Mycophenolate mofetil (MMF) (brand names CellCept, Myfortic) is a prodrug of mycophenolic acid (MPA), used extensively in transplant medicine. MPA can induce apoptosis of activated T-lymphocytes, which may eliminate clones of cells responding to antigenic stimulation. Second, by depleting guanosine nucleotides, MPA suppresses glycosylation and the expression of some adhesion molecules, thereby decreasing the recruitment of lymphocytes and monocytes into sites of inflammation and graft rejection. Third, by depleting guanosine nucleotides MPA also depletes tetrahydrobiopterin, a co-factor for the inducible form of nitric oxide synthase (iNOS). Mycophenolate mofetil shows inhibitory activity of lymphocyte functions. Mycophenolate mofetil inhibits type 1 collagen expression and enhances MMP-1 expression. Mycophenolate mofetil reduces α-smooth muscle actin gene expression. The total area under the curve of Mycophenolate mofetil showed a 37% reduction in PPI patients vs those treated with no PPIs (P < 0.01), and the maximum peak concentration of Mycophenolate mofetil was 60% lower in the pantoprazole patients (P < 0.001). The Mycophenolate mofetil exposure correlated with the inhibition of IMPDH activity. The co-medication of pantoprazole with MMF significantly influences the compound exposure and immunosuppressive potency of MMF in patients with autoimmune diseases.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 25 mg/mL|
Proton pump inhibitors interfere with the immunosuppressive potency of mycophenolate mofetil.
Schaier M, et al. Rheumatology (Oxford). 2010 Nov;49(11):2061-7. PMID: 20671023.
Mycophenolate mofetil and its mechanisms of action.
Allison AC, et al. Immunopharmacology. 2000 May;47(2-3):85-118. PMID: 10878285.
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