Class/mechanism: EGFR/HER2 tyrosine kinase inhibitor; 4-anilinoquinazoline inhibitor of the intracellular tyrosine kinase domains of EGFR (epidermal growth factor receptor/ErbB1) and HER2 (human epidermal growth factor receptor 2/ErbB2), which drive proliferation in certain malignancies.
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 prescribing information.
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 3/13/2007: Initial FDA approval in combination with capecitabine, for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab.
- 1/29/2010: New indication in combination with letrozole for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated.
Also known as
- Code name: GW572016
- Brand name: Tykerb