Product Description
Reference Standards &Impurity
AI Product Description
*The following content is generated by AI and is for reference only.
Gilteritinib, chemically known as (S)-N-(1-((3-chlorophenyl)methyl)pyrrolidin-3-yl)-2-(4-(4-isopropylpiperazin-1-yl)phenyl)acetamide, is a potent and selective tyrosine kinase inhibitor (TKI) specifically designed to target the FLT3 receptor. Its molecular formula is C26H30ClN5O, with a corresponding CAS registry number of 1899747-56-6. This small molecule exhibits high affinity for both the FLT3 internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations, which are prevalent in acute myeloid leukemia (AML). Gilteritinib functions by binding to the ATP-binding pocket of the FLT3 protein, thereby inhibiting downstream signaling pathways essential for leukemic cell proliferation and survival.
Clinically, gilteritinib has emerged as a standard-of-care treatment for patients with relapsed or refractory AML harboring FLT3 mutations. It was approved by regulatory agencies globally based on robust clinical trial data demonstrating significant overall response rates and improved survival outcomes compared to conventional chemotherapy regimens. Unlike earlier-generation FLT3 inhibitors, gilteritinib possesses an optimized pharmacokinetic profile that allows for once-daily oral administration, enhancing patient compliance and quality of life. Furthermore, it demonstrates efficacy against various FLT3 resistance mutations, making it a versatile therapeutic option in the management of this aggressive hematologic malignancy.
The drug is typically administered orally until disease progression or unacceptable toxicity occurs. Common adverse events include fatigue, diarrhea, nausea, and thrombocytopenia, though serious side effects like differentiation syndrome require careful monitoring and management. As research continues, gilteritinib is also being investigated in combination therapies with other agents such as venetoclax or hypomethylating agents to broaden its applicability in newly diagnosed AML cases. Its development represents a significant milestone in precision oncology, offering a targeted approach that addresses the specific genetic drivers of AML while minimizing damage to healthy cells. By selectively inhibiting mutant FLT3, gilteritinib provides a crucial tool for clinicians aiming to achieve deeper remissions and prolong survival in patients who have exhausted other treatment options.