title: Apatinib: A novel receptor tyrosine kinase inhibitor for the treatment of gastric cancer.
abstract: 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.
authors.affiliation: Section of Pharmacology and University Center DIFF - Drug Innovation Forward Future, Department of Molecular and Translational Medicine, University of Brescia, Viale Europa 11, 25124 Brescia, Italy; Unit of Molecular Therapy and Pharmacogenomic, AO Azienda Istituti Ospitalieri di Cremona, Viale Concordia 1, 26100 Cremona, Italy. Electronic address: giandomenicoroviello@hotmail.it.
authors.forename: Giandomenico
authors.initials: G
authors.lastname: Roviello
authors.affiliation: Unit of Molecular Therapy and Pharmacogenomic, AO Azienda Istituti Ospitalieri di Cremona, Viale Concordia 1, 26100 Cremona, Italy; Section of Experimental Oncology, Department of Clinical and Experimental Medicine, University of Parma, Via Università, 12, 43121 Parma, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Ravelli
authors.affiliation: Department of Medical, Surgical and Neuroscience; Unit of General and Minimally Invasive Surgery, University of Siena, Viale Bracci 11, 53100 Siena, Italy.
authors.forename: Karol
authors.initials: K
authors.lastname: Polom
authors.affiliation: Medical Oncology Unit, University of Siena, Viale Bracci 11, 53100 Siena, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Petrioli
authors.affiliation: General, Minimally Invasive and Robotic Surgery, Department of Surgery, "San Matteo degli Infermi" Hospital, ASL Umbria 2, 06049 Spoleto, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Marano
authors.affiliation: Department of Medical, Surgical and Neurosciences, Section of Advanced Surgical Oncology, University of Siena, Viale Bracci 11, 53100 Siena, Italy.
authors.forename: Daniele
authors.initials: D
authors.lastname: Marrelli
authors.affiliation: Department of Medical, Surgical and Neuroscience; Unit of General and Minimally Invasive Surgery, University of Siena, Viale Bracci 11, 53100 Siena, Italy.
authors.forename: Franco
authors.initials: F
authors.lastname: Roviello
authors.affiliation: Unit of Molecular Therapy and Pharmacogenomic, AO Azienda Istituti Ospitalieri di Cremona, Viale Concordia 1, 26100 Cremona, Italy; Department of Medical, Surgery and Health Sciences, University of Trieste, Piazza Ospitale 1, 34129 Trieste, Italy.
authors.forename: Daniele
authors.initials: D
authors.lastname: Generali
mesh_terms: D020533:Angiogenesis Inhibitors / Q000627:therapeutic use*; D000818:Animals; D006801:Humans; D058990:Molecular Targeted Therapy; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011725:Pyridines / Q000627:therapeutic use*; D015398:Signal Transduction / Q000187:drug effects; D013274:Stomach Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000473:pathology; D016896:Treatment Outcome; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D020533:Angiogenesis Inhibitors; D047428:Protein Kinase Inhibitors; D011725:Pyridines; C553458:apatinib; C000588866:KDR protein, human; D040301:Vascular Endothelial Growth Factor Receptor-2
keywords: Apatinib; Gastric cancer; VEGFR2