3.4 Lenvatinib Story Case
Lenvatinib (49; E7080; Lenvima™; Eisai; Fig. 15) is the most recent VEGFR TKI
approved by FDA for clinical use in cancer treatment. This drug actually consists an
oral multi-kinase inhibitor that selectively inhibits VEGFR 1–3 and other
pro-angiogenic and prooncogenic receptor tyrosine kinases, including fibroblast
growth factor receptors 1–4 (FGFR1-4), platelet-derived growth factor receptor-α
(PDGFR-α), c-KIT, and RET. Compound 49 is a quinoline-functionalized derivative
belonging to the general formula depicted in Fig. 16, which was first described as a
Fig. 15 Examples of VEGFR TKIs on clinical trials as anticancer drug candidates
Case Study on Receptor Tyrosine Kinases EGFR, VEGFR, and PDGFR
177
Lenvatinib (49; E7080; Lenvima™; Eisai; Fig. 15) is the most recent VEGFR TKI
approved by FDA for clinical use in cancer treatment. This drug actually consists an
oral multi-kinase inhibitor that selectively inhibits VEGFR 1–3 and other
pro-angiogenic and prooncogenic receptor tyrosine kinases, including fibroblast
growth factor receptors 1–4 (FGFR1-4), platelet-derived growth factor receptor-α
(PDGFR-α), c-KIT, and RET. Compound 49 is a quinoline-functionalized derivative
belonging to the general formula depicted in Fig. 16, which was first described as a
Fig. 15 Examples of VEGFR TKIs on clinical trials as anticancer drug candidates
Case Study on Receptor Tyrosine Kinases EGFR, VEGFR, and PDGFR
177