An evaluation of sirolimus in renal transplantation

Fabian Halleck, Michael Duerr, Johannes Waiser, Lu Yu Huber, Mareen Matz, Susanne Brakemeier, Lutz Liefeldt, Hans Hellmut Neumayer, Klemens Budde

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Introduction: Sirolimus is a powerful antiproliferative immunosuppressive drug approved for the prevention of kidney allograft rejection. By its unique mechanism of action, sirolimus provides a multitude of clinical potential and has been used effectively in different drug combinations. Extensive experience has been gained regarding the best timing of its application, side effect profile and potential benefits and limitations compared with other immunosuppressive drugs. Areas covered: The authors evaluate the recent experience with sirolimus in kidney transplantation. Pivotal randomized controlled trials were used to provide an overview with special attention to pharmacokinetic and dynamic aspects of sirolimus, its current clinical use as well as perspectives for its future role. Expert opinion: Sirolimus enriches the possibilities of immunosuppressive therapies after renal transplantation. Beneficial effects toward kidney function by allowing CNI sparing, lower incidence of malignancies and less viral infections have been suggested. Sirolimus should be used cautiously in de novo patients for reasons of wound healing. An early conversion to a sirolimus-based CNI-free regimen has shown promising results, whereas late conversion is more challenging. Finally, sirolimus-associated side effects are causing tolerability concerns and frequent discontinuations. Future research should aim to better define the therapeutic window and those patients most likely to benefit.

Original languageEnglish (US)
Pages (from-to)1337-1356
Number of pages20
JournalExpert Opinion on Drug Metabolism and Toxicology
Volume8
Issue number10
DOIs
StatePublished - Oct 1 2012

Fingerprint

Sirolimus
Kidney Transplantation
Immunosuppressive Agents
Kidney
Pharmacokinetics
Expert Testimony
Virus Diseases
Drug Combinations
Pharmaceutical Preparations
Wound Healing
Allografts
Randomized Controlled Trials
Incidence
Therapeutics

Keywords

  • Calcineurin inhibitors
  • Kidney transplantation
  • MTOR inhibitors
  • Rapamycin
  • Sirolimus

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology

Cite this

Halleck, F., Duerr, M., Waiser, J., Huber, L. Y., Matz, M., Brakemeier, S., ... Budde, K. (2012). An evaluation of sirolimus in renal transplantation. Expert Opinion on Drug Metabolism and Toxicology, 8(10), 1337-1356. https://doi.org/10.1517/17425255.2012.719874

An evaluation of sirolimus in renal transplantation. / Halleck, Fabian; Duerr, Michael; Waiser, Johannes; Huber, Lu Yu; Matz, Mareen; Brakemeier, Susanne; Liefeldt, Lutz; Neumayer, Hans Hellmut; Budde, Klemens.

In: Expert Opinion on Drug Metabolism and Toxicology, Vol. 8, No. 10, 01.10.2012, p. 1337-1356.

Research output: Contribution to journalArticle

Halleck, F, Duerr, M, Waiser, J, Huber, LY, Matz, M, Brakemeier, S, Liefeldt, L, Neumayer, HH & Budde, K 2012, 'An evaluation of sirolimus in renal transplantation', Expert Opinion on Drug Metabolism and Toxicology, vol. 8, no. 10, pp. 1337-1356. https://doi.org/10.1517/17425255.2012.719874
Halleck F, Duerr M, Waiser J, Huber LY, Matz M, Brakemeier S et al. An evaluation of sirolimus in renal transplantation. Expert Opinion on Drug Metabolism and Toxicology. 2012 Oct 1;8(10):1337-1356. https://doi.org/10.1517/17425255.2012.719874
Halleck, Fabian ; Duerr, Michael ; Waiser, Johannes ; Huber, Lu Yu ; Matz, Mareen ; Brakemeier, Susanne ; Liefeldt, Lutz ; Neumayer, Hans Hellmut ; Budde, Klemens. / An evaluation of sirolimus in renal transplantation. In: Expert Opinion on Drug Metabolism and Toxicology. 2012 ; Vol. 8, No. 10. pp. 1337-1356.
@article{dd5ac753549142918de1f5abfaf025fc,
title = "An evaluation of sirolimus in renal transplantation",
abstract = "Introduction: Sirolimus is a powerful antiproliferative immunosuppressive drug approved for the prevention of kidney allograft rejection. By its unique mechanism of action, sirolimus provides a multitude of clinical potential and has been used effectively in different drug combinations. Extensive experience has been gained regarding the best timing of its application, side effect profile and potential benefits and limitations compared with other immunosuppressive drugs. Areas covered: The authors evaluate the recent experience with sirolimus in kidney transplantation. Pivotal randomized controlled trials were used to provide an overview with special attention to pharmacokinetic and dynamic aspects of sirolimus, its current clinical use as well as perspectives for its future role. Expert opinion: Sirolimus enriches the possibilities of immunosuppressive therapies after renal transplantation. Beneficial effects toward kidney function by allowing CNI sparing, lower incidence of malignancies and less viral infections have been suggested. Sirolimus should be used cautiously in de novo patients for reasons of wound healing. An early conversion to a sirolimus-based CNI-free regimen has shown promising results, whereas late conversion is more challenging. Finally, sirolimus-associated side effects are causing tolerability concerns and frequent discontinuations. Future research should aim to better define the therapeutic window and those patients most likely to benefit.",
keywords = "Calcineurin inhibitors, Kidney transplantation, MTOR inhibitors, Rapamycin, Sirolimus",
author = "Fabian Halleck and Michael Duerr and Johannes Waiser and Huber, {Lu Yu} and Mareen Matz and Susanne Brakemeier and Lutz Liefeldt and Neumayer, {Hans Hellmut} and Klemens Budde",
year = "2012",
month = "10",
day = "1",
doi = "10.1517/17425255.2012.719874",
language = "English (US)",
volume = "8",
pages = "1337--1356",
journal = "Expert Opinion on Drug Metabolism and Toxicology",
issn = "1742-5255",
publisher = "Informa Healthcare",
number = "10",

