Drug Detail

Information about Gleevec, Tasigna

Generic Name	Imatinib, Nilotinib
IND	Imatinib or Nilotinib
Brand Name (US)	Gleevec, Tasigna
Manufacturer	Novartis + Novartis
Drug Type	Tyrosine Kinase Inhibitor
Delivery	Oral
Approval Status	Both are approved
Indications	GIST (imatinib only), Both are approved for CML and others
Overall Strategy	KIT Protein Based
Strategy	Block KIT
Drug Category	KIT/PDGFRA inhibitor

A phase III trial opened in January, 2009 to test whether nilotinib is better than imatinib when given as initial (front-line) therapy in metastatic/unresectable GIST. This trial failed to demonstrate superiority for nilotinib.
Dr. Cristina Antonescu and her colleagues at Memorial Sloan-Kettering Cancer Center have shown that nilotinib is a very potent inhibitor of wild-type KIT. It is also a strong inhibitor of the most common secondary mutation in GIST, the V654A mutation in exon 13 of KIT. Nilotinib does not depend on the OCT1 protein for uptake into tumor cells (Gleevec is dependent on OCT1) and in test tube experiments reaches higher concentrations inside tumor cells than Gleevec.