Ovarian carcinoma has the highest mortality rate among gynecologic malignancies, due in part to the primary drug resistance and multidrug resistance that represent major clinical obstacles to treatment.1 Apatinib is a small-molecule tyrosine kinase inhibitor independently developed in China that mainly functions by competitively blocking the binding of VEGF with VEGFR-2 and preventing the autophosphorylation of VEGFR-2. Antitumor effects are thereby elicited by preventing VEGF-mediated endothelial cell proliferation and migration, and reducing tumor angiogenesis. In this prospective, open-label, single-arm clinical trial, Sun and colleagues evaluated the efficacy and safety of apatinib mesylate as treatment after failure of second-line chemotherapy in patients with advanced epithelial ovarian cancer.2
Of 17 evaluable patients who received oral apatinib for 3 treatment cycles (each cycle included 500 mg or 250 mg apatinib once daily for 28 days), 6 (35.3%) and 2 (11.8%) patients achieved partial response and stable disease, respectively. The objective response rate (ORR) and disease control rate (DCR) were 35.3% and 47.1%, respectively. Efficacy signals were not significantly different between groups receiving initial dosages of 500 mg (ORR, 30%; DCR, 30%) and 250 mg (ORR, 42.8%; DCR, 71.4%). The median progression-free survival was 2.2 months (95% confidence interval [CI], 1.0-8.9 months) and the median overall survival was 6.3 months (95% CI, 1.5-12.8 months). The most common adverse events reported were hypertension (70.6%), hand-foot syndrome (52.9%), and oral mucosa damage (35.3%).
The results of this study suggest that oral apatinib treatment is efficacious and well-tolerated in patients with advanced epithelial ovarian cancer who have failed second-line chemotherapy.
- Norouzi-Barough L, et al. J Cell Physiol. 2018;233(6):4546-4562.
- Sun S, et al. ESMO 2018. Abstract 974P.