Drug Detail

Information about Tandutinib

Generic Name	Tandutinib
IND	MLN518
Brand Name (US)
Manufacturer	Millennium
Drug Type	Tyrosine Kinase Inhibitor
Delivery	Oral
Approval Status	Phase2
Indications
Overall Strategy	KIT Protein Based
Strategy	Block KIT
Drug Category	KIT/PDGFRA inhibitor

MLN518 is an oral tyrosine kinase inhibitor. It is manufactured by Millennium. As of August, 2008 it had advanced to phase 2 trials (not in trials for GIST). Tandutinib (MLN518), previously known as CT53518, is a small-molecule inhibitor of the type III receptor tyrosine kinases, including the Fms-like tyrosine kinase 3 receptor (FLT3), platelet-derived growth factor receptor (PDGFR), and c-Kit receptor tyrosine kinase. Tandutinib is relatively selective, having no appreciable activity against EGFR, FGFR, KDR, or several non-receptor kinases. FLT3, c-Kit, and ßPDGFR are equally inhibited by tandutinib, while the agent is much less active against CSF-1R (in vitro IC50 of 3.4 µM).
MLN518 has been shown to inhibit the KIT D816V mutation. A similar mutation in PDGFA, D842V, is resistant to Gleevec and Sutent. Since it is very similar to the D816V mutation, it is possible that it may be inhibited by MLN518.