Sutent is used for Gleevec-resistant GIST and intolerance to Gleevec
Sutent is a potent inhibitor of KIT, PDGFRA and other signaling proteins. It is used as second-line therapy for advanced GIST and for patients that are unable to tolerate Gleevec.
Sutent is known by several different names:
- Sutent, the brand name
- Sunitinib malate or sunitinib, the generic name
- SU11248 (sometimes written as SU011248) in clinical trials
Sutent is a pill that is taken once daily. The usual dosage is 50 mg per day. It is given daily for four weeks, before a two week rest period. This cycle is then repeated as long as the patient continues to show benefit. It is sometimes given continuously at a dose of 37.5 mg.
Sutent is a tyrosine kinase inhibitor that is similar to Gleevec in some ways. Both drugs inhibit the KIT protein and the PDGFRα protein. Inhibition of these proteins provides a direct anti-tumor effect when the target protein (KIT or PDGFRα) is mutated. In addition, some tumors that don’t have KIT or PDGFRα mutations (called “wild-type” GISTs) might still benefit from KIT inhibition.
Sutent is particularly effective for GIST tumors with KIT exon 9 mutations and, to a lesser degree, wild-type GIST, although it is not used as first-line therapy, even for these types.