6-Quinolinecarboxamide, 4-[3-chloro-4-[[(cyclopropyl-2,2,3,3-d4-amino)carbonyl]amino]phenoxy]-7-methoxy-

Description

Lenvatinib-d₄ is intended for use as an internal standard for the quantification of lenvatinib by GC- or LC-MS. Lenvatinib is an inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and VEGFR3 (IC₅₀s = 4.0 and 5.2 nM, respectively).^1,2 It is slightly less potent against the related kinases VEGFR1, FGFR1, PDGFRα, PDGFRβ, and Kit (IC₅₀s = 22, 46, 51, 39, and 100 nM, respectively).¹ Lenvatinib (30 mg/kg, twice per day) reduces tumor growth in an H146 small cell lung cancer mouse xenograft model and induces tumor regression when administered at a dose of 100 mg/kg twice per day. Formulations containing lenvatinib have been used in the treatment of differentiated thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.

References

1. Matsui, J., Yamamaoto, Y., Funahashi, Y., et al. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition Int. J. Cancer 122(3),664-671(2008).
2. Matsui, J., Funahashi, Y., Uenaka, T., et al. Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R) 2 and VEGF-R3 kinase Clin. Cancer Res. 14(17),5459-5465(2008).