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MYCOPHENOLATE MOFETIL

Marketedupdated 2mo ago

by $AMRX Amneal Pharmaceuticals, Inc.🔗 ChEMBL

Approved

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Small molecule drug with a maximum clinical stage of Approval (across all indications), with 54 investigational indications.

targets

Inosine-5'-monophosphate dehydrogenase (IMPDH)

all catalysts(17)

approval · 17

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brand

MYCOPHENOLATE MOFETIL

trade names

Arzip, Cellcept, Myclausen, Mycophenolate mofetil, Mycophenolate mofetil teva, Myfenax

generic

MYCOPHENOLATE MOFETIL

MOA

12.1 Mechanism of Action Mycophenolate mofetil (MMF) is absorbed following oral administration and hydrolyzed to mycophenolic acid (MPA), the active metabolite. MPA is a selective uncompetitive inhibitor of the two isoforms (type I and type II) of inosine monophosphate dehydrogenase (IMPDH) leading to inhibition of the de novo pathway of guanosine nucleotide synthesis and blocks DNA synthesis. The mechanism of action of MPA is multifaceted and includes effects on cellular checkpoints responsible for metabolic programming of lymphocytes. MPA shifts transcriptional activities in lymphocytes from a proliferative state to catabolic processes. In vitro studies suggest that MPA modulates transcriptional activities in human CD4+ T-lymphocytes by suppressing the Akt/mTOR and STAT5 pathways that are relevant to metabolism and survival, leading to an anergic state of T-cells whereby the cells become less responsive to antigenic stimulation. Additionally, MPA enhanced the expression of negative co-stimulators such as CD70, PD-1, CTLA-4, and transcription factor FoxP3 as well as decreased the expression of positive co-stimulators CD27 and CD28. MPA decreases proliferative responses of T- and B-lymphocytes to both mitogenic and allo-antigenic stimulation, antibody responses, as well as the production of cytokines from lymphocytes and monocytes such as GM-CSF, IFN-ɣ, IL-17, and TNF-α. Additionally, MPA prevents the glycosylation of lymphocyte and monocyte glycoproteins that are involved in intercellular adhesion to endothelial cells and may inhibit recruitment of leukocytes into sites of inflammation and graft rejection. Overall, the effect of MPA is cytostatic and reversible.

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MYCOPHENOLATE MOFETIL

targets

all catalysts(17)

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Trials studying MYCOPHENOLATE MOFETIL