- Sunitinib Malate Overviews
- What Can We Used Sunitinib Malate For?
- How Sunitinib Malate Works?
- How To Take Sunitinib Malate?
- How To Storage Sunitinib Malate?
- How Much We Know The Side Effects Of Sunitinib Malate?
- What Other Drugs Will Affect Sunitinib Malate?
- FDA approves Sunitinib Malate As Adjuvant Treatment Of Renal Cell Carcinoma
- Where Can I Buy Sunitinib Malate Online?
Sunitinib Malate(CAS:341031-54-7) was discovered at SUGEN, a biotechnology company which pioneered protein kinase inhibitors. It was the third in a series of compounds including SU5416 and SU6668. The concept was of an ATP mimic that would compete with ATP for binding to the catalytic site of receptor tyrosine kinases. This concept led to the invention of many small-molecule tyrosine kinase inhibitors, including Gleevec, Sutent, Tarceva and many others.
Sunitinib Malate Overviews
Sunitinib Malate is a yellow to orange powder. Sunitinib Malate is a small-molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor. On January 26, 2006, the agent was formally approved by the US FDA for the indications of treating renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). For these purposes, Sunitinib Malate is generally available as an orally administered formulation. Sunitinib Malate inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib Malate also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, Sunitinib Malate inhibits other RTKs including RET, CSF-1R, and flt3.
What Can We Used Sunitinib Malate For?
Sunitinib Malate is used to treat adults with kidney cancer that has not spread (localized) and who are at high risk of RCC coming back again after having kidney surgery.
Sunitinib Malate is used to treat advanced kidney cancer (advanced renal cell carcinoma or RCC).
Sunitinib Malate is used to treat a rare cancer of the stomach, bowel, or esophagus called gastrointestinal stromal tumor (GIST) and when you have taken the medicine imatinib mesylate and it did not stop the cancer from growing or you cannot take imatinib mesylate. Gleevec is a registered trademark of Novartis Pharmaceuticals Corporation.
Sunitinib Malate is used to treat a type of pancreatic cancer known as pancreatic neuroendocrine tumors (pNET) that has progressed and cannot be treated with surgery.
How Sunitinib Malate Works?
Sunitinib Malate is a small-molecule inhibitor of multiple receptor tyrosine kinases, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. The agent inhibits platelet-derived growth factor receptors -(PDGFRα and PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), FMS-like tyrosine kinase 3, colony-stimulating factor receptor type 1, and the glial cell-line derived neurotrophic factor receptor (RET). Sunitinib Malate inhibition of the activity and function of these receptor tyrosine kinases has been demonstrated in biochemical and cellular assays and cell proliferation assays. The primary metabolite of Sunitinib Malate exhibits potency similar to the parent compound in biochemical and cellular assays.
Sunitinib Malate inhibits phosphorylation of multiple receptor tyrosine kinases (PDGFRβ, VEGFR2, KIT) in tumor xenografts expressing receptor tyrosine kinase targets in vivo and inhibits tumor growth and metastasis in some experimental models. The agent inhibits growth of tumor cells expressing dysregulated target receptor tyrosine kinases (PDGFR, RET, or KIT) in vitro and PDGFRβ-and VEGFR2-dependent tumor angiogenesis in vivo.
How To Take Sunitinib Malate?
The Sunitinib Malate dosage your doctor prescribes will depend on several factors. These include:
❶ the type and severity of the condition you’re using Sunitinib Malate to treat
❷ other medical conditions you may have
❸ other medications you are taking
Your doctor will ultimately prescribe the smallest dosage that provides the desired effect.
The following information describes dosages that are commonly used or recommended. However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to fit your needs.
♦ Drug forms and strengths
Sunitinib Malate comes as a capsule that you swallow. It’s available in these strengths: 12.5 milligrams (mg), 25 mg, 37.5 mg, and 50 mg.
♦ Dosage for gastrointestinal cancer
The usual dosage of Sunitinib Malate for gastrointestinal stromal tumors (GISTs) is 50 mg once per day for 4 weeks. This is followed by 2 weeks without medication. Then, you’ll repeat the cycle.
You’ll likely continue taking Sunitinib Malate until your cancer worsens or your body can’t tolerate treatment with the drug. Your doctor will determine when you should stop taking Sunitinib Malate. For details on how Sunitinib Malate is used to treat GISTs, see the link as below.
♦ Dosage for kidney cancer
Sunitinib Malate is also used to treat a type of kidney cancer called advanced renal cell carcinoma (RCC). The usual dosage of Sunitinib Malate for advanced RCC is 50 mg once per day for 4 weeks. This is followed by 2 weeks without medication. Then, you’ll repeat the cycle.
You’ll likely continue taking Sunitinib Malate until your cancer worsens or your body can’t tolerate treatment with the drug. Your doctor will determine when you should stop taking Sunitinib Malate. For more information on how Sunitinib Malate is used to treat advanced RCC, see the link as below.
