Erlotinib (Tarceva)

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General information

Class/mechanism: Small molecule tyrosine kinase inhibitor. Inhibits the intracellular phosphorylation activity of the epidermal growth factor receptor (EGFR) tyrosine kinase; may also have activity against other tyrosine kinase receptors. Exact mechanism of antitumor action is not fully characterized.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, 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.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Non-small cell lung cancer

Pancreatic cancer

  • 11/2/2005: Approved as first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine. (Based on NCIC-CTG PA.3)

History of changes in EMA indication

  • 9/19/2005: Initial marketing authorization as Tarceva.

Also known as

  • Code names: CP-358, CP-774, OSI-774
  • Generic name: erlotinib hydrochloride
  • Brand names: Erlocip, Erlonat, Melacyte, Tarceva