Lucitanib [6-[7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl]oxy-N-methylnaphthalene-1-carboxamide] is an oral, potent inhibitor of the tyrosine kinase activity of fibroblast growth factor receptors 1 through 3 (FGFR-1,2,3), vascular endothelial growth factor receptors 1 through 3 (VEGFR-1,2,3) and platelet-derived growth factor receptors alpha and beta (PDGFR- a,ß). As an inhibitor of FGFR-1,2,3, VEGFR-1,2,3 and PDGFR a/ß, and the role that each of these receptor kinases plays in tumor progression and metastasis formation, Lucitanib has the potential benefit of targeting three relevant pro-angiogenic growth factors in targeted patient populations identified by molecular markers.
Clovis Oncology holds exclusive development and commercial rights to lucitanib on a global basis, excluding China. Lucitanib rights to markets outside of the U.S. and Japan have been sublicensed to Les Laboratoires Servier (Servier).
Common Name: Lucitanib
Synonyms: CO-3810; S 80881; E-3810
IUPAC Name: 6-({7-[(1-aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl}oxy)-N- methylnaphthalene-1-carboxamide
CAS Number: 1058137-23-7Mechanism of Action: Kinase Inhibitor; FGFR Inhibitor; VEGFR Inhibitor; PDGFR Inhibitor
Indication: Various cancers, tumors
Development Stage: Phase I/II
Company: Clovis Oncology
A Phase I/IIa clinical trial of Lucitanib was initiated in 2010 and has demonstrated multiple objective responses in FGFR1 gene-amplified breast cancer patients, and objective responses were also observed in patients with tumors often sensitive to VEGFR inhibitors, such as renal cell and thyroid cancer. FGFR amplification is common in a number of tumor types, including breast cancer and lung cancer, and it is intended to study Lucitanib in these cancers as well as other solid tumors exhibiting FGFR pathway activation. A broad Phase II development program has been initiated by Clovis and Servier in multiple indications, including advanced breast and lung cancers.
