Apatinib: A Review in Advanced Gastric Cancer and Other Advanced Cancers

Apatinib [Aitan ® (brand name in China)], also known as rivoceranib, is a novel, small molecule, selective vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor and is the second anti-angiogenic drug to be approved in China for the treatment of advanced or metastatic gast...

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Veröffentlicht in:Drugs (New York, N.Y.) N.Y.), 2018-05, Vol.78 (7), p.747-758
1. Verfasser: Scott, Lesley J.
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description Apatinib [Aitan ® (brand name in China)], also known as rivoceranib, is a novel, small molecule, selective vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor and is the second anti-angiogenic drug to be approved in China for the treatment of advanced or metastatic gastric cancer. This article summarizes the pharmacological properties of apatinib and reviews its clinical use in chemotherapy-experienced patients with advanced gastric adenocarcinoma, including gastroesophageal adenocarcinoma (GEA), or with other advanced cancers such as non-small cell lung cancer (NSCLC), breast cancer, gynaecological cancers, hepatocellular carcinoma (HCC), thyroid cancer and sarcomas. As third- or subsequent-line therapy, oral apatinib significantly prolonged median progression-free survival (PFS) and overall survival (OS) compared with placebo and had a manageable safety profile in Chinese patients with advanced or metastatic gastric cancer or GEA participating in randomized, double-blind, multicentre, phase 2 and 3 trials. More limited evidence also supports it use as subsequent-line treatment in Chinese patients with other advanced or metastatic solid tumours, including NSCLC, breast cancer and HCC. Further clinical experience and long-term pharmacovigilance data are required to more definitively establish the efficacy and safety profile of apatinib, including its use in combination with other chemotherapy agents and its role in the management of other types of advanced or metastatic solid tumours. In the meantime, given its convenient administration regimen and the limited treatment options and poor prognosis for patients with advanced or metastatic solid tumours, apatinib is an important, emerging treatment option for adult patients with advanced gastric adenocarcinoma or GEA who have progressed or relapsed after chemotherapy.
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This article summarizes the pharmacological properties of apatinib and reviews its clinical use in chemotherapy-experienced patients with advanced gastric adenocarcinoma, including gastroesophageal adenocarcinoma (GEA), or with other advanced cancers such as non-small cell lung cancer (NSCLC), breast cancer, gynaecological cancers, hepatocellular carcinoma (HCC), thyroid cancer and sarcomas. As third- or subsequent-line therapy, oral apatinib significantly prolonged median progression-free survival (PFS) and overall survival (OS) compared with placebo and had a manageable safety profile in Chinese patients with advanced or metastatic gastric cancer or GEA participating in randomized, double-blind, multicentre, phase 2 and 3 trials. More limited evidence also supports it use as subsequent-line treatment in Chinese patients with other advanced or metastatic solid tumours, including NSCLC, breast cancer and HCC. Further clinical experience and long-term pharmacovigilance data are required to more definitively establish the efficacy and safety profile of apatinib, including its use in combination with other chemotherapy agents and its role in the management of other types of advanced or metastatic solid tumours. In the meantime, given its convenient administration regimen and the limited treatment options and poor prognosis for patients with advanced or metastatic solid tumours, apatinib is an important, emerging treatment option for adult patients with advanced gastric adenocarcinoma or GEA who have progressed or relapsed after chemotherapy.</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>29663291</pmid><doi>10.1007/s40265-018-0903-9</doi><tpages>12</tpages></addata></record>
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subjects Adenocarcinoma
Adis Drug Evaluation
Angiogenesis
Antineoplastic Agents - therapeutic use
Apoptosis
Biomarkers
Bone cancer
Brand names
Breast cancer
Cancer
Cancer therapies
Cell adhesion & migration
Chemotherapy
Clinical medicine
Clinical trials
Cost analysis
Drugs
Enzyme inhibitors
Gastric cancer
Growth factors
Gynecology
Humans
Internal Medicine
Liver cancer
Lung cancer
Medical prognosis
Medicine
Medicine & Public Health
Metastases
Metastasis
Neoplasms - drug therapy
Neoplasms - pathology
Non-small cell lung carcinoma
Patients
Pharmacology
Pharmacology/Toxicology
Pharmacotherapy
Pharmacovigilance
Phosphorylation
Physiology
Protein Kinase Inhibitors - therapeutic use
Protein-tyrosine kinase
Pyridines - therapeutic use
Safety management
Solid tumors
Stomach Neoplasms - drug therapy
Stomach Neoplasms - pathology
Survival
Thyroid
Thyroid cancer
Treatment Outcome
Tumors
Tyrosine
Vascular endothelial growth factor
Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors
Vascular endothelial growth factor receptors
title Apatinib: A Review in Advanced Gastric Cancer and Other Advanced Cancers
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