Reaction: Trametinib to 1 product

Reaction
Trametinib
DB08911
    Trametinib M3 metabolite
    DBMET03643
    Reaction type
    deacetylation; hydroxylation
    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 M3 metabolite demonstrated approximately equal or 10-fold less potent activity to inhibit phospho-MEK1 activity than the parent compound, trametinib.
    Enzymes
    Not Available