Abdelgalil Ahmed A, Al-Kahtani Hamad M, Al-Jenoobi Fahad I
Central Laboratory, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Profiles Drug Subst Excip Relat Methodol. 2020;45:93-117. doi: 10.1016/bs.podrm.2019.10.004. Epub 2019 Dec 6.
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.
厄洛替尼（OSI-774），由基因泰克公司以特罗凯®的名称上市销售，是一种经美国食品药品监督管理局批准用于治疗非小细胞肺癌（NSCLC）和胰腺癌的抗癌药物。厄洛替尼可抑制表皮生长因子受体（EGFR），该受体能阻断肿瘤细胞分裂、使细胞周期停滞，并在EGFR过表达的人类肿瘤细胞中引发程序性细胞死亡。本研究全面介绍了厄洛替尼，包括详细的命名、分子式、元素分析、制备方法、物理化学特性以及分析方法（包括光谱、电化学和色谱分析方法）。光谱和光谱分析包括紫外/可见光谱、振动光谱、核磁共振光谱（（1）H和（13）C NMR）以及质谱。色谱分析方法包括薄层色谱和高效液相色谱。文中还介绍了厄洛替尼的药理学，包括药效学、作用机制、药代动力学和药物相互作用。上述各部分均附有合适的表格和图表，以及总共48篇参考文献。
