MMF is the major metabolite, along with the cleaved prodrug fragments
methanol (DMF), 2-hydroxyethyl succinimide (DRF) and
N,N-diethyl-2-hydroxyacetamide (TPF). DMF is a symmetrical
diester and leads solely to MMF and methanol. For DRF, 2-hydroxyethyl
succinimide and methanol formation occurs asymmetrically in a 9:1 ratio [18]. The biologically inert 2-hydroxyethyl
succinimide is eliminated primarily through the renal system (58–63%) and
the small amount of RDC-8439 formed is presumably converted to FA and
2-hydroxyethyl succinimide in the liver [17]. It is expected that TPF undergoes similar asymmetric cleavage
and clearance, given its bioequivalent MMF production (Table 1), even though its spontaneous hydrolysis is
not asymmetric [19].