Description | 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. |
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Indication | Lenvatinib is indicated for the treatment of the following cancerous conditions:[L41120] **Differentiated Thyroid Cancer (DTC)** - Treatment of locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer **Renal Cell Carcinoma (RCC)** - First-line treatment, in combination with [pembrolizumab], in adult patients with advanced renal cell carcinoma (RCC) - Treatment of advanced renal cell carcinoma, in combination with [everolimus], in adult patients who have previously tried ≥1 anti-angiogenic therapy **Hepatocellular Carcinoma (HCC)** - First-line treatment of patients with unresectable hepatocellular carcinoma **Endometrial Carcinoma** - Treatment of advanced endometrial carcinoma that is not microsatellite instability-high (MSI-H) or mismatch repair deficient (dMMR), in combination with [pembrolizumab], in patients who have experienced disease progression following prior systemic therapy and are not candidates for curative surgery or radiation |
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