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厄洛替尼的特性及其在治疗晚期卵巢癌中的潜力。

Profile of erlotinib and its potential in the treatment of advanced ovarian carcinoma.

机构信息

Department of Oncology, McMaster University, Hamilton, ON, Canada.

出版信息

Onco Targets Ther. 2013 Apr 18;6:427-35. doi: 10.2147/OTT.S30373. Print 2013.

DOI:10.2147/OTT.S30373
PMID:23723710
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3665572/
Abstract

The epidermal growth-factor receptor (EGFR) is overexpressed in the majority of epithelial ovarian cancers and promotes cell proliferation, migration and invasion, and angiogenesis, as well as resistance to apoptosis. This makes EGFR an attractive therapeutic target in this disease. A number of strategies to block EGFR activity have been developed, including small-molecular-weight tyrosine kinase inhibitors such as erlotinib. Erlotinib has been evaluated as a single agent in recurrent ovarian cancer, as well as in combination with chemotherapeutic agents in the first-line and recurrent settings, and in combination with the antiangiogenic agent bevacizumab in the recurrent setting, as well as in the maintenance setting after completion of first-line chemotherapy. Unfortunately, erlotinib has shown only minimal efficacy as a single agent, and it has not enhanced the effects of chemotherapy or bevacizumab when combined with these agents. Ongoing and future studies of erlotinib and other agents blocking EGFR will need to define mechanisms resulting in resistance to such interventions, and to validate biomarkers of response to identify patients most likely to benefit from such approaches.

摘要

表皮生长因子受体(EGFR)在大多数上皮性卵巢癌中过度表达,促进细胞增殖、迁移和侵袭以及血管生成,并导致细胞凋亡抵抗。这使得 EGFR 成为该疾病有吸引力的治疗靶点。已经开发了许多阻断 EGFR 活性的策略,包括小分子酪氨酸激酶抑制剂,如厄洛替尼。厄洛替尼已被评估为复发性卵巢癌的单一药物,以及在一线和复发性治疗中与化疗药物联合使用,以及在复发性治疗中与抗血管生成药物贝伐珠单抗联合使用,以及在一线化疗完成后的维持治疗中。不幸的是,厄洛替尼作为单一药物的疗效仅为轻度,并且与这些药物联合使用并未增强化疗或贝伐珠单抗的效果。正在进行和未来的厄洛替尼和其他阻断 EGFR 的药物研究将需要确定导致对这些干预措施产生耐药性的机制,并验证反应的生物标志物,以确定最有可能从这些方法中受益的患者。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b9/3665572/f779a14e9240/ott-6-427Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b9/3665572/20b32c86b790/ott-6-427Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b9/3665572/f779a14e9240/ott-6-427Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b9/3665572/20b32c86b790/ott-6-427Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b9/3665572/f779a14e9240/ott-6-427Fig2.jpg

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