EGFR INHIBITORS: ROLE IN CANCER THERAPY

Sharba Tasneem, Garima Verma, Mohemmed Faraz Khan, Dr. Syed Rashiduddin Haider*, Mohammad Mumtaz Alam, Dr. Mohammad Shaquiquzzaman*

ABSTRACT

Among various strategies for cancer therapy, molecular targeting has been reported to have better potential to provide tumor specificity. One particular molecular target of high promise in oncology is the Epidermal Growth Factor Receptor (EGFR). EGFR is overexpressed, dysregulated or mutated in many epithelial malignancies, responsible for tumor growth and progress. EGFR belongs to ErbB family of Receptor Tyrosine Kinases (RTK). These are trans-membrane proteins which are activated by binding with peptide growth factors of the Epidermal Growth Factor family of proteins. The growth and survival of carcinoma cells appear to be sustained by a network of receptors/ligands of ErbB family. It has been found that in cancer patients, EGFR gene amplification and EGFR tyrosine kinase domain mutation occur. This phenomenon is also important for therapeutic approaches, since the response to anti-EGFR agents might depend on the total level of expression of ErbB receptors and ligands in tumor cells. A number of agents targeting EGFR include specific antibodies directed against its ligand-binding domain and small molecules inhibiting tyrosine kinase activity are either in clinical trials or are already approved for clinical treatment. This article deals with the role of various approved EGFR inhibitors in the treatment of different type of cancer.

Keywords: Epidermal growth factor receptors, Receptor Tyrosin kinases, Colorectal cancer, Head and neck squamous cell carcinoma.