}

TY - JOUR

T1 - An evaluation of sirolimus in renal transplantation

AU - Halleck, Fabian

AU - Duerr, Michael

AU - Waiser, Johannes

AU - Huber, Lu Yu

AU - Matz, Mareen

AU - Brakemeier, Susanne

AU - Liefeldt, Lutz

AU - Neumayer, Hans Hellmut

AU - Budde, Klemens

PY - 2012/10/1

Y1 - 2012/10/1

N2 - Introduction: Sirolimus is a powerful antiproliferative immunosuppressive drug approved for the prevention of kidney allograft rejection. By its unique mechanism of action, sirolimus provides a multitude of clinical potential and has been used effectively in different drug combinations. Extensive experience has been gained regarding the best timing of its application, side effect profile and potential benefits and limitations compared with other immunosuppressive drugs. Areas covered: The authors evaluate the recent experience with sirolimus in kidney transplantation. Pivotal randomized controlled trials were used to provide an overview with special attention to pharmacokinetic and dynamic aspects of sirolimus, its current clinical use as well as perspectives for its future role. Expert opinion: Sirolimus enriches the possibilities of immunosuppressive therapies after renal transplantation. Beneficial effects toward kidney function by allowing CNI sparing, lower incidence of malignancies and less viral infections have been suggested. Sirolimus should be used cautiously in de novo patients for reasons of wound healing. An early conversion to a sirolimus-based CNI-free regimen has shown promising results, whereas late conversion is more challenging. Finally, sirolimus-associated side effects are causing tolerability concerns and frequent discontinuations. Future research should aim to better define the therapeutic window and those patients most likely to benefit.

AB - Introduction: Sirolimus is a powerful antiproliferative immunosuppressive drug approved for the prevention of kidney allograft rejection. By its unique mechanism of action, sirolimus provides a multitude of clinical potential and has been used effectively in different drug combinations. Extensive experience has been gained regarding the best timing of its application, side effect profile and potential benefits and limitations compared with other immunosuppressive drugs. Areas covered: The authors evaluate the recent experience with sirolimus in kidney transplantation. Pivotal randomized controlled trials were used to provide an overview with special attention to pharmacokinetic and dynamic aspects of sirolimus, its current clinical use as well as perspectives for its future role. Expert opinion: Sirolimus enriches the possibilities of immunosuppressive therapies after renal transplantation. Beneficial effects toward kidney function by allowing CNI sparing, lower incidence of malignancies and less viral infections have been suggested. Sirolimus should be used cautiously in de novo patients for reasons of wound healing. An early conversion to a sirolimus-based CNI-free regimen has shown promising results, whereas late conversion is more challenging. Finally, sirolimus-associated side effects are causing tolerability concerns and frequent discontinuations. Future research should aim to better define the therapeutic window and those patients most likely to benefit.

KW - Calcineurin inhibitors

KW - Kidney transplantation

KW - MTOR inhibitors

KW - Rapamycin

KW - Sirolimus

UR - http://www.scopus.com/inward/record.url?scp=84866524136&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84866524136&partnerID=8YFLogxK

U2 - 10.1517/17425255.2012.719874

DO - 10.1517/17425255.2012.719874

M3 - Article

VL - 8

SP - 1337

EP - 1356

JO - Expert Opinion on Drug Metabolism and Toxicology

JF - Expert Opinion on Drug Metabolism and Toxicology

SN - 1742-5255

IS - 10

ER -