Drug intelligence / Profile preview

mycophenolate mofetil + methotrexate

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Mycophenolate mofetil + methotrexate is a combination of two immunosuppressive small molecule drugs used primarily in the management of autoimmune diseases and as steroid-sparing agents. Mycophenolate mofetil is a prodrug that is converted to mycophenolic acid, which inhibits inosine-5'-monophosphate dehydrogenase (IMPDH), leading to suppression of T and B lymphocyte proliferation by blocking de novo purine synthesis. Methotrexate acts mainly as an antimetabolite by inhibiting dihydrofolate reductase, thereby interfering with DNA synthesis, repair, and cellular replication; it also modulates immune function through inhibition of pro-inflammatory cytokines and promotion of anti-inflammatory cytokines such as IL-10. The combination has been studied for use in conditions such as uveitis, scleroderma, interstitial lung disease associated with autoimmune disorders, and other refractory or severe autoimmune diseases where monotherapy may be insufficient[2][3][4][7]. Combination therapy can increase the risk for adverse effects like myelosuppression but may offer enhanced efficacy in certain patient populations[3].

Brand names
CellCeptMyforticRheumatrexTrexall
Other names
mycophenolate mofetilMMF
02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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