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Mycophenolate mofetil, a prodrug form of mycophenolic acid used in medicine. Mycophenolate mofetil is the morpholino ethyl ester of mycophenolic acid; the ester masks the carboxyl group. [42] Mycophenolate mofetil is reported to have a pKa values of 5.6 for the morpholino moiety and 8.5 for the phenolic group.
Mycophenolate [ edit ] Mycophenolic acid acts as a non-competitive, selective, and reversible inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH), which is a key enzyme in the de novo guanosine nucleotide synthesis.
This was the first antibiotic compound isolated in pure and crystallised form. Though the original compound was abandoned in clinical practice due to its adverse effects, its chemical derivative mycophenolate mofetil became the drug of choice as an immunosuppressant in kidney, heart, and liver transplantations. [3]
Childhood-onset systemic lupus erythematosus (i.e., cSLE), also termed juvenile-onset systemic lupus erythematosus, juvenile systemic lupus erythematosus, and pediatric systemic lupus erythematosus, is a form of the chronic inflammatory and autoimmune disease, systemic lupus erythematosus (i.e., SLE), that develops in individuals up to 18 years old. [1]
It is mostly well tolerated (though side effects include mucositis, diarrhea, hyperlipidemia, delayed wound healing) with drug-drug interactions. It has better activity against autoimmune disease and lymphoproliferation than mycophenolate mofetil and other drugs; however, sirolimus requires therapeutic drug monitoring and can cause mucositis.
mycophenolic acid O-acyl-glucuronide + H 2 O mycophenolate + D-glucuronate. This liver enzyme deglucuronidates mycophenolic acid O-acyl-glucuronide. Mycophenolic acid acyl-glucuronide (AcMPAG) is an important product in the metabolism of mycophenolic acid, and ABHD10 is the major esterase responsible for the AcMPAG and probenecid acyl ...
More severe cases require the use of combined methotrexate, azathioprine, or mycophenolate with corticosteroids. [3] Severe cases of SAAM may fail to respond to 8–12 weeks of combination therapy. Rituximab or intravenous immunoglobulin are recommended as add-on therapy in such cases. [ 3 ]
Mycophenolate mofetil is an immunosuppressant drug used to prevent rejection in organ transplantation; it inhibits purine synthesis by blocking inosine monophosphate dehydrogenase (IMPDH). [5] Methotrexate also indirectly inhibits purine synthesis by blocking the metabolism of folic acid (it is an inhibitor of the dihydrofolate reductase ).