Generic Name  | 
        Sunitinib, + CP-751 | |
|---|---|---|
IND  | 
               SU11248 + CP-751 | |
Brand Name (US)  | 
        Sutent | |
Manufacturer  | 
        Pfizer, Pfizer | |
Drug Type  | 
        Tyrosine Kinase Inhibitor, Monoclonal Antibody | |
Delivery  | 
        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. | |
Indications  | 
        ||
Overall Strategy  | 
        GIST cell based | |
Strategy  | 
        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.