阿帕替尼在恶性肿瘤治疗中的临床应用与研究进展

Clinical application and research progress of apatinib in cancer treatment

抗血管生成靶向治疗是近年来肿瘤治疗的研究热点。其中,血管新生抑制剂阿帕替尼是我国自主研制的1.1类新药。临床前研究和临床试验研究表明,阿帕替尼对胃癌、肺癌、乳腺癌等多种肿瘤均具有显著的抑制活性,其安全性和有效性良好。然而,阿帕替尼的相关研究显示,目前仍存在作用机制不十分明确等问题。因此,开展进一步研究以不断提高药物的安全性、有效性和经济性,是阿帕替尼广泛应用于临床的前提。总结阿帕替尼在国内外研究现状,从作用机制、药动学过程、临床疗效、安全性和生物标志物等角度进行归纳,探讨了近年来阿帕替尼研究的热点与争议问题,实现对阿帕替尼的临床应用前景展望。

Antiangiogenic target therapy has been a hot topic in cancer treatment recently.Apatinib is a category 1.1 new medication developed domestically.It effectively inhibits angiogenic and exhibits promising anti-tumor activity in preclinical studies.Apatinib has been successfully applied in clinical trials of multiple malignancies,such as gastric cancer,lung cancer and breast cancer with satisfactory safety and efficacy profile.However,its mechanism of action is still not fully understood.Further researches should be carried on to improve its safety,effectiveness and marketability.This review summarized the mechanism of action,pharmacokinetics,clinical efficacy,safety and biomarkers,discussed the recent progress,hot issues and clinical prospects of apatinib,