共查询到14条相似文献,搜索用时 62 毫秒
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1例49岁男性患者因肺腺癌Ⅳ期接受化疗,具体方案为培美曲塞二钠0.8 g入0.9%氯化钠注射液100 ml静脉滴注、第1天,顺铂30 mg入0.9%氯化钠注射液250 ml静脉滴注、第1~4天,21 d为1个周期;同时给予靶向治疗,吉非替尼口服250 mg、1次/d。在第3个化疗周期停药第10天、服用吉非替尼第59天,... 相似文献
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目的 改进和优化吉非替尼的合成工艺,便于工业化生产.方法 以3,4-二甲氧基苯甲醛为原料,先硝化,后依次脱甲基、侧链烷基化、醛基转化为氰基、氰基氧化成酰胺、还原、闭环、氯代最后与3-氯-4-氟苯胺反应合成了抗肿瘤药物吉非替尼.结果 总收率约23.6%,产物经核磁共振氢谱、质谱、元素分析确证其结构为目标产物.结论 ... 相似文献
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王莉 《现代食品与药品杂志》2011,(12)
目的改进和优化吉非替尼的合成工艺,便于工业化生产。方法以3,4-二甲氧基苯甲醛为原料,先硝化,后依次脱甲基、侧链烷基化、醛基转化为氰基、氰基氧化成酰胺、还原、闭环、氯代最后与3-氯-4-氟苯胺反应合成了抗肿瘤药物吉非替尼。结果总收率约23.6%,产物经核磁共振氢谱、质谱、元素分析确证其结构为目标产物。结论该工艺在分离纯化过程中不需过柱,原料价格便宜,条件温和,操作简单,适合于工业化生产。 相似文献
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以3,4-二甲氧基苯甲酸为原料,经硝化、脱甲基、还原、环合、乙酰化、氯化、缩合、水解等反应,最后经过一步与N-(3-氯丙基)吗啉缩合得到抗肿瘤药吉非替尼。 相似文献
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先将3-羟基-4-甲氧基苯甲醛的醛基转化为氰基,再与N-(3-氯丙基)吗啉缩合,依次经硝化、氰基转化为酰胺、还原、环合得7-甲氧基-6-[3-(吗啉-4-基)丙氧基]-3,4-二氢喹唑啉-4-酮,最后经氯化、与3-氯-4-氟苯胺缩合得抗肿瘤药吉非替尼,总收率约36%。 相似文献
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Gefitinib 总被引:3,自引:0,他引:3
Gefitinib (ZD1839) is an orally active selective inhibitor of epidermal growth factor receptor tyrosine kinase, an enzyme that regulates intracellular signalling pathways implicated in the proliferation and survival of cancer cells. In human non-small cell lung cancer (NSCLC) cell lines and xenografts, gefitinib dose-dependently inhibited cellular proliferation and tumour growth, and potentiated the cytotoxic effects of chemotherapy and/or radiation. Gefitinib is orally bioavailable and is cleared via the cytochrome P450 3A4 pathway. In patients receiving gefitinib (50 to 700 mg/day) in phase I trials, steady-state plasma concentration was reached in 7 to 10 days. In patients with advanced NSCLC who had failed one or two prior chemotherapies, gefitinib 250 or 500mg once daily induced an objective response in approximately 19% of patients in a double-blind trial (n = 210). In another double-blind trial including 216 patients with NSCLC who had failed two or more prior chemotherapies, gefitinib 250 or 500mg once daily induced an objective response in 11.8 and 8.8% of patients, respectively; approximately 40% showed an improvement in disease-related symptoms. Gefitinib was generally well tolerated and the most common adverse events were mild skin rashes and diarrhoea. 相似文献
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The complexity of cancer chemotherapy requires pharmacists be familiar with the complicated regimens and highly toxic agents used. This column reviews various issues related to preparation, dispensing, and administration of antineoplastic therapy, and the agents, both commercially available and investigational, used to treat malignant diseases. Questions or suggestions for topics should be addressed to Dominic A. Solimando, Jr, President, Oncology Pharmacy Services, Inc., 4201 Wilson Blvd #110-545, Arlington, VA 22203, e-mail: ten.tsacmoc@cvSxRcnO; or J. Aubrey Waddell, Professor, University of Tennessee College of Pharmacy; Oncology Pharmacist, Pharmacy Department, Blount Memorial Hospital, 907 E. Lamar Alexander Parkway, Maryville, TN 37804, e-mail: ten.retrahc@ruofddaw.
Name: GefitinibSynonyms: Iressa, ZD1839 相似文献
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吉非替尼(gefitinib,1),化学名为N-(3-氯-4-氟苯基)-7-甲氧基-6-[3-(4-吗啉基)丙氧基]喹唑啉-4-胺,是英国AstraZeneca公司研发的表皮生长因子受体(EGFR)酪氨酸激酶抑制剂,于2002年首次在日本上市,2003年5月在美国及澳大利亚获准作为三线单一治疗药物用于晚期非小细胞肺癌,是第一个用于实体瘤治疗的针对特定靶点的小分子酪氨酸激酶抑制剂[1-4]. 相似文献