6α-Methylprednisolone 21-hemisuccinate is a prodrug form of the synthetic glucocorticoid methylprednisolone .1 It is converted to methylprednisolone by carboxylesterase 2 (CES2).2 Nanoliposomes containing 6α-methylprednisolone 21-hemisuccinate decrease disease severity in a rat model of adjuvant-induced arthritis.3 Formulations containing 6α-methylprednisolone 21-hemisuccinate have been used as anti-inflammatory agents and immunosuppressants with indications in allergic reactions and dermatologic, renal, gastrointestinal, respiratory, and ophthalmic diseases, as well as endocrine, hematologic, and rheumatic disorders.
1.Vree, T.B., Lagerwerf, A.J., Verwey-van Wissen, C.P., et al.High-performance liquid chromatography analysis, preliminary pharmacokinetics, metabolism and renal excretion of methylprednisolone with its C6 and C20 hydroxy metabolites in multiple sclerosis patients receiving high-dose pulse therapyJ. Chromatogr. B Biomed. Sci. Appl.732(2)337-348(1999) 2.Hori, T., Jin, L., Fujii, A., et al.Dexamethasone-mediated transcriptional regulation of rat carboxylesterase 2 geneXenobiotica42(7)614-623(2012) 3.Avnir, Y., Ulmansky, R., Wasserman, V., et al.Amphipathic weak acid glucocorticoid prodrugs remote-loaded into sterically stabilized nanoliposomes evaluated in arthritic rats and in a Beagle dog: A novel approach to treating autoimmune arthritisArthritis Rheum.58(1)119-129(2008)