Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study

Xu, Jian; Wang, Yan; Chen, Yu Ling; Jia, Ru; Li, Jie; Gong, Ji fang; Li, Jing; Qi, Chao; Hua, Yi-Jun; Cui, Tan; Wang, Jian; Li, Ké; Sai, Yang; Zhou, Feng; Ren, Yulin; Qing, Wei Guo; Jia, Hong; Wei, Su; Shen, Lin

doi:10.18632/oncotarget.14942

Cited by 44 publications

(37 citation statements)

References 19 publications

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“…Sulfatinib is a multi-target TKI targeting VEGFR-1/2/3, FGFR1, and colony stimulating factor 1 receptor (CSF1R). A phase I study (NCT02133157) observed an acceptable safety profile and encouraging antitumor activity in patients with advanced solid tumors, particularly in NETs [ 95 ]. At present, one phase II study (NCT02267967) and two phase III studies (NCT02589821, NCT02588170) conducted on advanced NETs are ongoing [ 96 ].…”

Section: Novel Anti-angiogenic Tkis Under Investigationmentioning

confidence: 99%

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

et al. 2019

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Angiogenesis has always been the topic of major scientific interest in the field of malignant tumors. Nowadays, targeting angiogenesis has achieved success in various carcinomas by several mechanisms, including the use of anti-angiogenic small molecule receptor tyrosine kinase inhibitors (TKIs). The development of TKIs targeting proangiogenic receptors, mainly vascular endothelial growth factor receptor (VEGFR) family, have significantly improved the outcome of certain types of cancers, like renal cell carcinoma, hepatocellular carcinoma, and colorectal carcinoma. However, the general response rate is not very satisfactory. The particular toxicity profile and resistance to anti-angiogenic targeted agents are unavoidable, and no specific marker is available to screen responsive patients to TKIs for precision therapy. To date, about 11 anti-angiogenic TKIs with different binding capacities to angiogenic receptor tyrosine kinase have been approved for the treatment of patients with advanced cancers. This review presents all approved antiangiogenic small molecule receptor TKIs so far with an emphasis on their indications and clinical efficacy. We also discuss the combination between TKIs and immune checkpoint blockade inhibitors based on the most recent exciting outcome in immunotherapy.

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Section: Novel Anti-angiogenic Tkis Under Investigationmentioning

confidence: 99%

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

et al. 2019

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“…Sulfatinib (HMPL012) is a potent small molecule TKI of VEGFR 1, 2, and 3, FGFR 1, and Colony Stimulating Factor 1 Receptor- CSF1R. Xu et al [ 83 ] investigated the sulfatinib safety, pharmacokinetics, and preliminary antitumor activity in advanced solid tumors. As for other anti-angiogenic drug the most frequent side effects during therapy were proteinuria, hypertension and diarrhea.…”

Section: Vegfr and Hypertensionmentioning

confidence: 99%

Hypertension in malignancy-an underappreciated problem

Małyszko

Kozłowski³

et al. 2018

Oncotarget

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Hypertension is one of the most common comorbidities in cancer patients with malignancy, in particular, in the elderly. On the other hand, hypertension is a long-term consequence of antineoplastic treatment, including both chemotherapy and targeted agents. Several chemotherapeutics and targeted drugs may be responsible for development or worsening of the hypertension. The most common side effect of anti-VEGF (vascular endothelial growth factor) treatment is hypertension. However, pathogenesis of hypertension in patients receiving this therapy appears to be associated with multiple pathways and is not yet fully understood. Development of hypertension was associated with improved antitumor efficacy in patients treated with anti-antiangiogenic drugs in some but not in all studies. Drugs used commonly as adjuvants such as steroids, erythropoietin stimulating agents etc, may also cause rise in blood pressure or exacerbate preexisiting hypertension. Hypotensive therapy is crucial to manage hypertension during certain antineoplastic treatment. The choice and dose of antihypertensive drugs depend upon the presence of organ dysfunction, comorbidities, and/or adverse effects. In addition, severity of the hypertension and the urgency of blood pressure control should also be taken into consideration. As there are no specific guidelines on the hypertension treatment in cancer patients we should follow the available guidelines to obtain the best possible outcomes and pay the attention to the individualization of the therapy according to the actual situation.

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“…Surufatinib is a potent TKI targeting VEGF receptors (VEGFR) 1, 2, and 3, FGFR1, and CSF-1R. In preliminary phase I and Ib/II studies surufatinib showed encouraging anti-tumor activity in advanced NENs ( 81 , 82 ).…”

Section: Fgfrs As Therapeutic Target In Nensmentioning

confidence: 99%

Role of FGF System in Neuroendocrine Neoplasms: Potential Therapeutic Applications

et al. 2021

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Neuroendocrine neoplasms (NENs) are a heterogeneous group of tumors originating from neuroendocrine cells dispersed in different organs. Receptor tyrosine kinases are a subclass of tyrosine kinases with a relevant role in several cellular processes including proliferation, differentiation, motility and metabolism. Dysregulation of these receptors is involved in neoplastic development and progression for several tumors, including NENs. In this review, we provide an overview concerning the role of the fibroblast growth factor (FGF)/fibroblast growth factor receptor (FGFR) system in the development and progression of NENs, the occurrence of fibrotic complications and the onset of drug-resistance. Although no specific FGFR kinase inhibitors have been evaluated in NENs, several clinical trials on multitarget tyrosine kinase inhibitors, acting also on FGF system, showed promising anti-tumor activity with an acceptable and manageable safety profile in patients with advanced NENs. Future studies will need to confirm these issues, particularly with the development of new tyrosine kinase inhibitors highly selective for FGFR.

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Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study

Cited by 44 publications

References 19 publications

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

Hypertension in malignancy-an underappreciated problem

Role of FGF System in Neuroendocrine Neoplasms: Potential Therapeutic Applications

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