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Surufatinib for the treatment of advanced extrapancreatic neuroendocrine tumors
Xiuhua Lu1, Shibin Yan2, Kelly Ann Koral3
1Department of Clinical Pharmacy, Linyi Central Hospital, Linyi, Shandong, China.
Abstract:
Introduction: Surufatinib (also known as HMPL-012, sulfatinib) is a novel oral tyrosine kinase inhibitor (TKI), which has the dual activity of anti-angiogenesis and immune regulation. In December 2020, surufatinib was approved as a monotherapy for unresectable locally advanced or metastatic, progressive nonfunctioning, well differentiated (grade 1 or 2) extrapancreatic neuroendocrine tumors (epNETs) in China.Areas covered: In this paper, the chemical properties, mechanism of action, pharmacokinetics, clinical efficacy, safety, and tolerability of surufatinib for treatment of advanced extrapancreatic NETs are introduced in detail. We performed a systematic review of the literature in PubMed and the following keywords were used: 'surufatinib,' 'sulfatinib' and 'HMPL-012.'Expert opinion: Surufatinib is a potent, selective, and small-molecule TKI that targets vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor 1 (FGFR1) and colony stimulating factor 1 receptor (CSF1R). Surufatinib showed an acceptable safety profile and encouraging antitumor activity in patients with advanced epNETs. The most frequently observed adverse events (AEs) were hypertension and proteinuria. Surufatinib provides a new treatment option for patients with advanced epNETs. More clinical trials of surufatinib are ongoing to develop a combination of therapy strategies and new indications for malignancies.
Insights
Surufatinib, a novel tyrosine kinase inhibitor (TKI), is approved for advanced extrapancreatic neuroendocrine tumors (epNETs). It demonstrates antitumor activity and an acceptable safety profile, offering a new treatment option.
Area of Science:
- Oncology
- Pharmacology
- Drug Development
Background:
- Surufatinib (HMPL-012, sulfatinib) is an oral tyrosine kinase inhibitor (TKI).
- It possesses dual anti-angiogenic and immune regulatory activities.
- Approved in China for advanced epNETs, it targets VEGFR, FGFR1, and CSF1R.
Purpose of the Study:
- To detail the chemical properties, mechanism of action, pharmacokinetics, clinical efficacy, safety, and tolerability of surufatinib.
- To review the literature on surufatinib for advanced extrapancreatic neuroendocrine tumors (epNETs).
Main Methods:
- Systematic literature review using PubMed.
- Keywords: 'surufatinib,' 'sulfatinib,' 'HMPL-012.'
Main Results:
- Surufatinib exhibits potent, selective TKI activity.
- It showed encouraging antitumor activity and an acceptable safety profile in advanced epNET patients.
- Common adverse events include hypertension and proteinuria.
Conclusions:
- Surufatinib represents a new therapeutic option for advanced epNETs.
- Ongoing trials explore combination therapies and new indications for surufatinib.
- The drug offers a favorable safety profile for patients with advanced epNETs.
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