Mechanisms of action of mycophenolate mofetil
Abstract
Mycophenolate mofetil (MMF, CellCept®) is a prodrug of mycophenolic acid (MPA), an inhibitor of inosine-5′‘monophosphate dehydrogenase. MPA depletes guanosine nucleotides preferentially in T and B lymphocytes and inhibits their proliferation, thereby suppressing cell-mediated immune responses and antibody formation. MPA also inhibits the glycosylation and expression of adhesion molecules, and the recruitment of lymphocytes and monocytes into sites of inflammation. MPA depletes tetrahydrobiopterin and decreases the production of nitric oxide by inducible NO synthase without affecting the activity of constitutive NO synthases. Activated macrophages produce NO and superoxide, which combine to generate tissue-damaging peroxynitrite. By these two mechanisms MMF exerts anti-inflammatory activity. Unlike calcineurin inhibitors, MMF is not nephrotoxic and does not induce the production of TGF β, which is fibrogenic. MMF does not increase blood pressure, cholesterol levels or triglyceride levels in recipients. MMF reduces acute and chronic rejection in allograft recipients and is efficacious in some nephropathies. Evidence is accumulating that MMF may have clinical utility in some autoimmune disorders.
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Mycophenolate mofetil (MMF), prodrug of mycophenolic acid, preferentially inhibits type II IMPDH, suppressing T and B cells proliferation.
“Mycophenolate mofetil (MMF), prodrug of mycophenolic acid, preferentially inhibits type II IMPDH, suppressing T and B cells proliferation (74).”
From Immunomodulation in Administration of RAAV: Preclinical and Clinical Adjuvant Pharmacotherapies (2021) · cites this paper as [74]
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“8 The intestinal microbiota has recently been investigated as a potential therapeutic target to achieve higher efficacy and lower toxicity of several chemotherapeutic drugs, including MTX. 9,10 Further research in experimental autoimmune uveitis (EAU) demonstrates a strong influence of the gut…”
- Authors
- Allison, A.
- Affiliations
- SurroMed, Inc., Menlo Park, CA, USA
- Venue
- Lupus
- Publisher
- SAGE Publications
- Published
- 2005-01
- Volume
- 14
- Issue
- 1_suppl
- Pages
- 2-8
- ISSN
- 0961-2033 (ISSN-L)
- 1477-0962
- OpenAlex
- W2074604840
- Cited by
- 480
- References
- 48
- Citations by year
- 2026: 24 · 2025: 35 · 2024: 42 · 2023: 38 · 2022: 56 · 2021: 42 · 2020: 30 · 2019: 18 · 2018: 17 · 2017: 21 · 2016: 23 · 2015: 12 · 2014: 7 · 2013: 16 · 2012: 13
- FWCI
- 7.65
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Lupus (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Transplantation › Renal Transplantation Outcomes and Treatments
- Health Sciences › Medicine › Rheumatology › Systemic Lupus Erythematosus Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
- Keywords
- mycophenolate mofetil, mycophenolic acid, adhesion molecule expression, tetrahydrobiopterin, nitric oxide, inducible nitric oxide synthase, peroxynitrite, macrophages, anti-inflammatory activity, calcineurin inhibitors, allograft rejection, kidney disease, autoimmune disease, immunosuppression
- MeSH terms
- Azathioprine, B-Lymphocytes, Humans, Immunosuppressive Agents, Mycophenolic Acid, Nitric Oxide, T-Lymphocytes, Vascular Diseases, Cytokines
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