Erlotinib

Definition

Erlotinib is a targeted cancer therapy that acts as an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. By blocking the activity of EGFR, which is often overexpressed in various cancers, erlotinib interferes with the signaling pathways that promote tumor growth and survival. This makes it particularly significant in the treatment of non-small cell lung cancer and pancreatic cancer.

5 Must Know Facts For Your Next Test

1. Erlotinib is particularly effective in patients with specific mutations in the EGFR gene, which make tumors more responsive to this therapy.
2. This drug is usually taken orally and has a half-life that allows for once-daily dosing, making it more convenient for patients.
3. Common side effects of erlotinib include skin rash, diarrhea, and liver enzyme abnormalities, which are often manageable with supportive care.
4. Erlotinib is sometimes used in combination with chemotherapy to enhance treatment efficacy in advanced cancer cases.
5. Resistance to erlotinib can develop over time, often due to secondary mutations in the EGFR gene or activation of alternative signaling pathways.

Review Questions

• How does erlotinib specifically target cancer cells compared to traditional chemotherapy?
  • Erlotinib targets cancer cells by specifically inhibiting the EGFR tyrosine kinase, which is often overactive in certain types of tumors. Unlike traditional chemotherapy that attacks all rapidly dividing cells, erlotinib is more selective, aiming at the molecular mechanisms driving tumor growth. This targeted approach can lead to fewer side effects and a more effective treatment for patients with tumors expressing high levels of EGFR.
• What are some common post-translational modifications that might affect the efficacy of erlotinib?
  • Post-translational modifications such as phosphorylation can significantly impact the function of proteins involved in cell signaling pathways related to EGFR. If key proteins are phosphorylated or otherwise modified after translation, it may alter their interaction with erlotinib or contribute to resistance mechanisms. Understanding these modifications can help identify biomarkers for response to erlotinib and tailor treatments accordingly.
• Evaluate the implications of developing resistance to erlotinib on future cancer treatment strategies.
  • Developing resistance to erlotinib has major implications for future cancer treatment strategies as it highlights the need for personalized medicine approaches. Identifying the specific mutations or alternative pathways that lead to resistance can guide clinicians in selecting subsequent therapies, such as newer generation EGFR inhibitors or combination therapies that target multiple pathways. This evolving landscape emphasizes the importance of ongoing research into tumor biology and treatment adaptation based on genetic profiling.

Related terms

EGFR: Epidermal Growth Factor Receptor, a cell surface receptor that, when activated, triggers signaling pathways involved in cell division and survival.

Tyrosine Kinase Inhibitors: A class of drugs that inhibit the activity of enzymes known as tyrosine kinases, which play a crucial role in many cellular processes, including cancer progression.

Post-translational Modification: The chemical modification of a protein after its translation, which can affect the protein's function, localization, and stability.