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TKI258 (formerly CHR-258)
TKI258 is a multi-target tyrosine kinase inhibitor under development by Novartis (acquired from Chiron). Targets of this drug include:
- VEGF receptors 1, 2, and 3
- PDGF receptor beta
- fibroblast growth factor receptors 1, 2, and 3
- fetal liver TK receptor 3
- KIT
- Ret
- TrkA
- CSF-1
A Phase I clinical trial using TKI258 in 35 patients with solid tumors has been published:
Sarker D, Molife R, Evans TR, Hardie M, Marriott C, Butzberger-Zimmerli P, Morrison R, Fox JA, Heise C, Louie S, Aziz N, Garzon F, Michelson G, Judson IR, Jadayel D, Braendle E, de Bono JS.
A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors.
Clin Cancer Res. 2008 Apr 1;14(7):2075-81. PMID: 18381947
One GIST patient in this study (who had previously experienced progression on imatinib and on sorafenib) showed stable disease for 8 months at a dose of 75 mg/day on an intermittent schedule.
