What question did this study set out to answer?

To determine the safety, tolerance, and preliminary pharmacokinetics of escalating single oral doses of sirolimus in stable renal transplant recipients.

August 1, 1997Therapeutic Drug Monitoring

Kinetics and Dynamics of Single Oral Doses of Sirolimus in Sixteen Renal Transplant Recipients

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To determine the safety, tolerance, and preliminary pharmacokinetics of escalating single oral doses of sirolimus in stable renal transplant recipients.
Randomized phase I trial of 16 stable kidney transplant recipients divided into four ascending dose cohorts: 3 mg/m2, 5 mg/m2, 10 mg/m2, and 15 mg/m2.
Patients in each cohort were randomly assigned to receive either a single oral dose of sirolimus (n = 3) or placebo (n = 1) on a background of standard immunosuppression.
Blood and plasma concentrations were quantified using electrospray-high performance liquid chromatography-mass spectrometry.
Sirolimus demonstrated extensive red blood cell partitioning with a mean blood-to-plasma ratio of 49.1, an oral clearance between 42 and 339 ml/h·kg, and a mean elimination half-life of 56.9 hours (range 43.8–86.5 hours).
Both Cmax and AUC correlated with dose escalation across the 3 to 15 mg/m2 range without altering cyclosporine trough levels or AUCs.
Five of 12 patients receiving sirolimus experienced mild transient adverse events without nephrotoxicity, with one instance of thrombocytopenia at 15 mg/m2 identified as the likely dose-limiting toxicity.

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Implication

Randomized trial demonstrates that single oral doses of sirolimus are safe and dose-proportional in renal transplant recipients, indicating its viability for preventing organ rejection.

Cite This Study

Brattström et al. (1997) studied this question.

synapsesocial.com/papers/6a86d4f2bb0787ff27ca0afc https://doi.org/10.1097/00007691-199708000-00007

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Implication

Randomized trial demonstrates that single oral doses of sirolimus are safe and dose-proportional in renal transplant recipients, indicating its viability for preventing organ rejection.

Kinetics and Dynamics of Single Oral Doses of Sirolimus in Sixteen Renal Transplant Recipients

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Discussion

Implication

Cite This Study

Kinetics and Dynamics of Single Oral Doses of Sirolimus in Sixteen Renal Transplant Recipients

Key Points

Discussion

Implication

Cite This Study

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