3002 Mycophenolic acid Mycophenolic acid is an an immunosuppresant drug and potent anti-proliferative, and can be used in place of the older anti-proliferative azathioprine. It is usually used as part of triple therapy including a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone. It is also useful in research for the selection of animal cells that express the E. coli gene coding for XGPRT (xanthine guanine phosphoribosyltransferase). 24280-93-1 446541 C17H20O6 320.125990 White powder. 141°C Insoluble Bioavailability following oral administration of Myfortic delayed-release tablet ranges from 70-95% Mycophenolic acid is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA. Because T- and B-lymphocytes are critically dependent for their proliferation on de novo synthesis of purines, whereas other cell types can utilize salvage pathways, mycophenolic acid has potent cytostatic effects on lymphocytes. Mycophenolic acid inhibits proliferative responses of T- and B-lymphocytes to both mitogenic and allospecific stimulation. Addition of guanosine or deoxyguanosine reverses the cytostatic effects of mycophenolic acid on lymphocytes. Mycophenolic acid also suppresses antibody formation by B-lymphocytes. Mycophenolic acid prevents the glycosylation of lymphocyte and monocyte glycoproteins that are involved in intercellular adhesion to endothelial cells and may inhibit recruitment of leukocytes into sites of inflammation and graft rejection. Mycophenolic acid is metabolized mainly by glucuronyl transferase to glucuronidated metabolites, predominantly the phenolic glucuronide, mycophenolic acid glucuronide (MPAG). MPAG does not manifest pharmacological activity. The acyl glucuronide minor metabolite has pharmacological activity similar to mycophenolic acid. The AUC ratio of Mycophenolic acid:MPAG:acyl glucuronide is approximately 1:24:0.28 at steady state. Half Life: The mean elimination half-life for mycophenolic acid ranges from 8-16 hours, while that of the MPAG metabolite ranges from 13-17 hours. LD50: 352 mg/kg (Oral, Rat) (A308) LD50: 1000 mg/kg (Oral, Mouse) (A308) LD50: >6000 mg/kg (Oral, Rabbit) (A308) No indication of carcinogenicity to humans (not listed by IARC). For the prophylaxis of organ rejection in patients receiving allogeneic renal transplants, administered in combination with cyclosporine and corticosteroids. Possible signs and symptoms of acute overdose could include the following: hematological abnormalities such as leukopenia and neutropenia, and gastrointestinal symptoms such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia. 2009-07-21T20:28:11Z 2014-12-24T20:25:54Z Mycophenolic_acid C20380 168396 Mycophenolic acid DB01024 MOA true [H]C(CC1=C(O)C2=C(COC2=O)C(C)=C1OC)=C(C)CCC(O)=O C17H20O6 InChI=1S/C17H20O6/c1-9(5-7-13(18)19)4-6-11-15(20)14-12(8-23-17(14)21)10(2)16(11)22-3/h4,20H,5-8H2,1-3H3,(H,18,19)/b9-4+ InChIKey=HPNSFSBZBAHARI-RUDMXATFSA-N 320.3371 320.125988372 Exogenous Solid 2.8 HMDB15159 CHEMBL866 393865 <p>Bernard J. Abbott, John G. Whitney, &#8220;Method of preparing mycophenolic acid glucoside.&#8221; U.S. Patent US4234684, issued January, 1976.</p>