Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET. These receptor tyrosine kinases (RTKs) located in the cell membrane play a central role in the activation of signal transduction pathways involved in the normal regulation of cellular processes, such as cell proliferation, migration, apoptosis and differentiation, and in pathogenic angiogenesis, lymphogenesis, tumour growth and cancer progression. In particular, VEGF has been identified as a crucial regulator of both physiologic and pathologic angiogenesis and increased expression of VEGF is associated with a poor prognosis in many types of cancers.
Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer. Most patients with thyroid cancer have a very good prognosis with treatment (98% 5 year survival rate) involving surgery and hormone therapy. However, for patients with RAI-refractory thyroid cancer, treatment options are limited and the prognosis is poor, leading to a push for the development of more targeted therapies such as lenvatinib.
Lenvatinib is indicated for the treatment of the following cancerous conditions:
Differentiated Thyroid Cancer (DTC)
Renal Cell Carcinoma (RCC)
Hepatocellular Carcinoma (HCC)
Endometrial Carcinoma
Beijing Tsinghua Changgung Hospital, Beijing, Beijing, China
Tianjin Medical University Cancer Institute and Hospital, Tianjin, China
Department of Minimally Invasive and Interventional Radiology, Liver Cancer Study and Service Group, Sun Yat-sen University Cancer Center,, Guangzhou, Guangdong, China
Tianjin Medical University Cancer Institute & Hospital, Tianjin, Tianjin, China
the First Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, Zhejiang, China
Icahn School of Medicine at Mount Sinai, New York, New York, United States
Freeman Hospital, Newcastle Upon Tyne, United Kingdom
Queen Elizabeth Hospital, Birmingham, United Kingdom
Addenbrooke's Hospital, Cambridge, United Kingdom
Houston Methodist Research Institute, Houston, Texas, United States
Mayo Clinic in Arizona, Scottsdale, Arizona, United States
Rapid City Regional Hospital, Rapid City, South Dakota, United States
University of Chicago Comprehensive Cancer Center, Chicago, Illinois, United States
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