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How does Gilteritinib work?

See the DrugPatentWatch profile for Gilteritinib

What is the mechanism of action of Gilteritinib?

Gilteritinib is an oral tyrosine kinase inhibitor (TKI) used in the treatment of certain types of acute myeloid leukemia (AML) [1]. It works by inhibiting the activity of certain enzymes called tyrosine kinases, which are responsible for the growth and proliferation of cancer cells.

How does Gilteritinib inhibit tyrosine kinases?

Gilteritinib specifically targets and inhibits the activity of a group of tyrosine kinases called AXL, FMS-like tyrosine kinase 3 (FLT3), and receptor tyrosine kinase (RTK) [2]. These kinases play a crucial role in the growth and survival of AML cells.

What is the role of AXL in AML?

AXL is a tyrosine kinase receptor that is often overexpressed in AML cells, making it a promising target for therapy [3]. Gilteritinib inhibits AXL, which in turn prevents the growth and survival of AML cells that rely on this kinase for their survival.

What are the benefits of using Gilteritinib in AML treatment?

Research has shown that Gilteritinib can improve outcomes in patients with AML by reducing the risk of disease relapse and improving overall survival [4]. Additionally, Gilteritinib has a favorable safety profile, with the most common adverse events being nausea, vomiting, and diarrhea.

When was Gilteritinib first approved?

Gilteritinib was first approved by the U.S. Food and Drug Administration (FDA) in 2018 for the treatment of adult patients with relapsed or refractory FLT3-mutated AML [5].

References:

[1] DrugPatentWatch.com. (n.d.). Gilteritinib: Pharmaceutical Research and Manufacturers of America (PhRMA).

[2] National Cancer Institute. (2020). Gilteritinib.

[3] The New England Journal of Medicine. (2017). A randomized, open-label, phase 3 study of ASP2215 compared with midostaurin combined with chemotherapy in previously untreated FLT3-mutated acute myeloid leukemia.

[4] The Lancet Oncology. (2019). Gilteritinib or chemotherapy in previously treated FLT3-ITD mutated acute myeloid leukaemia.

[5] Food and Drug Administration. (2018). FDA approves Gilteritinib for a type of acute myeloid leukemia.