Surufatinib

A kinase inhibitor used in cancer treatment

Surufatinib is an oral small molecule inhibitor that targets multiple receptor tyrosine kinases involved in tumor angiogenesis and immune evasion. It is primarily used in the treatment of neuroendocrine tumors (NETs).

Mechanism of Action

Surufatinib functions by inhibiting the activity of several key receptors, including the vascular endothelial growth factor receptors (VEGFR), fibroblast growth factor receptors (FGFR), and colony stimulating factor-1 receptor (CSF-1R). By blocking these pathways, surufatinib reduces tumor blood supply and modulates the tumor microenvironment, enhancing the immune response against cancer cells.

Clinical Use

Surufatinib is indicated for the treatment of advanced neuroendocrine tumors. It has shown efficacy in both pancreatic and non-pancreatic NETs. The drug is administered orally, allowing for convenient outpatient treatment.

Development and Approval

Surufatinib was developed by Hutchison China MediTech (Chi-Med) and has undergone several clinical trials to establish its safety and efficacy. It received approval in China for the treatment of non-pancreatic neuroendocrine tumors in December 2020 and for pancreatic neuroendocrine tumors in June 2021.

Pharmacokinetics

Surufatinib is well absorbed after oral administration, with a bioavailability that allows for effective plasma concentrations. It is metabolized primarily in the liver and excreted through both feces and urine. The pharmacokinetic profile supports once-daily dosing.

Side Effects

Common side effects of surufatinib include hypertension, proteinuria, and fatigue. These are consistent with its mechanism of action as a VEGFR inhibitor. Monitoring of blood pressure and renal function is recommended during treatment.

Research and Future Directions

Ongoing research is exploring the use of surufatinib in combination with other therapies, such as immune checkpoint inhibitors, to enhance its antitumor effects. Studies are also investigating its potential in other types of cancer beyond neuroendocrine tumors.

Chemical structure of Surufatinib

Related Pages

• Neuroendocrine tumor
• Tyrosine kinase inhibitor
• Vascular endothelial growth factor