Reaction: Trametinib to 1 product

Reaction
Trametinib
DB08911
    Trametinib M1 metabolite
    DBMET03641
    Reaction type
    deacetylation
    Direction
    Major circulating metabolite?
    No
    Spontaneous?
    No
    Activity
    active
    References
    1. Ho MY, Morris MJ, Pirhalla JL, Bauman JW, Pendry CB, Orford KW, Morrison RA, Cox DS: Trametinib, a first-in-class oral MEK inhibitor mass balance study with limited enrollment of two male subjects with advanced cancers. Xenobiotica. 2014 Apr;44(4):352-68. doi: 10.3109/00498254.2013.831143. Epub 2013 Aug 23. [Article]
    2. FDA Approved Drug Products: MEKINIST (trametinib) tablets or solution, for oral use (March 2023) [Link]
    Comments
    In vitro, the M1 metabolite demonstrated approximately equal or 10-fold less potent activity to inhibit phospho-MEK1 activity than the parent compound, trametinib.
    Enzymes
    Not Available