Isolation, identification and immunosuppressive activity of SDZ-IMM-125 metabolites from human liver microsomes.
(1999) European Journal of Drug Metabolism and Pharmacokinetics — Vol. 24, n° 1, p. 83-90 (1999)
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- Abstract
- SDZ-IMM-125 N-methyl leucine 9 hydroxylated in the gamma position is a metabolite which was extracted from incubated human liver microsomes and subsequently separated by normal and reverse-phase HPLC. This metabolite was identified by fast atom bombardment mass spectrometry, electrospray-ms/ms mass spectrometry and nuclear magnetic resonance spectroscopy. The in vitro 50% inhibitory concentration, tested against bidirectional mixed lymphocyte reaction was 80 microg/l indicating that this metabolite does not retain in vitro immunosuppressive activity most probably due to the structural modification of SDZ-IMM-125 in the recognized binding region to cyclophilin A reducing its binding affinity relative to the parent drug.
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Dieden, R., Verbeeck, R.-K., Latinne, D., Wallemacq, P., Maton, N., & Lhoëst, G. (1999). Isolation, identification and immunosuppressive activity of SDZ-IMM-125 metabolites from human liver microsomes. European Journal of Drug Metabolism and Pharmacokinetics, 24(1), 83-90. https://hdl.handle.net/2078.5/85213 (Original work published 1999)