Old and New Calcineurin Inhibitors in Lupus Nephritis

Calcineurin inhibitors (CNIs) are drugs that inhibit calcineurin, a key phosphatase that dephosphorylates a transcription factor called the nuclear factor of activated T cells (NFAT), allowing its translocation into the nucleus of quiescent T cells. In the nucleus, NFAT activates interleukin 2, whic...

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Autores principales:	Claudio Ponticelli, Francesco Reggiani, Gabriella Moroni
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	lupus nephritis proteinuria calcineurin inhibitors cyclosporine tacrolimus voclosporin Medicine R
Acceso en línea:	https://doaj.org/article/0934bce1493d4d1f850c6a2ebc291c97
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spelling	oai:doaj.org-article:0934bce1493d4d1f850c6a2ebc291c972021-11-11T17:30:14ZOld and New Calcineurin Inhibitors in Lupus Nephritis10.3390/jcm102148322077-0383https://doaj.org/article/0934bce1493d4d1f850c6a2ebc291c972021-10-01T00:00:00Zhttps://www.mdpi.com/2077-0383/10/21/4832https://doaj.org/toc/2077-0383Calcineurin inhibitors (CNIs) are drugs that inhibit calcineurin, a key phosphatase that dephosphorylates a transcription factor called the nuclear factor of activated T cells (NFAT), allowing its translocation into the nucleus of quiescent T cells. In the nucleus, NFAT activates interleukin 2, which stimulates the proliferation and differentiation of T-cells. CNIs can also stabilize the actin cytoskeleton of podocytes reducing proteinuria. Thanks to these characteristics, CNIs have been often used in the treatment of autoimmune diseases. However, the therapeutic index of CNIs is narrow, and their interactions with other drugs can increase toxicity or reduce efficacy. In lupus nephritis, cyclosporine and tacrolimus have been used both in induction and maintenance therapies. Observational studies and randomized controlled trials showed that both cyclosporine and tacrolimus can increase efficacy. Tolerance is satisfactory if low doses are used and the patient is carefully monitored. More recently, a new CNI, called voclosporin (VCS), has been approved by the Food and Drug Administration for use in lupus nephritis. VCS offers potential advantages over other CNIs. In two large multiethnic trials, VCS was not associated with adverse renal and metabolic events and obtained positive results despite a novel and rapid corticosteroid tapering regime.Claudio PonticelliFrancesco ReggianiGabriella MoroniMDPI AGarticlelupus nephritisproteinuriacalcineurin inhibitorscyclosporinetacrolimusvoclosporinMedicineRENJournal of Clinical Medicine, Vol 10, Iss 4832, p 4832 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	lupus nephritis proteinuria calcineurin inhibitors cyclosporine tacrolimus voclosporin Medicine R
spellingShingle	lupus nephritis proteinuria calcineurin inhibitors cyclosporine tacrolimus voclosporin Medicine R Claudio Ponticelli Francesco Reggiani Gabriella Moroni Old and New Calcineurin Inhibitors in Lupus Nephritis
description	Calcineurin inhibitors (CNIs) are drugs that inhibit calcineurin, a key phosphatase that dephosphorylates a transcription factor called the nuclear factor of activated T cells (NFAT), allowing its translocation into the nucleus of quiescent T cells. In the nucleus, NFAT activates interleukin 2, which stimulates the proliferation and differentiation of T-cells. CNIs can also stabilize the actin cytoskeleton of podocytes reducing proteinuria. Thanks to these characteristics, CNIs have been often used in the treatment of autoimmune diseases. However, the therapeutic index of CNIs is narrow, and their interactions with other drugs can increase toxicity or reduce efficacy. In lupus nephritis, cyclosporine and tacrolimus have been used both in induction and maintenance therapies. Observational studies and randomized controlled trials showed that both cyclosporine and tacrolimus can increase efficacy. Tolerance is satisfactory if low doses are used and the patient is carefully monitored. More recently, a new CNI, called voclosporin (VCS), has been approved by the Food and Drug Administration for use in lupus nephritis. VCS offers potential advantages over other CNIs. In two large multiethnic trials, VCS was not associated with adverse renal and metabolic events and obtained positive results despite a novel and rapid corticosteroid tapering regime.
format	article
author	Claudio Ponticelli Francesco Reggiani Gabriella Moroni
author_facet	Claudio Ponticelli Francesco Reggiani Gabriella Moroni
author_sort	Claudio Ponticelli
title	Old and New Calcineurin Inhibitors in Lupus Nephritis
title_short	Old and New Calcineurin Inhibitors in Lupus Nephritis
title_full	Old and New Calcineurin Inhibitors in Lupus Nephritis
title_fullStr	Old and New Calcineurin Inhibitors in Lupus Nephritis
title_full_unstemmed	Old and New Calcineurin Inhibitors in Lupus Nephritis
title_sort	old and new calcineurin inhibitors in lupus nephritis
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/0934bce1493d4d1f850c6a2ebc291c97
work_keys_str_mv	AT claudioponticelli oldandnewcalcineurininhibitorsinlupusnephritis AT francescoreggiani oldandnewcalcineurininhibitorsinlupusnephritis AT gabriellamoroni oldandnewcalcineurininhibitorsinlupusnephritis
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Old and New Calcineurin Inhibitors in Lupus Nephritis

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