Abstract
BackgroundApatinib is a tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 2(VEGFR-2). This study was conducted to assess the efficacy and safety of apatinib in patients with non-triple-negative metastatic breast cancer who had received prior chemotherapy for their metastatic disease.MethodsThis multicenter, open-label, single arm study enrolled patients with non-triple-negative breast cancer, pretreated with anthracycline, taxanes and capecitabine, and who failed in the metastatic setting at least 1 and at most 4 prior chemotherapy regimens and at least one endocrine drug for hormone receptor-positive patients as well as at least one anti-Her2 drug for Her2-positive patients. The primary end point of this study was progression free survival (PFS). Secondary end points included objective response rate (ORR), disease control rate (DCR), overall survival (OS), and toxicity. Apatinib was administered as 500 mg daily on days 1 through 28 of each 4-week cycle.Results38 patients were enrolled with a median age of 49 years (range, 35 to 62 years) and received apatinib for a median of 4 cycles (range from 0 to 10 cycles). 18 (47.4%) patients experienced dose reduction during treatment. The median relative dose intensity (relative to assigned dose for each cycle) was 82% (range, 45.0% to 100.0%). Median follow-up time was 10.1 months. Median PFS of all 38 patients was 4.0 months (95% confidence interval (CI), 2.8 m – 5.2 m). 36 patients were eligible for efficacy analysis. ORR was 16.7% (6/36). DCR was 66.7% (24/36). Median OS was 10.3 months (95% CI, 9.1 m – 11.6 m). The most common grade 3/4 treatment-related AEs were hypertension (20.5%), hand-foot syndrome (10.3%), and proteinuria (5.1%). Of three possibly drug-related SAEs recorded in the study, 2 (3.4%) deaths occurred within 28 days of last treatment and were both considered to be the result of disease progression. The other one was grade 2 diarrhea needing hospitalization.ConclusionsApatinib exhibited objective efficacy in heavily pretreated, metastatic non-triple-negative breast cancer with manageable toxicity, and it might be better to be tested in breast cancer with high angiogenesis dependency.Trial registrationClinicalTrials.gov: NCT01653561.
Highlights
Apatinib is a tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 2(VEGFR-2)
Median progression free survival (PFS) of all 38 patients was 4.0 months (95% confidence interval (CI), 2.8 m – 5.2 m) (Figure 2). 36 patients were eligible for efficacy analysis. 1 patient got a confirmed complete response and 5 got partial response according to Response Evaluation Criteria in Solid Tumors (RECIST) 1.0 criteria
Of the three possibly drugrelated SAEs recorded in the study, 2 (3.4%) deaths occurred within 28 days of last treatment and the other one was grade 2 diarrhea needing hospitalization
Summary
Apatinib is a tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 2(VEGFR-2). For patients with metastatic non-triple-negative breast cancer, endocrine therapy or HER2-targeted therapy plays an important role in the treatment besides chemotherapy, most patients will eventually develop drug resistance. Novel drugs for such patients with MBC are needed. VEGFR inhibitors, including sorafenib and sunitinib, have been investigated in the treatment of MBC They are both orally administered small-molecular inhibitors of multiple tyrosine kinases (TKI), involved in tumor progression and angiogenesis including VEGFR-1 (Flt1), VEGFR-2 (KDR), and VEGFR-3 (Flt4), platelet-derived growth factor receptors (PDGFRs), and c-KIT [13,14]. Sunitinib has some antitumor activity, but relatively high toxicity and no additional benefit when combined with chemotherapy [17]
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