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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 mofetil is used at an oral daily dosage of 1200 to 1800 mg per square meter of body size (maximum daily dosage of 3000 mg per square meter of body size) as induction and maintenance therapy to treat the proliferative and membranous glomerulonephritis forms of lupus nephritis (see Classification of lupus nephritis and the following ...
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 ...
Since decreasing proteinuria in the first year of treatment of lupus nephritis is known to be associated with improved long-term outcomes, the available clinical data support the use of voclosporin as first-line therapy in combination with mycophenolate mofetil and low-dose glucocorticosteroid.
The drug also inhibits lymphokine production and interleukin release, leading to a reduced function of effector T-cells. Ciclosporin is used in the treatment of acute rejection reactions, but has been increasingly substituted with newer, and less nephrotoxic , [ 7 ] immunosuppressants.
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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.
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