Erlotinib

Profiles Drug Subst Excip Relat Methodol. 2020:45:93-117. doi: 10.1016/bs.podrm.2019.10.004. Epub 2019 Dec 6.

Abstract

Erlotinib (OSI-774), marketed by Genentech as Tarceva®, is anticancer drug approved by US-FDA for the treatment of Non-Small Cell Lung Cancer (NSCLC) and Pancreatic Cancer. Erlotinib inhibited epidermal growth factor receptor (EGFR) that blocks tumor cell division, produces cell cycle arrest, and initiates programmed cell death in EGFR-overexpressing human tumor cells. This study presents a comprehensive profile of erlotinib, including detailed nomenclature, formula, elemental analysis, methods of preparation, physico-chemical characteristics, and methods of analysis (including spectroscopic, electrochemical, and chromatographic methods of analysis). Spectroscopic and spectrometric analyses include UV/vis spectroscopy, vibrational spectroscopy, nuclear magnetic resonance spectrometry ((1)H and (13)C NMR), and mass spectrometry. Chromatographic methods of analyses include thin layer chromatography, and high-performance liquid chromatography. Pharmacology of erlotinib including pharmacodynamics, mechanism of action, pharmacokinetics and drug-drug interactions were also presented. An appropriate table and figures were attached to each of the above mentioned sections along with total of 48 references.

Keywords: Cancer drug; Drug-drug interactions; Erlotinib; Non-small cell lung cancer (NSCLC) and pancreatic cancer; Tyrosine kinase inhibitors.

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Erlotinib Hydrochloride / pharmacology*
  • Humans
  • Lung Neoplasms / drug therapy
  • Pancreatic Neoplasms / drug therapy
  • Protein Kinase Inhibitors / pharmacology*

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Erlotinib Hydrochloride