Clinical Development of Sunitinib Malate

摘要: Sunitinib malate (SUTENT®, SU11248, Pfizer Inc.) is an oral multitargeted receptor tyrosine kinase (RTK) inhibitor with antiangiogenic and antitumor activity. RTKs are transmembrane proteins, the dysregulated activity of which has been linked to growth metastatic spread human cancers. shown efficacy in phase II III trials renal cell carcinoma (RCC) gastrointestinal stromal tumors (GIST). The study imatinib-resistant or -intolerant GIST patients was unblinded early when planned interim analysis revealed a significant time progression advantage for sunitinib compared placebo (27.3 weeks vs 6.4 weeks; P≪0.0001). In recently reported comparison first-line interferon alfa (IFN-α) RCC patients, treatment also resulted significantly longer progression-free survival than IFN-α (11 5 months; P0.001). well tolerated consistent, predictable safety profile. most common treatment-related adverse events clinical program have fatigue, diarrhea, nausea, vomiting, anorexia. Fatigue not commonly associated discontinuation. Gastrointestinal toxicities were generally manageable. Encouraging results from single-agent studies other tumor types such as breast cancer non-small lung led ongoing investigations this agent firstand second-line combination these solid types.