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Review

Selumetinib

No authors listed
In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012.
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Review

Selumetinib

No authors listed.
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Excerpt

Selumetinib is an oral, small molecule inhibitor of the mitogen activated protein kinase 1 and 2 (MEK1/2) that is used to treat symptomatic, refractory fibromas in neurofibromatosis type 1. Selumetinib is associated with transient and usually mild elevations in serum aminotransferase levels during therapy, but has not been linked to cases of clinically apparent acute liver injury.

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References

    1. Zimmerman HJ. Zimmerman HJ. Hepatotoxicity: the adverse effects of drugs and other chemicals on the liver. 2nd ed. Philadelphia: Lippincott, 1999.(Review of hepatotoxicity published in 1999 before the availability of protein kinase inhibitors such as selumetinib).
    1. DeLeve LD. Erlotinib. Cancer chemotherapy. In, Kaplowitz N, DeLeve LD, eds. Drug-induced liver disease. 3rd ed. Amsterdam: Elsevier, 2013, pp. 556.(Review of hepatotoxicity of cancer chemotherapeutic agents discusses several kinase inhibitors including imatinib, gefitinib, erlotinib and crizotinib, but not selumetinib).
    1. Wellstein A, Giaccone G, Atkins MB, Sausville EA. Pathway-targeted therapies: monoclonal antibodies, protein kinase inhibitors, and various small molecules. In, Brunton LL, Hilal-Dandan R, Knollman BC, eds. Goodman & Gilman's the pharmacological basis of therapeutics. 13th ed. New York: McGraw-Hill, 2018, pp. 1203-36.(Textbook of pharmacology and therapeutics; selumetinib is not discussed specifically).
    1. FDA . https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213756Orig1s000M...(FDA website with medical review of efficacy and safety of selumetinib which formed the basis of its approval for use in neurofibromatosis, mentions that in registration trials in adults and children with neurofibromatosis there were no liver related serious adverse events, and although ALT elevations arose in 35% of children, none were associated with symptoms or jaundice).
    1. Shah RR, Morganroth J, Shah DR. Hepatotoxicity of tyrosine kinase inhibitors: clinical and regulatory perspectives. Drug Saf. 2013;36:491–503. [ (Review of the hepatotoxicity of 18 tyrosine kinase inhibitors approved for use in cancer in the US as of 2013; selumetinib is not discussed). ] - PubMed

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