DMD Highlight: Metabolism of the MEK1/2 Inhibitor Pimasertib Involves a Novel Conjugation with Phosphoethanolamine in Patients with Solid Tumors
Pimasertib is a selective inhibitor of MEK1/2, which is often dysregulated in cancer cells, and its clinical activity is being investigated in various tumor types. In a phase I mass balance study, one of the two major metabolites in urine was a phosphoethanolamine conjugate on the propanediol moiety. Phosphoethanolamine conjugates of any drug have not been reported previously, and studies of the enzymes involving their generation are ongoing.
See the article by Scheible et al. at Drug Metabolism and Disposition February 2017, 45 (2) 174-182; DOI: https://doi.org/10.1124/dmd.116.072934