易瑞沙中文说明书（Iressa Chinese instructions）.docVIP

易瑞沙中文说明书（Iressa Chinese instructions） IRESSA. [drug name] generic name: gefitinib The main ingredient of this product is gefitinib. Its chemical name is N - (3 - chloro - phenyl) - 7 methoxy - 6 - (3 - morpholine) - quinazoline - 4 - amines Molecular formula: C22H24CLFN4O3 Molecular weight: 446.90 [pharmacological toxicity] pharmacodynamics characteristics Gefitinib is a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that is normally expressed in epithelial derived solid tumors. Gefitinib inhibits the growth of human tumor cells and inhibits angiogenesis in nude mice. In vitro, it can increase the apoptosis of human tumor cell derived lines and inhibit the invasion and secretion of angiogenic factors. In animal experiments or in vitro studies have confirmed that gefitinib can improve the antitumor activity of chemotherapy, radiotherapy and hormone therapy. Toxicological studies Non clinical (off) studies suggest that gefitinib has the potential to inhibit repolarization (e.g., QT interval) of cardiac action potentials. However, safety data obtained by clinical studies and postmarketing surveillance did not suggest any adverse effects of gefitinib on the heart. Carcinogenic, teratogenic, and reproductive toxicity Carcinogenicity study of gefitinib was not carried out. Gefitinib was not genotoxic in gene mutation analysis (bacterial and mammalian cells in vitro) and lysis tests (in vitro mammalian and in vivo micronucleus tests in rats). The dose of gefitinib 20mg/kg/ days (4 times the body surface area) was 0.7 times longer than 7 days before mating, which could affect ovulation in female rats, resulting in a decrease in the total corpus luteum volume. In the organ, hair and period, gefitinib, which could produce a maternal toxicity dose, was observed in rats; the incidence of osteogenesis was increased and fetal weight loss was observed in rabbits. Malformations were not observed in rats, and abnormalities were observed only in rabbits a