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Sunitinib Malate

Basic information Anticancer drug Uses Safety Related Supplier
Sunitinib Malate Basic information
Sunitinib Malate Chemical Properties
  • Melting point:189-191°C
  • storage temp. Store at +4°C
  • solubility DMSO: >10mg/mL
  • form powder
  • InChIKeyXGQXULJHBWKUJY-LYIKAWCPSA-N
  • CAS DataBase Reference341031-54-7(CAS DataBase Reference)
Safety Information
Sunitinib Malate Usage And Synthesis
  • Anticancer drugSunitinib malate is a kind of novel oral multi-targeted anticancer drugs and belongs to multi-targeted tyrosine kinase inhibitor with its trade name being “suntent”. It was successfully developed by Pfizer Company and has dual anti-tumor effect. Moreover, it is the only therapeutic drug which can go beyond the 2-year survival period of advanced kidney cancer and plays a central role in the field of carcinoma and gastrointestinal stromal tumor therapeutic areas. It entered into market in February 2006 in the United States. This drug was the first anti-cancer drug which was approved by the US FDA and can simultaneously treat two diseases.
    Sunitinib exerts its therapeutic role through preventing the tumor cells from getting the blood and nutrients needed for growth. Clinical trials have showed that the drug can delay the growth rate of gastrointestinal stromal tumors, and can shrink the size of renal cell tumors. Sunitinib malate is the first novel targeted drug being capable of selectively targets drugs for a variety of new tyrosine kinase receptors. It combine two kinds of anti-tumor mechanisms including both stopping the formation of anti-angiogenic which is responsible for supplying blood to tumor and direct attack of tumor cells. It represents the advent of a new round of targeted therapies, being able to attack the tumor directly without the toxicity of the conventional chemotherapy.
    The indications of Sunitinib malate are as follows:
    1, Patients who failed in the treatment with matinib mesylate or of intolerant gastrointestinal stromal tumors (GIST).
    2, inoperable advanced renal cell carcinoma (RCC).
    3, advanced pancreatic endocrine tumors.
    The above information is edited by the Chemicalbook of Dai Xiongfeng.
  • UsesAnti-cancer drugs
  • Chemical PropertiesYellow Solid
  • UsesSunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
  • UsesSunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit
  • UsesA multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). Antineoplastic.
  • brand name(Pfizer).
  • General DescriptionSunitinib is available in 12.5-, 25-, and 50-mg capsules fororal administration for the treatment of advanced RCC andGIST upon the failure of imatinib. The agent is a multikinaseinhibitor and has been shown to inhibit PDGF-R,VEGF-R, Kit, RET, and the colony-stimulating factor receptor(CSR-1R). The result of this spectrum of activity isa slowing of tumor progression and inhibition of angiogenesisboth of which are useful in the highly vascularizedcancers, RCC and GIST. The median TTP (time to tumorprogression) was 27.3 weeks for sunitinib and 6.4 weeks with a median time of 24.1 weeks for sunitinib and 6 weeksfor placebo. The agent is well absorbed upon oral administration,and both the parent and major metabolite are highly(90%–95%) protein bound. Metabolism is mediated primarilyby CYP3A4 to give the N-desethyl derivative, which isthe major metabolite (23%–37%), equally active with theparent and undergoes further metabolism by CYP3A4. Theterminal elimination half-life for the parent and N-desethylderivative are 40 to 60 hours and 80 to 110 hours, respectively.Elimination occurs primarily via the feces. Commonadverse effects of sunitinib include fatigue, diarrhea, yellowskin discoloration, anorexia, nausea, and mucositis.Mild myelosuppression has been reported in patients withGIST including neutropenia, lymphopenia, thrombocytopenia,and anemia. There have been reports of cardiotoxicityincluding decreases in left ventricular ejectionfraction, which occurred in 11% of patients during a GISTstudy.
  • Biological ActivityPotent, ATP-competitive VEGFR, PDGFR β and KIT inhibitor (K i values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFR β and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.
Sunitinib Malate(341031-54-7)Related Product Information
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