Difference between revisions of "Neratinib (Nerlynx)"
Warner-admin (talk | contribs) m (Text replacement - ",_HER-2_p" to ",_HER2-p") |
m |
||
| Line 9: | Line 9: | ||
==Diseases for which it is used== | ==Diseases for which it is used== | ||
*[[Breast cancer, HER2-positive|HER2+ breast cancer]] | *[[Breast cancer, HER2-positive|HER2+ breast cancer]] | ||
| + | *[[ERBB2 (HER2)|HER2+ tumors (site-agnostic)]] | ||
| + | *[[ERBB3 (HER3)|HER3+ tumors (site-agnostic)]] | ||
==Patient drug information== | ==Patient drug information== | ||
| Line 30: | Line 32: | ||
[[Category:EGFR inhibitors]] | [[Category:EGFR inhibitors]] | ||
[[Category:ERBB2 inhibitors]] | [[Category:ERBB2 inhibitors]] | ||
| + | [[Category:ERBB3 inhibitors]] | ||
[[Category:ERBB4 inhibitors]] | [[Category:ERBB4 inhibitors]] | ||
[[Category:Breast cancer medications]] | [[Category:Breast cancer medications]] | ||
| + | [[Category:ERBB2 (HER2) medications]] | ||
| + | [[Category:ERBB3 (HER3) medications]] | ||
[[Category:Drugs FDA approved in 2017]] | [[Category:Drugs FDA approved in 2017]] | ||
Revision as of 18:05, 26 April 2018
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]
[2][3][4]
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.[1]
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 7/17/2017: FDA approved "for the extended adjuvant treatment of adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy."
Also known as
- Code name: HKI-272
- Brand name: Nerlynx
References
- ↑ 1.0 1.1 1.2 Neratinib (Nerlynx) package insert
- ↑ Neratinib (Nerlynx) package insert (locally hosted backup)
- ↑ Nerlyn manufacturer's website
- ↑ 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