| Drug Name |
Lenvatinib |
| Drug ID |
BADD_D01254 |
| 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. |
| Indications and Usage |
Lenvatinib is indicated for the treatment of following conditions.
- Treatment of locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.
- Treatment of advanced renal cell carcinoma (RCC) in combination with everolimus following one prior antiangiogenic therapy.
- First-line treatment of unresectable hepatocellular carcinoma (HCC). |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EX08 |
| DrugBank ID |
DB09078
|
| KEGG ID |
D09919
|
| MeSH ID |
C531958
|
| PubChem ID |
9823820
|
| TTD Drug ID |
D0R0FO
|
| NDC Product Code |
62856-704; 62856-710; 62856-712; 63285-758; 54893-0080; 62856-708; 62856-718; 11071-912; 11071-913; 63285-757; 62856-714; 62856-724; 62856-720 |
| UNII |
EE083865G2
|
| Synonyms |
lenvatinib | 4-(3-chloro-4-((cyclopropylaminocarbonyl)amino)phenoxy)-7-methoxy-6-quinolinecarboxamide | 4-(3-chloro-4-(N'-cyclopropylureido)phenoxy)-7-methoxyquinoline-6-carboxamide | lenvatinib mesylate | E7080 mesylate | N-(4-((6-carbamoyl-7-methoxyquinolin-4-yl)oxy)-2-chlorophenyl)-N'-cyclopropylurea monomethanesulfonate | lenvatinib mesilate | lenvatinib methanesulfonate | Lenvima | E-7080 mesylate | E 7080 | E-7080 | ER-203492-00 | E7080 | lenvatinib metabolite M2 | 4-(3-chloro-4-(((cyclopropylamino)carbonyl)amino)phenoxy)-7-hydroxy-6-quinolinecarboxamide |
