#
Erlotinib
  • Drugs A to Z

Erlotinib

Generic name: erlotinib
Brand name: Tarceva
Dosage form: oral tablet
Drug class:EGFR inhibitors

Medically reviewed by N. France, BPharm. Last updated on Apr 22, 2022.

What is erlotinib?

Erlotinib is a type of targeted therapy used to treat cancer.

Erlotinib is a tyrosine kinase inhibitor that works by blocking the kinase activity of a protein called epidermal growth factor receptor (EGFR), which is involved in cell growth and survival.

EGFR is found on the surface of normal and cancerous cells. Sometimes normal versions of the EGFR protein can contribute to the development of cancer, but in other cases mutations can occur in the EGFR protein, which enable cancer cells to grow, divide and spread faster.

Erlotinib is used to treat pancreatic cancer and non-small cell lung cancer (NSCLC). It is only used to treat cases of NSCLC that have specific mutations in their EGRF protein - exon 19 deletions or exon 21 substitution mutations.

Erlotinib was first approved by the US Food and Drug Administration (FDA) in 2004. It is available under the brand name Tarceva and also as a generic tablet.

What is erlotinib used for?

Erlotinib is a prescription medication used:

  • For the treatment of patients with metastatic (cancer that has spread) NSCLC whose tumors have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations who are receiving first-line, maintenance, or second or greater line treatment after progression following at least one prior chemotherapy regimen.
    • You healthcare provider will use an FDA-approved test to check if you have one of these mutations. The safety and efficacy of erlotinib has not been established in patients with NSCLC whose tumors have other EGFR mutations.
  • In combination with gemcitabine in patients with advanced-stage pancreatic cancer whose cancer has spread, grown, or cannot be surgically removed and who have not received previous chemotherapy (first-line).

Erlotinib tablets are not recommended for use in combination with platinum- based chemotherapy.

Important information

Erlotinib can cause serious side effects, including

  • Lung problems called interstitial lung disease events. Erlotinib has been shown to cause lung problems, including death. Symptoms of lung problems may include shortness of breath, cough, and fever. Erlotinib may need to be stopped if you have any of these symptoms.
  • Liver and kidney problems. Erlotinib has been shown to cause severe kidney and liver problems, including death. Some people had their kidneys and liver stop working. Let your healthcare provider know if you have a history of liver or kidney disease.
  • Stomach and intestinal problems called gastrointestinal perforation. Erlotinib has been shown to cause gastrointestinal perforation, which has led to death. A gastrointestinal perforation is a hole that develops in your stomach or intestine. Erlotinib patients may be at a higher risk for gastrointestinal perforation if they:
    • Are taking medicines including those that.