Apatinib: A Review in Advanced Gastric Cancer and Other Advanced Cancers
- 349 Downloads
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.
During the peer review process, the manufacturer of apatinib was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.
Compliance with Ethical Standards
The preparation of this review was not supported by any external funding.
Conflict of interest
Lesley Scott is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
- 15.Peng Q-A, Han Y-W, Zhang Y-L, et al. Apatinib inhibits VEGFR-2 and angiogenesis in an in vivo murine model of nasopharyngeal carcinoma. Oncotarget. 2017;8(32):52803–22.Google Scholar
- 20.Li J, Zhao X, Chen L, et al. Safety and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor YN968D1 in patients with advanced malignancies. BMC Cancer. 2010;10(529):1–8.Google Scholar
- 24.Yu W, He JH, Huang M, et al. Phase II study of apatinib in patients with advanced esophageal squamous cell carcinoma after failure of prior radiation and/or chemotherapy [abstract no. 119]. In: 14th World Conference of the Organization for Specialized Studies on the diseases of the Esophagus. 2017.Google Scholar
- 29.Liu X, Qin S, Wang Z, et al. Early presence of anti-angiogenesis-related adverse events as a potential biomarker of antitumor efficacy in metastatic gastric cancer patients treated with apatinib: a cohort study. J Hematol Oncol. 2017;10(153):1–9.Google Scholar
- 30.Feng J, Shen B, He Z, et al. Real world data about clinical efficacy and safety of apatinib in the treatment of advanced gastric cancer [abstract no. 695P]. Ann Oncol. 2017;28(Suppl 5).Google Scholar
- 31.Bai C, Zhang R, Ren X, et al. Prospective, multicenter, non-interventional and registry clinical study of apatinib in patients with advanced gastric cancer [abstract no. 137]. J Clin Oncol. 2018;36(4 Suppl).Google Scholar
- 32.Zhu H, Sun X, Zhou Q, et al. Clinical study of apatinib combined chemotherapy in the treatment of advanced gastric cancer [Chinese]. Chin J Clinl Oncol. 2016;8(6):394–6.Google Scholar
- 35.Wenying D, Qin S, Li J, et al. Initial dose of apatinib in Chinese patients with chemotherapy-refractory advanced or metastatic adenocarcinoma or gastroesophageal junction in third- and later-line setting: 500 mg or 850 mg? [abstract no. 35]. J Clin Oncol. 2018;36(4 Suppl).Google Scholar
- 36.Zhang L, Shi M, Huang C, et al. A phase II, multicenter, placebo-controlled trial of apatinib in patients with advanced nonsquamous non-small cell lung cancer (NSCLC) after two previous treatment regimens [abstract no. 7548]. J Clin Oncol. 2012;30(15 Suppl).Google Scholar
- 38.Wang SY, Liu Z, Ou W, et al. Apatinib monotherapy for advanced non-small cell lung cancer after the failure of chemotherapy or other targeted therapy [abstract no. e20626]. J Clin Oncol. 2017;35(15 Suppl).Google Scholar
- 41.Ying C, Wu Y. The addition of apatinib to gefitinib or icotinib for advanced non-small cell lung cancer with acquired resistance to first-generation epidermal growth factor receptor tyrosine kinase inhibitor: an assessment of effectiveness and safety [abstract no. 1351P]. Ann Oncol. 2017;28(Suppl 5):483.Google Scholar
- 44.Hu X, Cao J, Hu W, et al. Multicenter phase II study of apatinib in non-triple-negative metastatic breast cancer. BMC Cancer. 2014;14(820):1–8.Google Scholar
- 47.Zhu A, Yuan P, Wang J, et al. A real-world retrospective study of apatinib plus chemotherapy in metastatic breast cancer [abstract no. e12507]. J Clin Oncol. 2017;35(15 Suppl).Google Scholar
- 50.Zhang X, Lin Y. 500 mg versus 750 mg daily, pilot dose comparison of apatinib in Chinese patients with progressive radioiodine refractory differentiated thyroid cancer: initial experience of efficacy and safety [abstract no. 427]. Thyroid. 2017;27(Suppl 1):A148.Google Scholar
- 52.Xie C, Su M, Jin X. Apatinib as a salvage treatment in gynecologic cancer patients failed from two or more lines of prior chemotherapy [abstract no. e17009]. J Clin Oncol. 2017;35(15 Suppl).Google Scholar
- 53.Li L, Xiao S, Young KH, et al. Efficacy and safety of novel targeted drug apatinib in relapse and refractory non-Hodgkin lymphoma: an open-label, single-armed, exploratory study [abstract]. In: ASH 2017.Google Scholar
- 56.Yang W, Zhu B, Li J, et al. Response of advanced soft tissue sarcoma to apatinib: a retrospective analysis [abstract no. e22502]. J Clin Oncol. 2017;35(15 Suppl).Google Scholar
- 58.Yu W, Yu X, Wu S, et al. Apatinib for patients with unresectable high-grade osteosarcoma progressing after standard chemotherapy: a multi-center retrospective study [abstract no. 11031]. J Clin Oncol. 2017;35(15 Suppl.).Google Scholar
- 59.Zhou Y, Tang F, Min L, et al. A preliminary study of apatinib in Chinese patients with osteosarcoma [abstract no. e22500]. J Clin Oncol. 2017;35(15 Suppl.).Google Scholar
- 60.Qin S. Apatinib in Chinese patients with advanced hepatocellular carcinoma: a phase II randomized, open-label trial [abstract no. 4019]. J Clin Oncol. 2014;32(15 Suppl).Google Scholar
- 62.Jiangsu Hengrui Pharmaceutical Co. Ltd. AiTan (apatinib mesylate tablets): product information sheet. 2014. http://www.xinyao.com.cn/yaopin/s128423.htm. Accessed 23 Jan 2018.
- 63.LSK BioPharma. LSK BioPharma’s apatinib receives orphan drug designation in the European Union [media release]. 2017. http://www.lskbiopharma.com. Accessed 22 Jan 2018.
- 64.LSK BioPharma. The US FDA grants apatinib orphan drug designation for treatment of gastric cancer [media release]. 2017. http://www.lskbiopharma.com. Accessed 23 Jan 2018.
- 65.World Health Organization. Cancer: fact sheet. 2018. http://www.who.int/mediacentre/factsheets/fs297/en/. Accessed 22 Feb 2018.