Erlotinib

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Erlotinib (brand name Tarceva) is a prescription cancer medicine that helps stop the growth of some cancer cells. It works by blocking EGFR, a protein that signals cancer cells to grow.

What it’s used for
- Non-small cell lung cancer (NSCLC) that has spread, especially when the tumor has certain EGFR mutations (del19 or L858R).
- Pancreatic cancer in combination with gemcitabine for locally advanced or metastatic disease (FDA-approved in 2005).

How to take it
- By mouth as a tablet, taken as prescribed by a doctor.

Common and serious side effects
- Common: rash, diarrhea, muscle or joint pain, cough.
- Serious: problems with the lungs, kidneys, or liver; risk of stomach or intestinal perforation; stroke; corneal ulcers. Pregnancy can harm the baby.

How it works
- Erlotinib is a receptor tyrosine kinase inhibitor that reversibly blocks EGFR signaling, slowing cancer cell growth.

Interactions and safety
- It is processed mainly by the liver enzyme CYP3A4. Other medicines can raise or lower its levels; St. John’s wort can reduce levels, so avoid it unless your doctor says otherwise.

Efficacy and resistance
- In some settings, adding erlotinib to chemotherapy has improved survival and the time before the cancer worsens, especially in patients with EGFR mutations.
- Most patients eventually develop resistance to the drug, often after about 8–12 months, due to changes in EGFR or other mechanisms.

Additional notes
- Erlotinib is on the World Health Organization’s List of Essential Medicines. The U.S. patent expired in 2020, and generic versions are available in many places.