7-hydroxy Methotrexate (7-hydroxy MTX) is a phase I metabolite of MTX, which is converted by hepatic aldehyde oxidases.[1] Elimination of 7-hydroxy MTX is associated with the multi-drug transporters Abcc2, Abcc3, and Abcg2 in transgenic mouse models. It and the parent compound rapidly accumulate when all three transporters are absent.[2] Formulations containing methotrexate have been used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions.[3],[4] Various methods have been described to quantify 7-hydroxy MTX levels during cancer therapy to avoid toxicity.[5],[6]

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