All About Sutent

The United States Food and Drug Administration (FDA) announced Jan. 26 2006, that it has approved Sutent (sunitinib) for patients with GISTs that had stopped responding to Gleevec or that were unable to tolerate Gleevec. It is also approved for advanced kidney cancer and for pancreatic neuroendocrine tumors (pNET).

Sutent is also approved in a number of countries outside of the United States.

Sutent is known by several different names:

• Sutent, the brand name
• Sunitinib malate, 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. A phase II trial examining the effects of giving a lower dose of Sutent (37.5 mg) on a continuous basis concluded that Sutent appeared to be a safe and potentially effective dosing strategy for GIST patients. Although significant caution should be applied when comparing two different trial results, the median progression-free survival time of continuous dosing was 34 weeks (7.8 months) (see results). This compares favorably with the standard dosing schedule which produced a median progression-free survival time of 6.3 months. For GIST and Renal Cell Carcinoma, the FDA approved dosage remains (2011) at 50 mg on a 4/2 schedule. Interestingly, a later approval (2011) for pancreatic neuroendocrine tumors (pNET), is for the continuous dosing schedule at 37.5 mg.

Sutent is a tyrosine kinase inhibitor that is similar to Gleevec in some ways. Both drugs inhibit the KIT protein (mutated in 75-80% of GISTs) and the PDGFRα protein (mutated in 5-8% of GISTs). 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 provide a growth/survival signal through KIT activation and might still benefit from KIT inhibition (either by Gleevec or by Sutent).

Sutent also inhibits the "VEGF" receptors. VEGF is one of the most promising of the antiangiogenesis targets. For detailed information about angiogenesis visit the website of The Angiogenesis Foundation.

Financial Assistance

Patients and physicians can visit www.sutent.com or phone FirstRESOURCE at (877) 744-5675 for information about patient assistance for those who don’t have drug coverage and for information about reimbursement issues or appeals assistance.

Helpful Sites

Sutent Given US Approval

SU11248 works, trial ends 7 months early

Results from the (phase 1/2) Continuation Trial of SU11248 in Patients with Imatinib-resistant Gastrointestinal Stromal Tumor (GIST)

2005 ASCO presentation by Dr. Robert Maki

Fact sheet (Phase 1/2 trial summary)

(Results) Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled Trial of SU11248 in Patients Following Failure of Imatinib for Metastatic GIST

2005 ASCO presentation by Dr. George Demetri

Fact sheet (Phase 3 trial summary)

SU11248, a multi-targeted tyrosine kinase inhibitor, can overcome imatinib (IM) resistance caused by diverse genomic mechanisms in patients (pts) with metastatic gastrointestinal stromal tumor (GIST)

Managing the side effects of Sutent - a practical guide

Safety and efficacy of second-line sunitinib in GIST

Clinical evaluation of continuous daily dosing of sunitinib malate in patients with advanced gastrointestinal stromal tumour after imatinib failure
 

For more information about Sutent, call your doctor, visit www.sutent.com or see the full Prescribing Information.

Also see Sutent Dose Card and GIST Patient Brochure.