A Phase 1 interventional study of Sirolimus in Transplant Rejection and Renal Transplantation, sponsored by Pfizer. Completed at 2 sites in China. Open to participants aged 18 Years and older. Per ClinicalTrials.gov, last updated 2012-03-01.
Sponsored by Pfizer · Phase 1, Interventional, and Treatment
Sirolimus, 1 mg, white, triangular tablets (Rapamune®) was approved on 03 April 2007 in China for prophylaxis of organ rejection in renal transplantation. A pharmacokinetic (PK) study to be conducted in renal allograft recipients was requested by State Food and Drug Administration (SFDA) to provide further guidance for clinical use.
To minimize risk to patients, this study is designed to collect blood PK samples from renal allograft recipients who are currently under sirolimus (1 mg tablets) treatment with or without concomitant medication(s). PK samples will be collected from these patients to characterize the steady state PK of sirolimus during sirolimus maintenance therapy. This study will not involve any changes to the established treatment regimen for the patients who enroll in the study
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Of its 582 completed or terminated interventional studies of FDA-regulated products, 381 (65%) have results posted.
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Exclusion Criteria:
Subjects must be taking sirolimus (1 mg tablet formulation) with or without concomitant medications, unless specifically excluded below, for prophylaxis of renal rejection.
Drug: Sirolimus
Sirolimus, 1 mg, white, triangular tablets, daily dose, dosages of any of these medications must be stable for at least 2 weeks prior to screening and continue with no change until completion of the last PK sample collection.
Also known as: Rapamune
Maximum Observed Blood Concentration at Steady State (Cmax,ss)
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Time to Reach Maximum Observed Blood Concentration at Steady State (Tmax,ss)
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Observed Blood Trough Concentration at Steady State (Ctrough,ss)
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Average Blood Concentration at Steady State (Cave,ss)
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) at Steady State
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Degree of Fluctuation (DF)
DF, also known as peak to trough fluctuation (PTF) (calculated as \[Cmax minus Ctrough\] divided by Cave), is a unit-less ratio of the Cmax to Ctrough decrease expressed as a fraction of the average concentration during a dosing interval.
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Apparent Oral Clearance (CL/F)
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed.
Time frame: Predose (0 hour) and 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 and 24 hours post dose
Number of Participants With Serum Creatinine Levels More Than (>) 1.3 Times the Upper Limit of Normal
Serum creatinine, an indicator of kidney function, formed from the metabolism of creatine, commonly found in blood, urine, and muscle tissue, is removed from blood by kidneys and excreted in urine. Increased creatinine in blood indicates decreased kidney function. Creatinine levels are age, gender and race dependent as they are related to an individual's muscle mass. Renal transplant recipients may have elevated serum creatinine. For this study an abnormal serum creatinine level is defined as 1.3 times the upper limit of normal (ULN) for the laboratory where the determination was performed.
Time frame: From baseline up to Day 4
Number of Participants With Estimated Glomerular Filtration Rate (GFR) Less Than (<) 60 mL/Min/1.73 m^2
GFR, an index of kidney function, describes flow rate of filtered fluid through the kidney. GFR can be measured directly or estimated using established formulas. GFR was calculated using the Simplified Modification of Diet in Renal Dysfunction (MDRD) GFR equation. Normal GFR is \>90 mL/min/1.73 m\^2; children and older people usually have lower GFR. Often, kidney transplant recipients do not have normal GFRs. Lower values indicate poor kidney function. GFR \<15 mL/min/1.73 m\^2 is consistent with kidney failure. For this posting, the number of subjects with a GFR \<60 mL/min/1.73 m\^2 is listed.
Time frame: From baseline up to Day 4
| Milestone | Sirolimus |
|---|---|
| Started | 24 |
| Completed | 24 |
| Not completed | 0 |
| nanogram per milliliter (ng/mL) | Sirolimus |
|---|---|
| Maximum Observed Blood Concentration at Steady State (Cmax,ss) | 14.07 ± 13.433 |
| hours | Sirolimus |
|---|---|
| Time to Reach Maximum Observed Blood Concentration at Steady State (Tmax,ss) | 2.49 (0.983 to 12.0) |
| ng/mL | Sirolimus |
|---|---|
| Observed Blood Trough Concentration at Steady State (Ctrough,ss) | 5.906 ± 6.2621 |
| ng/mL | Sirolimus |
|---|---|
| Average Blood Concentration at Steady State (Cave,ss) | 8.297 ± 8.7384 |
| nanogram hour per milliliter (ng*h/mL) | Sirolimus |
|---|---|
| Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) at Steady State | 199.3 ± 209.96 |
DF, also known as peak to trough fluctuation (PTF) (calculated as \[Cmax minus Ctrough\] divided by Cave), is a unit-less ratio of the Cmax to Ctrough decrease expressed as a fraction of the average concentration during a dosing interval.
| ratio | Sirolimus |
|---|---|
| Degree of Fluctuation (DF) | 1.064 ± 0.3226 |
Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Clearance was estimated from population pharmacokinetic (PK) modeling. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed.
| liter per hour (L/h) | Sirolimus |
|---|---|
| Apparent Oral Clearance (CL/F) | 10.14 ± 4.3678 |
Serum creatinine, an indicator of kidney function, formed from the metabolism of creatine, commonly found in blood, urine, and muscle tissue, is removed from blood by kidneys and excreted in urine. Increased creatinine in blood indicates decreased kidney function. Creatinine levels are age, gender and race dependent as they are related to an individual's muscle mass. Renal transplant recipients may have elevated serum creatinine. For this study an abnormal serum creatinine level is defined as 1.3 times the upper limit of normal (ULN) for the laboratory where the determination was performed.
| participants | Sirolimus |
|---|---|
| Baseline | 5 |
| Day 4 | 4 |
GFR, an index of kidney function, describes flow rate of filtered fluid through the kidney. GFR can be measured directly or estimated using established formulas. GFR was calculated using the Simplified Modification of Diet in Renal Dysfunction (MDRD) GFR equation. Normal GFR is \>90 mL/min/1.73 m\^2; children and older people usually have lower GFR. Often, kidney transplant recipients do not have normal GFRs. Lower values indicate poor kidney function. GFR \<15 mL/min/1.73 m\^2 is consistent with kidney failure. For this posting, the number of subjects with a GFR \<60 mL/min/1.73 m\^2 is listed.
| participants | Sirolimus |
|---|---|
| Baseline | 7 |
| Day 4 | 7 |
Non-serious events are listed at a 0% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Sirolimus | — | 0/24 (0%) | 0/24 (0%) |
| Age, Customized(participants) | Sirolimus |
|---|---|
| 18 to 44 years | 16 |
| 45 to 64 years | 8 |
| Sex: Female, Male(Participants) | Sirolimus |
|---|---|
| Female | 3 |
| Male | 21 |
This study is completed, as verified in Apr 2011. You cannot join it, but the record below documents what was studied.
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