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

• Carcinoma of unknown primary
• Cholangiocarcinoma
• Colorectal cancer
• EGFR-mutated tumors (tissue-agnostic)
• Esophageal cancer
  • Esophageal adenocarcinoma
• Gallbladder cancer
• Head and neck 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)
• Some regimens suggest that the drug be taken 1 hour before or 2 hours after meals

History of changes in FDA indication

Non-small cell lung cancer

• 2004-11-18: Approved for treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen. (Based on NCIC-CTG BR.21)
• 2010-04-16: 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. (Based on SATURN)
• 2013-05-14: 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. (Based on EURTAC)
• 2016-10-18: 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. (Based on IUNO)

Pancreatic cancer

• 2005-11-02: 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

• 2005-09-19: Initial marketing authorization as Tarceva. Tarceva is indicated for the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. (Based on NCIC-CTG BR.21)
• 2010-03-18: Extension of indication as monotherapy for maintenance treatment in patients with locally advanced or metastatic non-small cell lung cancer with stable disease after 4 cycles of standard platinum-based first-line chemotherapy.
• 2011-08-24: Extension of indication of Tarceva for the first-line treatment of locally advanced or metastatic NSCLC with EGFR activating mutations.
• 2016-01-25: Modification of the indication to limit maintenance treatment to NSCLC patients with an EGFR-activating mutation and stable disease after first-line chemotherapy. (Based on IUNO)

History of changes in Health Canada indication

• 2005-07-07: Initial notice of compliance (unclear details)
• 2011-03-11: New Indication as monotherapy for maintenance treatment in patients with locally advanced or metastatic non-small cell lung cancer with stable disease after 4 cycles of standard platinum-based first-line chemotherapy.
• 2012-07-20: New indication as monotherapy for the first-line treatment of patients with locally advanced (stage III b) not amenable to curative therapy) or metastatic (stage IV) non-small cell lung cancer (NSCLC) with EFGR activating mutations.
• 2017-03-29: Revision to the maintenance indication for locally advanced or metastatic non-small cell lung cancer (NSCLC) based on the IUNO study and SATURN study results to limit use to patients with locally advanced or metastatic non-small cell lung cancer whose tumors have activating mutations in the epidermal growth factor receptor (EGFR) gene.

History of changes in PMDA indication

• 2007-10-19: Initial approval for the treatment of unresectable, relapsed/advanced non-small cell lung cancer exacerbated after cancer chemotherapy.
• 2011-07-01: New additional indication and a new dosage for the treatment of unresectable pancreatic cancer.
• 2013-06-14: New additional indication and a new dosage for the treatment of unresectable advanced or recurrent non-small cell lung cancer with EGFR gene mutation in patients who have not been treated with chemotherapy.

Also known as

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