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
Emory University Winship Cancer Institute ( Site 0639), Atlanta, Georgia, United States
Beth Israel Deaconess Medical Center ( Site 0716), Boston, Massachusetts, United States
Massachusetts General Hospital ( Site 0603), Boston, Massachusetts, United States
Eisai trial site 1, Osaka, Japan
Eisai trial site 2, Tokyo, Japan
H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, United States
NationalCCHE, Kashiwa, Tokyo, Japan
Deenanath Mangeshkar Hospital, Pune, Maharashtra, India
BL Kapoor Hospital, New Delhi, New Delhi, India
Indrayani Hospital, Alandi, Pune, India
Princess Margaret Cancer Centre ( Site 0033), Toronto, Ontario, Canada
Seattle Cancer Care Alliance ( Site 0010), Seattle, Washington, United States
University of California at San Francisco ( Site 0004), San Francisco, California, United States
Hospital Sirio Libanes, Sao Paulo, São Paulo, Brazil
National Taiwan University Hospital, Taipei, Taiwan
Taipei Veterans General Hospital, Taipei, Taiwan
Dolnoslaskie Centrum Onkologii. ( Site 0993), Wroclaw, Dolnoslaskie, Poland
Jewish General Hospital ( Site 0307), Montreal, Quebec, Canada
University of California Davis Comprehensive Cancer Center ( Site 0137), Sacramento, California, United States
North Shore University Health System, Evanston, Illinois, United States
Greater Baltimore Medical Center, Baltimore, Maryland, United States
University of Texas Southwestern Medical Center at Dallas, Dallas, Texas, United States
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