Abstract:Apatinib's efficacy, tolerability and safety have been evaluated in one Phase II and one Phase III study in metastatic/advanced gastric cancer. In this review, we focus on the mechanism of action of apatinib, its pharmacokinetic profile and its clinical activity in the treatment of advanced/metastatic gastric cancer. Expert commentary: Unfortunately, as yet, there is no definitive biomarker data for apatinib in gastric cancer.
“…For instance, BLU-667 is a potent RET inhibitor designed to target RET directly, which has successfully induced tumor regression without notable toxicity in patients harboring RET alterations, exhibiting enormous therapeutic potential (26). Finally, we chose apatinib for its broad antineoplastic efficacy (27)(28)(29)(30) and fewer side effects compared with sorafenib (30). Apatinib, a multikinase inhibitor, specifically targets VEGFR-2 to partially block the pathways of mitogenic and angiogenic, by which it plays an essential role in tumor oncogenesis and metastasis (31).…”
Anaplastic thyroid cancer is known to be the most lethal malignancy among endocrine tumors for its extremely limited survival rate after diagnosis. As a result of this poor survival prognosis, multimodal therapy is currently under investigation to address this global concern. In this reported case, the 125 I seed implantation and vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor apatinib were co-applied to treat a 49-year-old woman with anaplastic thyroid cancer. After the patient began apatinib administration and underwent 125 I seed implantation twice, the tumor size shrank successfully. After a follow-up of 13 months since the initial diagnosis of anaplastic thyroid cancer, the patient survived with a stable disease pathology. In conclusion, this study supports 125 I seed implantation and apatinib as effective therapeutic alternatives for inoperable anaplastic thyroid cancer patients.
“…For instance, BLU-667 is a potent RET inhibitor designed to target RET directly, which has successfully induced tumor regression without notable toxicity in patients harboring RET alterations, exhibiting enormous therapeutic potential (26). Finally, we chose apatinib for its broad antineoplastic efficacy (27)(28)(29)(30) and fewer side effects compared with sorafenib (30). Apatinib, a multikinase inhibitor, specifically targets VEGFR-2 to partially block the pathways of mitogenic and angiogenic, by which it plays an essential role in tumor oncogenesis and metastasis (31).…”
Anaplastic thyroid cancer is known to be the most lethal malignancy among endocrine tumors for its extremely limited survival rate after diagnosis. As a result of this poor survival prognosis, multimodal therapy is currently under investigation to address this global concern. In this reported case, the 125 I seed implantation and vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor apatinib were co-applied to treat a 49-year-old woman with anaplastic thyroid cancer. After the patient began apatinib administration and underwent 125 I seed implantation twice, the tumor size shrank successfully. After a follow-up of 13 months since the initial diagnosis of anaplastic thyroid cancer, the patient survived with a stable disease pathology. In conclusion, this study supports 125 I seed implantation and apatinib as effective therapeutic alternatives for inoperable anaplastic thyroid cancer patients.
“…When targeting to VEGFR-2, the tyrosine kinase activity of the cells was inhibited, resulting in the inhibition of VEGF/VEGFR-2 signaling pathway and subsequent inhibition of tumor angiogenesis and tumor progression. The process of inhibiting tumor angiogenesis can effectively reduce tumor progression and metastasis [30].…”
Background The 5-year survival rate for extensive-disease small-cell lung carcinoma (ED-SCLC) is only 1%. Recently, apatinib exerted promising effects on cancer patients after failure of first-line chemotherapy. Methods This study enrolled 24 ED-SCLC patients to study the efficacy and toxicity of apatinib in combination with chemotherapy and maintenance therapy. The primary endpoints were overall survival (OS) and progression-free survival (PFS). The secondary endpoints included toxicity and safety. Apatinib was given 250 mg/day during the chemotherapy interval, and as maintenance therapy after 4-6 cycles until the patient progressed, died, or was intolerant to drug toxicity. The study further evaluated the cytotoxicity, cell-cycle arrest and apoptotic induction of apatinib in A549 and H446 cells. Results There was no difference in short-term efficacy between combined and chemotherapy groups. Long-term efficacy showed that the median PFS was 7.8 months and 4.9 months in combination and chemotherapy groups, respectively [p = 0.002, HR(95%CI): 0.18(0.06-0.60)]. The median OS was 12.1 months and 8.2 months in combination and chemotherapy groups, respectively [p = 0.023, HR(95%CI): 0.38 (0.16-0.90)]. Multivariate Cox regression analysis showed that apatinib combined with chemotherapy was an independent prognostic factor for OS and PFS. The ECOG score was an independent prognostic factor affecting OS. In vitro analysis showed that apatinib inhibited cell proliferation and caused cell-cycle arrest and apoptosis. Conclusion Apatinib combination/maintenance therapy showed promising efficacy and safety to extend OS/PFS in ED-SCLC and will be a potent therapeutic option in future practice. Although the scale of this study is small, further research on large sample sizes is needed.
“…Thus, the therapy of targeting VEGF or VEGFR is mainly to focus on anti-angiogenesis. Apatinib, also known as Aitan (brand name in China) and developed independently by Shanghai Hengrui Pharmaceutical Co., Ltd (Shanghai, China) [22], is a typical representative of anti-angiogenesis agents for antineoplastic functions, which could induce apoptosis and suppress tumor proliferation either alone or in combination with chemotherapy across a variety of advanced solid malignancies [23][24][25][26][27][28]. What needs to be emphasized is that, the e cacy of apatinib is comparable to that of sorafenib or lenvatinib, but with more manageable safety pro le and faster therapeutic response [26, [29][30][31].…”
Background: The majority of differentiated thyroid cancer (DTC) has good prognosis after a careful standardized therapy according to the current guidelines. However, approximately 13% to 15% of DTC shows surprisingly aggressive behavior and invades the surrounding structures, and then a few is very difficult to remove. In that specific context, preoperative neoadjuvant targeted therapy may improve the clinical stage and create an opportunity for operation.Case presentation: We reported a case of 64-year-old woman with locally advanced papillary thyroid cancer (PTC) who presented with dysphagia due to seemingly unresectable tumor, which severely invaded the left esophagus at the junction of neck and thorax, difficult to undergo a safe and complete removal. With an approvement of institution ethics committee, this patient was treated with neoadjuvant therapy (apatinib 500mg orally qd).Six weeks later, the tumor dramatically shrunk from 56*37mm to 29*26mm with well-controlled mild hypertension. After 10 days interval of apatinib withdrawal, complete tumor excision was accomplished without esophagus fistula. Postoperative inhibition and radioiodine 131I ablation were performed. At one-year follow-up evaluation, no tumor recurrence or metastasis was observed.Conclusion: Preoperative short-termed targeted treatment for locally advanced inoperable DTC may become a promising neoadjuvant therapy, which can reduce the tumor size and decrease stage, thus being convenient for complete and safe removal.
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