The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends

The confluence of a large variety of factors, achievements and developments has resulted in the current long-term success in graft transplants. Some of these events are reviewed, paying special attention to immunosuppressant drugs, which are one of the most relevant milestones in the prevention of o...

Full description

Saved in:
Bibliographic Details
Main Authors: Carlos Barreiro, Ana Ibañez, Sonia Garrido-Chamorro, José Luis Barredo
Format: Article
Language:English
Published: MDPI AG 2024-12-01
Series:Fermentation
Subjects:
Online Access:https://www.mdpi.com/2311-5637/10/12/645
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850040878844870656
author Carlos Barreiro
Ana Ibañez
Sonia Garrido-Chamorro
José Luis Barredo
author_facet Carlos Barreiro
Ana Ibañez
Sonia Garrido-Chamorro
José Luis Barredo
author_sort Carlos Barreiro
collection DOAJ
description The confluence of a large variety of factors, achievements and developments has resulted in the current long-term success in graft transplants. Some of these events are reviewed, paying special attention to immunosuppressant drugs, which are one of the most relevant milestones in the prevention of organ transplant rejection. The discovery, industrial exploitation, mechanisms of action and side effects of several drugs exhibiting immunosuppressive effects (e.g., corticosteroids, nitrogen mustards, mycophenolic acid, rapamycin) are deeply detailed. Furthermore, new trends in immunosuppressant research, improvement and reformulation are also reviewed. Nevertheless, the core of the manuscript is the immunosuppressant tacrolimus, also called FK506, which has been sought after due to the commercial success of cyclosporine and other immunosuppressant compounds, but also because of the side effects of those previous compounds. Thus, in the mid-1980s tacrolimus was described as a more potent immunosuppressive molecule, with less undesirable effects. Currently, tacrolimus is a well-stablished API that is used as a clinical treatment to avoid graft rejection, but also shows interesting properties in terms of decreasing the impact of some autoimmune diseases and acting as an enhancer of nerve regeneration treatments. Thus, in the 40th anniversary of its discovery, this paper describes the current state of the art of this drug and how it is adapting to new social needs and clinical trends.
format Article
id doaj-art-32673bda63204ae69ece4922c2b16341
institution DOAJ
issn 2311-5637
language English
publishDate 2024-12-01
publisher MDPI AG
record_format Article
series Fermentation
spelling doaj-art-32673bda63204ae69ece4922c2b163412025-08-20T02:55:57ZengMDPI AGFermentation2311-56372024-12-01101264510.3390/fermentation10120645The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future TrendsCarlos Barreiro0Ana Ibañez1Sonia Garrido-Chamorro2José Luis Barredo3Área de Bioquímica y Biología Molecular, Departamento de Biología Molecular, Facultad de Veterinaria, Universidad de León, 24071 León, SpainÁrea de Bioquímica y Biología Molecular, Departamento de Biología Molecular, Facultad de Veterinaria, Universidad de León, 24071 León, SpainÁrea de Bioquímica y Biología Molecular, Departamento de Biología Molecular, Facultad de Veterinaria, Universidad de León, 24071 León, SpainCuria Spain Parque Tecnológico de León, C/Andrés Suárez s/n, 24009 León, SpainThe confluence of a large variety of factors, achievements and developments has resulted in the current long-term success in graft transplants. Some of these events are reviewed, paying special attention to immunosuppressant drugs, which are one of the most relevant milestones in the prevention of organ transplant rejection. The discovery, industrial exploitation, mechanisms of action and side effects of several drugs exhibiting immunosuppressive effects (e.g., corticosteroids, nitrogen mustards, mycophenolic acid, rapamycin) are deeply detailed. Furthermore, new trends in immunosuppressant research, improvement and reformulation are also reviewed. Nevertheless, the core of the manuscript is the immunosuppressant tacrolimus, also called FK506, which has been sought after due to the commercial success of cyclosporine and other immunosuppressant compounds, but also because of the side effects of those previous compounds. Thus, in the mid-1980s tacrolimus was described as a more potent immunosuppressive molecule, with less undesirable effects. Currently, tacrolimus is a well-stablished API that is used as a clinical treatment to avoid graft rejection, but also shows interesting properties in terms of decreasing the impact of some autoimmune diseases and acting as an enhancer of nerve regeneration treatments. Thus, in the 40th anniversary of its discovery, this paper describes the current state of the art of this drug and how it is adapting to new social needs and clinical trends.https://www.mdpi.com/2311-5637/10/12/645corticosteroidsFK506graftimmunosuppressantmycophenolic acidnitrogen mustards
spellingShingle Carlos Barreiro
Ana Ibañez
Sonia Garrido-Chamorro
José Luis Barredo
The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends
Fermentation
corticosteroids
FK506
graft
immunosuppressant
mycophenolic acid
nitrogen mustards
title The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends
title_full The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends
title_fullStr The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends
title_full_unstemmed The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends
title_short The Immunosuppressant Tacrolimus (FK506) Facing the 21st Century: Past Findings, Present Applications and Future Trends
title_sort immunosuppressant tacrolimus fk506 facing the 21st century past findings present applications and future trends
topic corticosteroids
FK506
graft
immunosuppressant
mycophenolic acid
nitrogen mustards
url https://www.mdpi.com/2311-5637/10/12/645
work_keys_str_mv AT carlosbarreiro theimmunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT anaibanez theimmunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT soniagarridochamorro theimmunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT joseluisbarredo theimmunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT carlosbarreiro immunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT anaibanez immunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT soniagarridochamorro immunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends
AT joseluisbarredo immunosuppressanttacrolimusfk506facingthe21stcenturypastfindingspresentapplicationsandfuturetrends