Apatinib: A novel receptor tyrosine kinase inhibitor for the treatment of gastric cancer

被引：291

作者：

Roviello, Giandomenico ^{[1
,2
,3
]}

Ravelli, Andrea ^{[3
,4
]}

Polom, Karol ^{[5
,6
]}

Petrioli, Roberto ^{[7
]}

Marano, Luigi ^{[8
]}

Marrelli, Daniele ^{[9
]}

Roviello, Franco ^{[5
,6
]}

Generali, Daniele ^{[3
,10
]}

机构：

[1] Univ Brescia, Dept Mol & Translat Med, Pharmacol Sect, Viale Europa 11, I-25124 Brescia, Italy

[2] Univ Brescia, Dept Mol & Translat Med, Univ Ctr DIFF Drug Innovat Forward Future, Viale Europa 11, I-25124 Brescia, Italy

[3] AO Azienda Ist Ospitalieri Cremona, Unit Mol Therapy & Pharmacogen, Viale Concordia 1, I-26100 Cremona, Italy

[4] Univ Parma, Sect Expt Oncol, Dept Clin & Expt Med, Via Univ 12, I-43121 Parma, Italy

[5] Univ Siena, Dept Med Surg & Neurosci, Viale Bracci 11, I-53100 Siena, Italy

[6] Univ Siena, Unit Gen & Minimally Invas Surg, Viale Bracci 11, I-53100 Siena, Italy

[7] Univ Siena, Med Oncol Unit, Viale Bracci 11, I-53100 Siena, Italy

[8] San Matteo degli Infermi Hosp, Dept Surg, Gen Minimally Invas & Robot Surg, ASL Umbria 2, I-06049 Spoleto, Italy

[9] Univ Siena, Sect Adv Surg Oncol, Dept Med Surg & Neurosci, Viale Bracci 11, I-53100 Siena, Italy

[10] Univ Trieste, Dept Med Surg & Hlth Sci, Piazza Ospitale 1, I-34129 Trieste, Italy

来源：

CANCER LETTERS | 2016年 / 372卷 / 02期

关键词：

Gastric cancer; Apatinib; VEGFR2; ENDOTHELIAL GROWTH-FACTOR; GASTROESOPHAGEAL JUNCTION; PHASE-II; ANTITUMOR-ACTIVITY; DOUBLE-BLIND; MULTICENTER; EPIRUBICIN; THERAPY; VEGF; ANGIOGENESIS;

D O I：

10.1016/j.canlet.2016.01.014

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 [肿瘤学];

摘要：

Metastatic gastric cancer is a lethal disease characterized by a very short overall survival, underlining a critical need of new therapeutic options. Unfortunately, although several molecular targets have been investigated, only very few recently approved agents, such as trastuzumab in the HER2-positive setting and ramucirumab, led to a clinical improvement in the outcome of metastatic gastric cancer patients. VEGF (vascular endothelial growth factor) is one of the most potent angiogenic factors and is a signalling molecule secreted by many solid tumours. Since high VEGF expression is one of the characteristic features of gastric carcinomas, targeting VEGF is therefore considered as a promising therapeutic strategy for gastric cancer. In the scenario of possible new target therapies with particular regard to angiogenesis, apatinib is a novel receptor tyrosine kinase inhibitor selectively targeting VEGFR-2. It is an orally-bioavailable agent currently being studied in several solid tumour types showing a promising activity in gastric cancer. Due to the recent positive results as a third line of treatment for metastatic gastric cancer patients, apatinib may be an interesting and novel type of targeted treatment for metastatic gastric cancer in several lines of therapy. In this review, we summarize the available data of apatinib, mainly focused on the clinical aspect, in advanced/metastatic gastric cancer. (C) 2016 Elsevier Ireland Ltd. All rights reserved.

引用

页码：187 / 191

页数：5

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