Neratinib (Nerlynx)

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General information

Class/mechanism: Irreversible pan-ErbB tyrosine kinase inhibitor of HER2 (human epidermal growth factor receptor 2), EGFR (epidermal growth factor receptor), and ERBB4. Neratinib inhibits activity and downstream signalling of the tyrosine kinase domains of these receptors, likely by interacting with cysteine residue in their ATP-binding pockets. This inhibition has been observed to cause cell cycle arrest in the G1-S (Gap 1/DNA synthesis) phase of the cell division cycle.[1]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the package insert.

Patient drug information

No information available.

References

  1. Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Floyd MB, Golas J, Hallett WA, Johnson BD, Nilakantan R, Overbeek E, Reich MF, Shen R, Shi X, Tsou HR, Wang YF, Wissner A. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004 Jun 1;64(11):3958-65. link to original article PubMed