PDF(Pubmed)
Abstract：
Digestive system malignancies are one of the primary causes of cancer-related death. Meanwhile, angiogenesis has been proved to play an important role in the process of cancer neovascularization. Apatinib, a novel targeted antiangiogenic molecule, could generate highly selective competition in the vascular endothelial growth factor receptor-2, involved in tumor progression and metastasis. It has been implied as a promising cancer treatment agent that can prevent tumor cell proliferation meanwhile inhibit tumor angiogenesis. Furthermore, completed clinical trials demonstrated that apatinib could prolong the progression-free survival and overall survival in advanced gastric cancer and primary liver cancer. Recent studies revealed that apatinib had a synergistic effect with immunotherapy as a second-line and third-line treatment regimen for some other cancers. In this review, we summarize the pharmacological properties of apatinib and the latest clinical application in chemotherapy-refractory patients with advanced digestive system cancer. Based on the comparable survival results, the molecular mechanisms of apatinib are prospective to include the antiangiogenic, apoptosis-inducing, and autophagy-inducing properties in the corresponding signaling pathway. Treatment of apatinib monotherapy or combination immunotherapy remains the optimal option for patients with digestive system malignancies in the future.
摘要：
消化系统恶性肿瘤是癌症相关死亡的主要原因之一。同时,血管生成已被证明在癌症新生血管形成过程中起着重要作用。阿帕替尼,一种新的靶向抗血管生成分子，可以在血管内皮生长因子受体2中产生高度选择性的竞争，参与肿瘤的进展和转移。它被认为是一种有前途的癌症治疗剂，可以防止肿瘤细胞增殖，同时抑制肿瘤血管生成。此外，已完成的临床试验表明,阿帕替尼可以延长晚期胃癌和原发性肝癌的无进展生存期和总生存期.最近的研究表明，阿帕替尼与免疫疗法作为其他一些癌症的二线和三线治疗方案具有协同作用。在这次审查中,我们总结了阿帕替尼的药理特性以及在晚期消化系统癌症化疗难治性患者中的最新临床应用。根据可比较的生存结果，阿帕替尼的分子机制包括抗血管生成，凋亡诱导，以及相应信号通路中的自噬诱导特性。阿帕替尼单药或联合免疫治疗仍是未来消化系统恶性肿瘤患者的最佳选择。
