Activity of nilotinib (AMN-107) alone in advanced gastrointestinal stromal tumors progressing on imatinib and sunitinib. Case report.

Nilotinib is a novel tyrosine kinase inhibitor targeting KIT (CD117), PDGFR and BCR-ABL and inhibiting the proliferation of both imatinib-sensitive and imatinib-resistant cells in vitro. Nilotinib, alone or in combination with imatinib, has promising activity in imatinib-resistant patients with advanced gastrointestinal stromal tumors (GISTs), including those who progressed on sunitinib and other tyrosine kinase inhibitors. We describe the beneficial effect of nilotinib 400 mg b.i.d. orally in a 53-year-old patient with metastatic GISTs who had radiologically confirmed disease progression on both imatinib (800 mg/day) and sunitinib (50 mg/day). A positron emission tomography-computerized tomography evaluation showed marked decreases in (18)F-fluorodeoxyglucose uptake in the liver and mesentery region after 3 months of therapy with nilotinib. Nilotinib is an option for patients with advanced GISTs progressing on both imatinib and sunitinib. Copyright 2009 S. Karger AG, Basel.