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Review

Fedratinib

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

Fedratinib

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Excerpt

Fedratinib is an oral selective inhibitor of Janus associated kinase 2 (JAK-2) and FMS-like tyrosine kinase 3 (FLT3) that is used in the therapy of intermediate or high-risk, primary or secondary myelofibrosis. Fedratinib has been associated with a high rate of serum enzyme elevations during therapy, but has been associated with only rare instances of clinically apparent acute liver injury.

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References

    1. 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 tyrosine kinase receptor inhibitors).
    1. DeLeve LD. Kinase inhibitors. Cancer chemotherapy. In, Kaplowitz N, DeLeve LD, eds. Drug-induced liver disease. 3rd ed. Amsterdam: Elsevier, 2013, p. 556.(Review of hepatotoxicity of cancer chemotherapeutic agents, does not discuss fedratinib).
    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).
    1. FDA . https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000M...(FDA website with product labels and initial multidiscipline review of the safety and efficacy of fedratinib; states that patients with myelofibrosis frequently have elevations in bilirubin and serum enzymes, but patients treated with fedratinib have a higher rate of ALT elevations [58%] compared to placebo [17%], but these elevations are generally mild and above 5 times ULN in 9% vs 1% with placebo; despite this, significant liver injury attributable to fedratinib is uncommon).
    1. Zhang M, Xu CR, Shamiyeh E, Liu F, Yin JY, von Moltke LL, Smith WB. A randomized, placebo-controlled study of the pharmacokinetics, pharmacodynamics, and tolerability of the oral JAK2 inhibitor fedratinib (SAR302503) in healthy volunteers. J Clin Pharmacol. 2014;54:415–21. [(A pharmacologic study in 57 healthy controls given one of 7 doses of fedratinib, found significant inhibition of STAT-signaling with doses of 300 mg or higher).] - PubMed

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