Sunitinib.
Sunitinib is a small-molecule inhibitor of several receptor tyrosine kinases relevant to tumor angiogenesis, including the vascular endothelial growth factor (VEGF) receptor. Potent inhibition of this related family of receptors and consequent antiangiogenic effects have been demonstrated in vitro and in murine models. Human studies have established 50 mg daily dosing given on an intermittent schedule as a tolerable dose. Significant antitumor effects have been observed, most notably in advanced renal cell carcinoma (RCC) and imatinib refractory/intolerant gastrointestinal stromal tumor (GIST). Sunitinib has received regulatory approval in these two indications, and is at present being investigated across a broad array of solid tumors. Despite these initial results, several questions remain to optimize the utility of this agent.
Rini
Brian I
BI
Cleveland Clinic Taussig Cancer Center, Department of Solid Tumor Oncology and Urology, 9500 Euclid Avenue/Desk R35, Cleveland, Ohio 44195, USA. rinib2@ccf.org
D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000378:metabolism; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D000077210:Sunitinib
D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D007211:Indoles; D011758:Pyrroles; D000077210:Sunitinib