Rational application of gefitinib in NSCLC patients with sensitive EGFR mutations based on pharmacokinetics and metabolomics

• Published in: Acta pharmacologica Sinica Vol. 43; no. 7; pp. 1857 - 1864
• Main Authors: Feng, Wei, Chen, Xi, Guan, Shao-xing, Ruan, Hong-lian, Huang, Yan, Zhang, Hui-zhen, Yang, Yun-peng, Fang, Wen-feng, Zhao, Hong-yun, Zhuang, Wei, Xin, Shuang, Chen, You-hao, Wang, Fei, Gao, Yue, Huang, Min, Wang, Xue-ding, Zhang, Li
• Format: Journal Article
• Language: English
• Published: Singapore Springer Nature Singapore 01.07.2022; Nature Publishing Group
• Subjects: Animals; Antineoplastic Agents - adverse effects; Biomedical and Life Sciences; Biomedicine; Blood-brain barrier; Brain cancer; Brain tumors; Carcinoma, Non-Small-Cell Lung - drug therapy; Carcinoma, Non-Small-Cell Lung - genetics; Carcinoma, Non-Small-Cell Lung - pathology; Epidermal growth factor receptors; ErbB Receptors - genetics; ErbB Receptors - metabolism; Gefitinib; Gefitinib - therapeutic use; Humans; Immunology; Inhibitor drugs; Internal Medicine; Lung cancer; Lung Neoplasms - drug therapy; Lung Neoplasms - genetics; Lung Neoplasms - pathology; Medical Microbiology; Metabolites; Metabolomics; Metastases; Metastasis; Mice; Mutation; Non-small cell lung carcinoma; Patients; Pharmacokinetics; Pharmacology/Toxicology; Plasma; Protein Kinase Inhibitors - pharmacology; Protein Kinase Inhibitors - therapeutic use; Quinazolines - pharmacology; Quinazolines - therapeutic use; Small cell lung carcinoma; Targeted cancer therapy; Vaccine; pharmacokinetics; EGFR mutations; gefitinib; NSCLC; metabolomics

Gefitinib has been available in the market for 20 years, but its pharmacokinetic mechanism of response is little known. In this study, we examined the pharmacokinetic and metabolomic profiles in non-small cell lung cancer (NSCLC) patients with sensitive EGFR mutations. A total of 216 advanced NSCLC...