Erlotinib (Tarceva)

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.
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 prescribing information.

Diseases for which it is used

• Adenocarcinoma of unknown primary
• Cholangiocarcinoma
• EGFR-mutated tumors (tissue-agnostic)
• Esophageal cancer
• Hepatocellular carcinoma
• Myelodysplastic syndrome
• Non-small cell lung cancer
• Pancreatic cancer
• Renal cell carcinoma
  • Papillary renal cell carcinoma

Patient drug information

• Erlotinib (Tarceva) patient drug information (Chemocare)
• Brief patient counseling information can be found on page 24 of the Erlotinib (Tarceva) package insert
• Erlotinib (Tarceva) patient drug information (UpToDate)

History of changes in FDA indication

• 11/18/2004: Approved for treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
• 11/2/2005: Approved as first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
• 4/16/2010: Approved for maintenance treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) whose disease has not progressed after four cycles of platinum-based first-line chemotherapy.
• 5/14/2013: Approved for first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
• 10/18/2016: Label revised to limit use to those patients whose tumors have EGFR exon 19 deletions or exon 21 L858R substitution mutations as detected by an FDA-approved test. This limitation pertains to patients with NSCLC receiving maintenance or second or greater line treatment.

Also known as

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