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.
In a world-wide treatment use trial of 1131 GIST patients1, a flexible dosing schedule resulted in a longer time on medication (12.6 months vs 5.2 months) and a longer overall survival (23.4 months vs 11.1 months) compared to patients that remained strictly on the starting dose schedule (4 weeks on/2 weeks off at 50 mg). A higher percentage of patients on the flexible dosing did experience increased side effects (adverse events) compaired to the strict starting dose schedule. The authors concluded, "Patients with GIST who received sunitinib using a FD (flexible dosing) approach to manage AEs (adverse events) remained on treatment longer than those who received the strict starting dose schedule and exhibited better clinical outcomes (longer time to progression and overall survival).
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.
|Target Proteins Inhibited|
|abl (including bcr/abl)||VEGFR1|
presentation about Sutent for GIST
Sutent comes in 12.5, 25 and 50 mg capsules
Side Effect Guide
Being able to properly manage the side effects of Sutent, or any drug, is one of the key steps required to allow patients to take their medication as prescribed by their doctor. It is also one of the keys for feeling better and being able to do the things that are important to you.
Sutent.com has an interactive guide to help patients create a list of symptoms and side effects to share with their doctor.
Note: These links take you to the Sutent.com website
Caution: Proper monitoring is required for patients on Sutent. This includes, but is not limited to, monitoring thyroid function, blood pressure, blood counts and monitoring for heart problems. See the Sutent prescribing information and the article below.
In a study of kidney cancer patients taking Sutent, severe toxicities were worse in older patients and females. Thus age and gender may predict those at higher risk for severe toxicity.
A possible drug interaction with bisphophonates (drugs used to treat osteoporosis and bone metastastes) has been reported. See osteonecrosis of the jaw
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.
View a presentation about accessing Sutent; financial assistance, etc
Fact sheet (Phase 1/2 trial summary)
Fact sheet (Phase 3 trial summary)
1. Optimizing Management of Sunitinib Treatment in a Worldwide Treatment-use Trial of Patients (Pts) With Advanced Gastrointestinal Stromal Tumour (GIST) 2011 European Multidisciplinary Cancer Congress, Abstract # 9421
P. Reichardt , Y.K. Kang, P. Rutkowski, J. Schuette, L.S. Rosen, B. Seddon, S. Yalcin, L. Chen, K. Fly, G.D. Demetri