Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang, China.
Expert Opin Ther Pat. 2021 Mar;31(3):223-238. doi: 10.1080/13543776.2021.1860210. Epub 2020 Dec 14.
: EGFR is the receptor for epidermal growth factor (EGF) and belongs to the protein tyrosine kinase (PTK) receptor. It is closely related to the inhibition of tumor cell proliferation, invasion, and apoptosis. Overexpression or mutation activation of EGFR is involved in the development of many human malignancies, especially non-small cell lung cancer (NSCLC). At present, numerous small molecule tyrosine kinase inhibitors (TKIs) have been developed to target the ATP-binding region of EGFR, aiming to develop selective and effective inhibitors for the treatment of NSCLC against EGFR mutants.: This review covers the latest progress in the patented EGFR inhibitors and the inhibition activity against NSCLC from 2014 to present.: EGFR is an important anti-tumor target, and small molecule inhibitors targeting EGFR have become important biologically active compounds for the treatment of cancer, especially against NSCLC. Among the recent patents available, great majority of them focus on selective inhibitors of EGFR mutants. Although great achievements have been made in the development of selective EGFR inhibitors, there is still an urgent need to discover new EGFR inhibitors which are safe, efficient, selective, and low-toxic to avoid the adverse pharmacokinetics caused by wild-type EGFR feature.
表皮生长因子受体（EGFR）是表皮生长因子（EGF）的受体，属于蛋白酪氨酸激酶（PTK）受体。它与抑制肿瘤细胞增殖、侵袭和凋亡密切相关。EGFR 的过度表达或突变激活与许多人类恶性肿瘤的发生有关，特别是非小细胞肺癌（NSCLC）。目前，已经开发出许多针对 EGFR ATP 结合区域的小分子酪氨酸激酶抑制剂（TKI），旨在开发针对 EGFR 突变体的选择性和有效的 NSCLC 治疗药物。
本综述涵盖了 2014 年至今 EGFR 抑制剂的最新专利进展及对 NSCLC 的抑制活性。
EGFR 是一个重要的抗肿瘤靶点，针对 EGFR 的小分子抑制剂已成为治疗癌症，特别是 NSCLC 的重要生物活性化合物。在现有的最新专利中，绝大多数都集中在针对 EGFR 突变体的选择性抑制剂上。尽管在开发选择性 EGFR 抑制剂方面已经取得了巨大的成就，但仍然迫切需要发现新的 EGFR 抑制剂，这些抑制剂安全、高效、选择性强、毒性低，以避免野生型 EGFR 特征引起的不良药代动力学。
