graded according to WHO worst grade observed (Grade 1=mild, Grade 2=moderate).

Spearman's Rank Correlation Coefficient Between MPA Levels and IMPDH ActivityBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH I Expression and MPA LevelsBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH I Expression and Free FractionBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH II Expression and MPA LevelsBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH II Expression and Free FractionBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH Inhibition and Risk of Acute RejectionBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH Expression and Risk of InfectionBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH Expression and Risk of Hematologic ToxicityBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between IMPDH Expression and Risk of Gastrointestinal ToxicityBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between MPA Levels and Risk of Hematologic ToxicityBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Percentage of Participants With Graft LossDay 1, Weeks 2, 4, 12, 24, and 28

An allograft was presumed to be lost if a participant started dialysis and was not able to subsequently be removed from dialysis.

Percentage of Participants SurvivingDay 1, Weeks 2, 4, 12, 24, and 28
Total Mycophenolate Acid (MPA) by Visit and TimepointWeeks 2, 4, 12, 24, and 28 (Safety Follow-Up Visit), and any unscheduled visits

Drug quantification of total MPA (micrograms per milliliter \[mcg/mL\]) in the plasma was measured at time (T) = 0 minutes (min), 40 mins, and 120 mins.

Free MPA (mcg/mL) by VisitWeeks 2, 4, 12, 24, safety follow-up (Week 28), and any unscheduled visits

Drug quantification of free MPA in the plasma was measured at T = 0, 40, and 120 mins.

MPA Area Under the Concentration - Time Curve From Time 0 to 12 Hours (AUC0-12) (mcg/mL) by VisitPredose and 40 minutes and 2 hours postdose at Weeks 2, 4, 12, and 24, and at the Safety follow-up (Week 28)

The AUC0-12 of MPA was estimated on the validated limited sampling strategy, AUC (milligrams multiplied by height over liter \[mg.h/L\]) = 7.182 + 4.607 multiplied by (\*) concentration at 0 minutes (C0)+ 0.998 \* the concentration at 40 minutes (C0.67) + 2.149 \* the concentration at 120 minutes (C2).

Inosine MonoPhosphate DeHydrogenase (IMPDH) Activity by Visit and TimepointBL and Weeks 2, 4, 12, and 24, and safety follow-up (Week 28) and any unscheduled visits

IMPDH activity in peripheral blood mononuclear cells (PBMCs) was measured at 2 timepoints per visit, 0 and 120 minutes and presented in enzyme units. The unit of measure of enzyme activity is "U". One U is defined as the amount of the enzyme that produces a certain amount of enzymatic activity that is, the amount that catalyzes the conversion of 1 micro mole of substrate per minute under pre-specified conditions (temperature, pH).

IMPDH Expression I by Visit and TimepointBL and Weeks 2, 4, 12, and 24, and safety follow-up (Week 28) and any unscheduled visits

IMPDH I gene expression was measured by real time polymerase chain reaction (QRT-PCR) based cytokine measurement of PBMCs at 2 timepoints per visit, 0 and 120 minutes and expressed as number of messenger ribonucleic acid (mRNA) copies per cell (copies/cell).

IMPDH Expression II by Visit and TimepointBL and Weeks 2, 4, 12, and 24, and safety follow-up (Week 28) and any unscheduled visits

IMPDH II gene expression was measured by QRT-PCR based cytokine measurement of PBMCs at 2 timepoints per visit, 0 and 120 minutes and expressed as number of mRNA copies/cell.

Interleukin 8 (IL-8) Expression by Visit and TimepointBL and Weeks 2, 4, 12, and 24, and safety follow-up (Week 28) and any unscheduled visits

IL-8 gene expression was measured by QRT-PCR based cytokine measurement of PBMCs at 2 timepoints per visit, 0 and 120 minutes and expressed as number of mRNA copies/cell.

Tumor Necrosis Factor (TNF) Expression by Visit and TimepointBL and Weeks 2, 4, 12, and 24, and safety follow-up (Week 28) and any unscheduled visits

TNF gene expression was measured by QRT-PCR based cytokine measurement of PBMCs at 2 timepoints per visit, 0 and 120 minutes and expressed as number of mRNA copies/cell.

Percentage of Participants With InfectionBL and Weeks 2, 4, 12, 24, and 28 (Safety Follow-Up)

Infections were graded according to the World Health Organization (WHO) worst grade observed.

Percentage of Participants With Gastrointestinal ToxicitiesBL and Weeks 2, 4, 12, 24, and 28 (Safety Follow-up Visit)

Gastrointestinal adverse events (AEs) according to WHO worst grade observed.

Spearman's Rank Correlation Coefficient Between MPA Levels and Risk of InfectionBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

Spearman's Rank Correlation Coefficient Between MPA Levels and Risk of Gastrointestinal ToxicityBL and Weeks 2, 4, 12, and 24

The Spearman's rank correlation coefficient was computed by ranking the data from 2 time points, 0 minutes and 120 minutes, and using the ranks in the Pearson product-moment correlation formula. In case of ties, the averaged ranks were used.

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