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Sunitinib Malate

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Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs).These include all receptors for platelet-derived growth factor (PDGF-Rs) and vascular endothelial growth factor receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation.

Product Description

Basic Characteristics

Product Name Sunitinib Malate
CAS Number 341031-54-7
Molecular Formula C22H27FN4O2
Molar mass 398.474
Synonyms 557795-19-4;

Sutent;

Sunitinib malate;

SU11248.

Appearance White powder
Storage and Handling Store it at room temperature and away from excess heat and moisture.

 

Sunitinib Malate Description

Sunitinib (marketed as Sutent by Pfizer, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications.

 

Sunitinib Malate Mechanism of Action

Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs).

These include all receptors for platelet-derived growth factor (PDGF-Rs) and vascular endothelial growth factor receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation. The simultaneous inhibition of these targets therefore reduces tumor vascularization and triggers cancer cell apoptosis and thus results in tumor shrinkage.

Sunitinib also inhibits CD117 (c-KIT),[2] the receptor tyrosine kinase that (when improperly activated by mutation) drives the majority of gastrointestinal stromal cell tumors.It has been recommended as a second-line therapy for patients whose tumors develop mutations in c-KIT that make them resistant to imatinib, or who the cannot tolerate the drug.

 

Sunitinib Malate Application

 Gastrointestinal stromal tumor

Like RCC, GIST does not generally respond to standard chemotherapy or radiation. Imatinib was the first cancer agent proven effective for metastatic GIST and represented a major development in the treatment of this rare but challenging disease.

 

 Meningioma

Sunitinib is being studied for treatment of meningioma which is associated with neurofibromatosis.

 

 Pancreatic neuroendocrine tumors

In November 2010, Sutent gained approval from the European Commission for the treatment of ‘unresectable or metastatic, well-differentiated pancreatic neuroendocrine tumors with disease progression in adults’.

 

 Renal cell carcinoma

Sunitinib is approved for treatment of metastatic RCC. Other therapeutic options in this setting are pazopanib (Votrient), sorafenib (Nexavar), temsirolimus (Torisel), interleukin-2 (Proleukin), everolimus (Afinitor), bevacizumab (Avastin), and aldesleukin.

 

Sunitinib MalateSide Effects & Warning

Sunitinib adverse events are considered somewhat manageable and the incidence of serious adverse events low.

The most common adverse events associated with sunitinib therapy are fatigue, diarrhea, nausea, anorexia, hypertension, a yellow skin discoloration, hand-foot skin reaction, and stomatitis. In the placebo-controlled Phase III GIST study, adverse events which occurred more often with sunitinib than placebo included diarrhea, anorexia, skin discoloration, mucositis/stomatitis, asthenia, altered taste, and constipation.

Dose reductions were required in 50% of the patients studied in RCC in order to manage the significant toxicities of this agent.

Serious (grade 3 or 4) adverse events occur in ≤10% of patients and include hypertension, fatigue, asthenia, diarrhea, and chemotherapy-induced acral erythema. Lab abnormalities associated with sunitinib therapy include lipase, amylase, neutrophils, lymphocytes, and platelets. Hypothyroidism and reversible erythrocytosis have also been associated with sunitinib.

 

Reference

[1] US Food and Drug Administration (2006). “FDA approves new treatment for gastrointestinal and kidney cancer”.

[2] Hartmann JT, Kanz L (November 2008). “Sunitinib and periodic hair depigmentation due to temporary c-KIT inhibition”. Arch Dermatol. 144 (11): 1525–6. doi:10.1001/archderm.144.11.1525. PMID 19015436. Archived from the original on 2011-07-25.

[3] Quek R, George S (February 2009). “Gastrointestinal stromal tumor: a clinical overview”. Hematol. Oncol. Clin. North Am. 23 (1): 69–78, viii. doi:10.1016/j.hoc.2008.11.006. PMID 19248971.

[4] Blay JY, Reichardt P (June 2009). “Advanced gastrointestinal stromal tumor in Europe: a review of updated treatment recommendations”. Expert Rev Anticancer Ther. 9 (6): 831–8. doi:10.1586/era.09.34. PMID 19496720. S2CID 23601578.

[5] Gan HK, Seruga B, Knox JJ (June 2009). “Sunitinib in solid tumors”. Expert Opin Investig Drugs. 18 (6): 821–34. doi:10.1517/13543780902980171. PMID 19453268. S2CID 25353839.

[6] “Prescribing information for Sutent (sunitinib malate)”. Pfizer, Inc, New York NY.