학술논문

Dovitinib (CHIR258, TKI258): structure, development and preclinical and clinical activity
Document Type
Report
Source
Future Oncology. January 2015, Vol. 11 Issue 1, p39, 12 p.
Subject
Cancer treatment -- Innovations
Molecular targeted therapy -- Innovations
Antineoplastic agents -- Patient outcomes
Health
Innovations
Patient outcomes
Language
English
ISSN
1479-6694
Abstract
ABSTRACT Dovitinib is an oral multikinase inhibitor targeting FGF receptors, PDGF receptors and VEGF receptors. Its activity against FGF receptors suggests its usefulness in treating cancers after the failure of VEGF/VEGF receptor-targeting agents. The identified dose and schedule to be used in further studies was 500 mg orally for 5 days on and 2 days off. Biological considerations and the results achieved in a Phase I/II trial suggested its activity in advanced renal cell carcinoma patients pretreated with a tyrosine kinase inhibitor and an mTOR inhibitor. Surprisingly, in a randomized controlled Phase III trial versus sorafenib in the same setting, dovitinib failed to demonstrate any superiority. At present, dovitinib is being tested in different tumor types. However, molecular-based patient selection seems to be key to fully exploit the activity of this drug.
Author(s): Camillo Porta [sup.[*]] [sup.aff1] [sup.aff2] , Palma Giglione [sup.aff1] , Wanda Liguigli [sup.aff3] , Chiara Paglino [sup.aff1] [sup.aff2] KEYWORDS dovitinib; drug development; FGFR inhibitor; renal cell carcinoma; VEGFR inhibitor [...]