Lifitegrast Degradation: Products and Pathways.

ABSTRACT: Background/Objectives: Lifitegrast is a recent therapeutic agent provoking scientific and regulatory interest due to its outstanding safety profile and high efficacy in the treatment of dry eye disease. Methods: Herein we employ NMR spectroscopy and mass spectrometry to investigate the weak spots of lifitegrast under standard to extreme stress conditions, resulting in the characterization of three known and nine new degradation products (of which DP7 presented the greatest structural challenge, but was eventually determined as C10 hydroxy derivative, warranting a revision of its previously suggested structure). Results: The first weak spot is identified as a N1-C40 amide bond, and its high susceptibility to hydrolysis is explained through computational DFT analysis. Th

SUBMITTER: Stefan L 

PROVIDER: S-EPMC12567358 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature