Therapeutic Approaches for the Treatment of Epidermal Growth Factor Receptor Mutated Lung Cancer

Curr Cancer Drug Targets. 2018;18(8):773-791. doi: 10.2174/1568009617666170623123848.

Abstract

Lung cancer surfaces to be the predominant determinant of mortality worldwide constituting 13% and 19% of all new cancer cases and deaths related to cancer respectively. Molecular profiling has now become a regular trend in lung cancer to identify the driver mutations. Epidermal Growth Factor Receptor (EGFR) is the most regular driver mutation encountered in Non-Small Cell Lung Cancer (NSCLC). Targeted therapies are now available for the treatment of EGFR mutant NSCLC. EGFR mutation is more frequently expressed in adenocarcinoma than squamous cell carcinoma. This article presents a detailed molecular insight of the therapeutic approaches for the treatment of EGFR mutant lung cancer. The article delineates molecular mechanism of the drugs that are approved, the drugs that are in clinical trial and the drugs that have not entered a clinical trial but shows promising future in the treatment of EGFR mutant lung cancer. Furthermore, this article provides concise information on relevant combinational or monotherapy clinical trials that have been completed for various approaches.

Keywords: Lung cancer; epidermal growth factor receptor; epidermal growth factor receptor protein-tyrosine kinase; heat-shock protein; histone deacetylase; monoclonal antibodies; ubiquitin..

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Agents, Immunological / metabolism
  • Antineoplastic Agents, Immunological / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Drug Resistance, Neoplasm
  • Endopeptidases
  • Endosomal Sorting Complexes Required for Transport / antagonists & inhibitors
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors
  • Histone Deacetylase Inhibitors / metabolism
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Humans
  • Lung Neoplasms / drug therapy*
  • Molecular Targeted Therapy
  • Mutation
  • Protein Kinase Inhibitors / metabolism
  • Protein Kinase Inhibitors / therapeutic use*
  • Ubiquitin Thiolesterase / antagonists & inhibitors

Substances

  • Antineoplastic Agents
  • Antineoplastic Agents, Immunological
  • Endosomal Sorting Complexes Required for Transport
  • HSP90 Heat-Shock Proteins
  • Histone Deacetylase Inhibitors
  • Protein Kinase Inhibitors
  • EGFR protein, human
  • ErbB Receptors
  • Endopeptidases
  • USP8 protein, human
  • Ubiquitin Thiolesterase