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靶向成纤维细胞生长因子受体治疗非小细胞肺癌的研究性药物。

Investigational drugs targeting fibroblast growth factor receptor in the treatment of non-small cell lung cancer.

作者信息

Rijavec Erika, Genova Carlo, Barletta Giulia, Biello Federica, Rossi Giovanni, Tagliamento Marco, Dal Bello Maria Giovanna, Coco Simona, Vanni Irene, Boccardo Simona, Alama Angela, Grossi Francesco

机构信息

a UOS Tumori Polmonari , IRCCS AOU San Martino IST- Istituto Nazionale per la Ricerca sul Cancro , Genova , Italy.

b Dipartimento di Medicina Interna e Specialità Mediche (DIMI) , Università di Genova , Genova , Italy.

出版信息

Expert Opin Investig Drugs. 2017 May;26(5):551-561. doi: 10.1080/13543784.2017.1316714. Epub 2017 Apr 13.

DOI:10.1080/13543784.2017.1316714
PMID:28388262
Abstract

Fibroblast growth factor receptor (FGFR) due to its central role in regulating cell survival, is a promising target for cancer therapeutics. Dysregulation of the FGFR pathway has been observed in several malignancies, including non-small cell lung cancer (NSCLC) particularly in patients with squamous histology. Areas covered: The aim of this article is to review the most relevant findings of clinical trials investigating drugs targeting FGFR pathway: such as FGFR tyrosine kinase inhibitors (TKIs), FGFR monoclonal antibodies and FGF ligand traps in NSCLC patients. Expert opinion: At present, clinical activity of drugs targeting FGFR in NSCLC is disappointing. Further studies are needed in order to better identify patients who might benefit from these drugs and to clarify the mechanisms of resistance to these compounds.

摘要

成纤维细胞生长因子受体(FGFR)因其在调节细胞存活中的核心作用,是癌症治疗的一个有前景的靶点。FGFR通路失调已在多种恶性肿瘤中被观察到,包括非小细胞肺癌(NSCLC),尤其是鳞状组织学类型的患者。涵盖领域:本文旨在综述针对FGFR通路的药物的临床试验的最相关研究结果:如FGFR酪氨酸激酶抑制剂(TKIs)、FGFR单克隆抗体和FGF配体陷阱在NSCLC患者中的应用。专家观点:目前,针对NSCLC中FGFR的药物的临床活性令人失望。需要进一步研究以更好地识别可能从这些药物中获益的患者,并阐明对这些化合物的耐药机制。

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