Gilteritinib, also known as ASP2215 or its chemical name N-[(3R,4S)-4-[7-Chloro-1-(2,6-dichloro-3-fluorophenyl)-2,3-dihydroimidazo[1,2-c]pyrimidin-5-yl]-3-cyano-1-azetidinyl]-4-methylbenzamide, is a small molecule drug that has been developed for the treatment of acute myeloid leukemia (AML). It belongs to a class of drugs called tyrosine kinase inhibitors (TKIs).
Chemical name: N-[(3R,4S)-4-[7-Chloro-1-(2,6-dichloro-3-fluorophenyl)-2,3-dihydroimidazo[1,2-c]pyrimidin-5-yl]-3-cyano-1-azetidinyl]-4-methylbenzamide
Molecular formula: C29H29Cl2N7O
Formula weight: 556.50 g/mol
CAS No: 1254053-43-4
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Health benefits of this product:
Gilteritinib has shown promising results in treating patients with AML who have a specific mutation in the FLT3 gene, known as an FLT3 mutation. This mutation is present in approximately one-third of patients with AML and is associated with a poorer prognosis. Gilteritinib works by blocking the activity of FLT3, which can help to slow down or stop the growth of cancer cells. Clinical trials have shown that gilteritinib can improve overall survival and reduce the risk of relapse in patients with AML who have an FLT3 mutation.
Potential effects:
The potential effects of gilteritinib include:
Product mechanism:
Gilteritinib is a selective inhibitor of FLT3, which is a receptor tyrosine kinase that plays a key role in the development and progression of AML. FLT3 is overexpressed in approximately one-third of patients with AML and is associated with a poor prognosis. Gilteritinib binds to the ATP-binding site of FLT3 and inhibits its activity, which can help to slow down or stop the growth of cancer cells. By blocking the activity of FLT3, gilteritinib can potentially improve outcomes in patients with AML who have an FLT3 mutation.
Safety:
In clinical trials, gilteritinib was generally well-tolerated, with most adverse events being mild or moderate in severity. The most common side effects were diarrhea, fatigue, nausea, increased blood creatinine levels, and elevated liver enzymes. Serious adverse events were reported in some patients, including pneumonia, sepsis, and cardiac events. Gilteritinib may also cause a prolongation of the QT interval, which can lead to an increased risk of arrhythmias. Therefore, patients should be closely monitored for any signs of cardiac toxicity.
Side effects:
The most common side effects of gilteritinib include:
Dosing information:
The recommended dose of gilteritinib is 120 mg once daily, taken orally with or without food. The dose may need to be adjusted based on individual patient factors, such as renal function or concomitant use of certain medications. Patients should be closely monitored for any signs of adverse events or cardiac toxicity.
Conclusion:
Gilteritinib is a promising new therapy for the treatment of AML in patients with an FLT3 mutation. It has been shown to significantly improve overall survival and reduce the risk of relapse in these patients. However, like all cancer treatments, it comes with potential risks and side