Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
Drugs. 2018 May;78(7):747-758. doi: 10.1007/s40265-018-0903-9.
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.
阿帕替尼[艾坦（中国商品名）]，又称维莫非尼，是一种新型小分子、选择性血管内皮生长因子受体-2（VEGFR-2）酪氨酸激酶抑制剂，是继重组人血管内皮抑制素后在中国获批用于治疗晚期或转移性胃腺癌的第二种抗血管生成药物。本文总结了阿帕替尼的药理学特性，并综述了其在化疗后进展或复发的晚期胃腺癌（包括胃食管腺癌）或其他晚期癌症（如非小细胞肺癌、乳腺癌、妇科癌症、肝细胞癌、甲状腺癌和肉瘤）患者中的临床应用。作为三线或四线治疗药物，口服阿帕替尼与安慰剂相比，显著延长了晚期或转移性胃腺癌或胃食管腺癌患者的中位无进展生存期（PFS）和总生存期（OS），且在中国患者中的安全性特征可控。在随机、双盲、多中心、Ⅱ期和Ⅲ期临床试验中，有限的证据也支持阿帕替尼在其他晚期或转移性实体瘤（包括非小细胞肺癌、乳腺癌和肝细胞癌）患者中作为二线治疗药物的应用。需要进一步的临床经验和长期药物警戒数据，以更明确地确定阿帕替尼的疗效和安全性，包括其与其他化疗药物联合应用的效果及其在其他类型晚期或转移性实体瘤治疗中的作用。在此期间，鉴于其方便的给药方案以及晚期或转移性实体瘤患者有限的治疗选择和较差的预后，阿帕替尼是化疗后进展或复发的晚期胃腺癌或胃食管腺癌成人患者的一种重要的新兴治疗选择。
