Mycophenolic acid (MPA) is an immunosuppressant requiring therapeutic drug monitoring. It is commonly prescribed in adult kidney transplant recipients for preventing graft rejection[3]. Mycophenolic acid, the active metabolite of mycophenolate mofetil, is administered with cyclosporine and oral steroids to prevent acute rejection after renal transplant. Total body weight, time after transplant, and mycophenolate mofetil dosage according to body weight affect mycophenolic acid pharmacokinetics[4]. Mycophenolic acid (MPA, 1), an inhibitor of IMP-dehydrogenase (IMPDH) and a latent PPARgamma agonist[5]. Mycophenolic acid (MPA), a reversible inhibitor of inosine 5''-monophosphate dehydrogenase (IMPDH), selectively inhibits T- and B-cell proliferation. MPA exposure correlates inversely with the risk of acute rejection[6].
体外研究
Mycophenolic acid (0.01-1 μM; 72 h) showed preferential antiproliferative activity against endothelial cells and fibroblasts. Endothelial cells are the most sensitive cells to Mycophenolic acid treatment, with an IC50 <500 nM for antimitotic effects [7].
Fibroblasts are also susceptible to Mycophenolic acid-induced cell cycle inhibition, but exhibit a higher IC50 (<1 μM) compared to endothelial cells. Two human tumour cell lines, A549 non-small cell lung cancer cells and PC3 prostate cancer cells, showed intermediate sensitivity with an IC50 >1 μM. U87 glioblastoma cells were resistant to MPA treatments up to 1 μM[7].
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