Drug Detail

Information about Sutent

Generic Name
Sunitinib, + CP-751
SU11248 + CP-751
Brand Name (US)
Pfizer, Pfizer
Drug Type
Tyrosine Kinase Inhibitor, Monoclonal Antibody
Oral + Intravenous
Approval Status
Sutent is approved for GIST. A trial of this combination was apparently halted due to the discontinuation of development of CP-751.
Overall Strategy
GIST cell based
Block KIT + Block related tumor signal paths
Drug Category
KIT/PDGFRA inhibitor + IGF1R inhibitor

This phase 1 trial combines sunitinib (SU11248) with CP-751, 871.
Sunitinib is approved for Gleevec-resistant GIST. It is a potent KIT inhibitor, especially KIT exon 9 mutations and wild-type KIT. It also inhibits secondary mutations in exon 13 and exon 14 (gatekeeper mutation). Sunitinib also inhibits the VEGF receptors.
CP-751, 871 is also made by Pfizer. It inhibits the IGF1R receptor. IGF1R has been shown to be overexpressed in wild-type GIST and in pediatric GIST.
Thus, this combination might be especially suitable for "wild-type" GIST since it combines a potent wild-type KIT inhibitor with a IGF1R inhibitor.