- Erlotinib is a highly selective and potent tyrosine kinase inhibitor (TKI) that targets the epidermal growth factor receptor (EGFR), specifically binding to the ATP-binding domain of the receptor’s intracellular tyrosine kinase region.
- As a small molecule inhibitor, Erlotinib exhibits high specificity for EGFR and is particularly effective against tumors harboring activating EGFR mutations, such as exon 19 deletions and the L858R point mutation in exon 21.
- The mechanism of action of Erlotinib involves reversible competitive inhibition of ATP binding at the EGFR tyrosine kinase domain. By blocking ATP access, Erlotinib prevents receptor autophosphorylation and subsequent activation of downstream signaling pathways essential for cell survival and proliferation. This inhibition is particularly potent in cancer cells with constitutively active EGFR mutations, leading to significant antitumor effects.
- Through EGFR inhibition, Erlotinib effectively disrupts multiple oncogenic signaling cascades, including the RAS/RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, and JAK/STAT pathway. The suppression of these critical signaling networks results in reduced cell proliferation, increased apoptosis, and impaired angiogenesis, ultimately inhibiting tumor progression in EGFR-dependent malignancies.
- Erlotinib has demonstrated substantial clinical efficacy, particularly in non-small cell lung cancer (NSCLC) and pancreatic cancer, where EGFR plays a crucial role in tumor growth and survival. Its role in targeted therapy has significantly advanced precision medicine in oncology, offering improved treatment outcomes for patients with EGFR-mutant NSCLC.
- Additionally, the molecular characteristics of Erlotinib have made it an essential tool for studying EGFR-driven oncogenesis and for developing novel strategies to overcome resistance mechanisms, such as secondary EGFR mutations and alternative signaling pathway activation.
Disclaimer: While we strive to continuously improve and update our content, we cannot guarantee its accuracy or completeness. Please note that the content is continuously evolving, and updates may not reflect the most current information. The information contained on this website is for general informational purposes only and should not be considered as professional advice. We disclaim any liability for any loss or damage resulting from the use of the information provided herein. Always consult qualified professionals for specific guidance and verify any critical information before relying on it. Read more