♦ Dosage for the adjuvant treatment of kidney cancer
Sunitinib Malate is also used as an adjuvant treatment for a type of kidney cancer called RCC after a nephrectomy (the surgical removal of a kidney). The usual dosage of Sunitinib Malate for this use is 50 mg once per day for 4 weeks. This is followed by 2 weeks without medication. You’ll typically repeat this cycle up to nine times. For details on how Sunitinib Malate is used as an adjuvant treatment for RCC, see the link as below.
♦ Dosage for pancreatic cancer
The usual dosage of Sunitinib Malate for advanced pancreatic neuroendocrine tumors (pNETs) is 37.5 mg once per day.
You’ll likely continue taking Sunitinib Malate until your cancer worsens or your body can’t tolerate treatment with the drug. Your doctor will determine when you should stop taking Sunitinib Malate.
Noted: the dosage was only reference, please help to check more details by this website:www.fda.gov .
How To Storage Sunitinib Malate?
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).
It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach.
Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website for more information if you do not have access to a take-back program.
How Much We Know The Side Effects Of Sunitinib Malate?
Sunitinib Malate adverse events are considered somewhat manageable and the incidence of serious adverse events low.
The most common adverse events associated with Sunitinib Malate 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 Malate 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 Malate therapy include lipase, amylase, neutrophils, lymphocytes, and platelets. Hypothyroidism and reversible erythrocytosis have also been associated with Sunitinib Malate. Most adverse events can be managed through supportive care, dose interruption, or dose reduction.
A recent study done at MD Anderson Cancer Center compared the outcomes of metastatic renal cell cancer patients who received Sunitinib Malate on the standard schedule (50 mg/4 weeks on 2 weeks off) with those who received Sunitinib Malate with more frequent and short drug holidays (alternative schedule). It was seen that the overall survival, progression free survival and drug adherence were significantly higher in the patients who received Sunitinib Malate on the alternative schedule. Patients also had a better tolerance and lower severity of adverse events which frequently lead to discontinuation of treatment of metastatic renal cell cancer patients.
What Other Drugs Will Affect Sunitinib Malate?
Sunitinib Malate can cause a serious heart problem. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.
Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.Tell your doctor about all your other medicines, especially: osteoporosis medicine.
This list is not complete. Other drugs may affect Sunitinib Malate, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.
FDA approves Sunitinib Malate As Adjuvant Treatment Of Renal Cell Carcinoma
On November 16, 2017, the Food and Drug Administration approved Sunitinib Malate (Sunitinib Malate, Pfizer Inc.) for the adjuvant treatment of adult patients at high risk of recurrent renal cell carcinoma following nephrectomy.
Approval was based on a multi-center, international, double-blind, placebo-controlled, trial (S-TRAC), in 615 patients with high risk of recurrent RCC following nephrectomy. Patients were randomized 1:1 to receive either 50 mg Sunitinib Malate once daily, 4 weeks on treatment followed by 2 weeks off, or placebo. Median disease-free survival for patients taking Sunitinib Malate was 6.8 years (95% CI: 5.8, not reached) compared with 5.6 years (95% CI: 3.8, 6.6) for patients receiving placebo (HR=0.76; 95% CI: 0.59, 0.98; p=0.03). At the time of DFS analysis, overall survival data were not mature.
The most common adverse reactions (≥25%) to Sunitinib Malate are fatigue/asthenia, diarrhea, mucositis/stomatitis, nausea, decreased appetite/anorexia, vomiting, abdominal pain, hand-foot syndrome, hypertension, bleeding events, dysgeusia/altered taste, dyspepsia, and thrombocytopenia. The labeling contains a boxed warning to alert healthcare professionals and patients about the risk of hepatoxicity, which may result in liver failure or death.
The recommended dose of Sunitinib Malate for the adjuvant treatment of RCC is 50 mg orally once daily, with or without food, 4 weeks on treatment followed by 2 weeks off for nine 6-week cycles.
Noted: Full prescribing information is available at:accessdata.fda.gov PDF.
Where Can I Buy Sunitinib Malate Online?
There are many supplier/manufacturers of Sunitinib Malate powder in the market, finding genuine one is very important for all peoples who need this product urgently. When we decide to buy Sunitinib Malate powder in the market, we need to learn more information about it, know how to use it and it’s mechanism of action, any risks when we take Sunitinib Malate powder…. In addition, price and quality must be our concerns before buy it.
After we surveyed datas from market, compared many suppliers, AASraw looks a good choices for those people who want buy lot of Sunitinib Malate powder, their production was controlled strictly under cGMP condition, the quality can be tracked at any time and they may provided all testing reports when you order it. As for the Sunitinib Malate powder costs/price, it should be reasonable, in my eyes. Because I have got many prices from different Sunitinib Malate suppliers, compared with quality, I think aasraw will be not bad choice.
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