Sunitinib Malate

Abstract

Sunitinib malate (Sutent ® , Pfizer Inc.) is a multitargeted tyrosine kinase inhibitor that inhibits tumor cell proliferation and angiogenesis. It is approved for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Sunitinib malate salt is a photosensitive yellowish powder soluble in DMSO, whereas very poorly soluble in ethanol and water. Several methods of sunitinib synthesis are included in this review. UV spectroscopy of sunitinib showed a λmax of approximately 430 nm, whereas IR spectroscopy of sunitinib base were reported at 3298, 3230, 2968, 1676, 1627, 1590, 1544, 1498, 1334 cm -1 . In addition, chromatographic, spectrofluorimetric, and immunoassay methods for the analysis of sunitinib are also described. Pharmacokinetically, following a single oral dose in healthy and cancer subjects, peak plasma sunitinib concentrations occur between 6 and 12h post dose, with prolonged half-lives of approximately 40 h. Sunitinib is primarily metabolized by CYP3A4 to produce its primary active metabolite, SU12662, which is further metabolized by CYP3A4 into inactive metabolites. Sunitinib is primarily eliminated with the feces (61%), with renal elimination accounting for only 16% of the administered dose. © 2012 Elsevier Inc.