All About Sutent
General Information | Phase III trial results | Why Sutent might work if Gleevec fails
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.
Sutent is also approved in a number of countries outside of the United States and is available in others through a treatment use protocol. See the clinical trials section for more information about this option.
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 on a continuous basis is in progress.
Sutent is a tyrosine kinase inhibitor that is similar to Gleevec in some ways. Both drugs inhibit the KIT protein (mutated in 80-85% of GISTs) and the PDGFRα protein (mutated in 5-7% 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).
Both Sutent and Gleevec also provide an antiangiogenic effect through inhibition of PDGFRβ. PDGFRβ is involved in the recruitment of pericytes, which are needed to form new blood vessels to feed the tumors.
In addition to inhibiting these three proteins, Sutent provides an additional antiangiogenic effect that Gleevec does not; Sutent 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 | |
|---|---|
| Gleevec | Sutent |
| KIT | KIT |
| PDGFRα | PDGFRα |
| PDGFRβ | PDGFRβ |
| abl (including bcr/abl) | VEGFR1 |
| VEGFR2 | |
| VEGFR3 | |
| FLT3 | |
| CSF-1R | |
| RET | |
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View a
presentation about Sutent for GIST
(loads slowly) |
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Sutent Capsules
Sutent comes in 12.5, 25 and 50 mg capsules
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.
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View a presentation about accessing Sutent; financial assistance, etc |
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Additional Links
- Sutent Given US Approval
- Sutent 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
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:
https://www.sutenthcp.com/downloads/Dose-Card.pdf
https://www.sutenthcp.com/downloads/GIST_Patient_Brochure.pdf
