Apatinib blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization. Apatinib has showed antitumor effects on many kinds of tumors, such as sarcoma, breast cancer, ovarian cancer, and acute lymphoblastic leukemia (ALL). Moreover, a recent case report provided supporting information for apatinib to treat epithelioid malignant plural mesothelioma.[1]
In vitro experiment indicated that apatinib inhibited cells proliferation in a dose-dependent and time-dependent manner. The IC50 values of apatinib in MPM cells for treatment time 24 h, 48 h, 72 h were 46.34 μM, 45.14 μM, 28.73 μM.[3]
In vivo experiments demonstrated that apatinib inhibits tumor growth and metastasis. The ePCI score of blank control, solvent control and apatinib groups were 9.8 ± 0.9, 10.3 ± 0.9, and 7.3 ± 1.6, respectively. The differences were statistically significant (P = 0.003 for all; P = 0.008, blank control vs. apatinib group; P = 0.001, solvent control vs. apatinib group; P = 0.394, blank control vs. solvent control). The positive rate of Ki-67 in apatinib group was (17.0 ± 8.0)%, which is significantly lower than that in control group (48.1 ±11.5) % (P = 0.000); the positive rate of VEGFR-2 in apatinib group was slightly lower than that in control group, indicating no statistical significance.[1]
References:
[1]. Yang ZR, et al. Apatinib Mesylate Inhibits the Proliferation and Metastasis of Epithelioid Malignant Peritoneal Mesothelioma In Vitro and In Vivo. Front Oncol. 2020 Dec 7;10:585079.
阿帕替尼阻断 VEGF 通路的下游信号转导，从而抑制新生血管形成。阿帕替尼对肉瘤、乳腺癌、卵巢癌、急性淋巴细胞白血病（ALL）等多种肿瘤均显示出抗肿瘤作用。此外，最近的病例报告为阿帕替尼治疗上皮样恶性多发性间皮瘤提供了支持信息。[1]
体外实验表明，阿帕替尼以剂量依赖性和时间依赖性方式抑制细胞增殖。阿帕替尼作用于MPM细胞24 h、48 h、72 h的IC50值分别为46.34 μM、45.14 μM、28.73 μM。[3]
体内实验表明，阿帕替尼可抑制肿瘤生长和转移。空白对照、溶剂对照和阿帕替尼组的ePCI评分分别为9.8±0.9、10.3±0.9和7.3±1.6。差异具有统计学意义（所有 P = 0.003；P = 0.008，空白对照与阿帕替尼组；P = 0.001，溶剂对照与阿帕替尼组；P = 0.394，空白对照与溶剂对照）。阿帕替尼组Ki-67阳性率为（17.0±8.0）%，显着低于对照组的（48.1±11.5）%（P=0.000）；阿帕替尼组VEGFR-2阳性率略低于对照组，无统计学意义。[1]