Why giritinib/segatan is the first choice for leukemia treatment

Gilitinib/Segatan as a new type of FLT3 tyrosine kinase inhibitor, has become the drug of choice for the treatment of patients with FLT3 mutations in acute myeloid leukemia (AML). Its advantages in mechanism, efficacy, safety and clinical application make it occupy an important position in the treatment of AML.

FLT3 gene mutation is one of the common driver mutations in AML, accounting for approximately 25% to 30% of all AML cases. These mutations mainly include internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations. FLT3 mutations lead to continuous activation of its receptor tyrosine kinase, promoting the proliferation and survival of leukemia cells, thereby accelerating the progression of the disease and reducing the prognosis of patients. Therefore, targeted therapy targeting FLT3 mutations has become a key strategy to improve the prognosis of AML patients.

Giritinib, as a second-generationFLT3 inhibitor, has significant pharmacological properties. Compared with the first-generation FLT3 inhibitors, giritinib has a potent inhibitory effect on both FLT3 ITD and TKD mutations, and also inhibits the AXL receptor, which may enhance its anti-leukemia activity. In addition, the inhibition of AXL receptors by giritinib may help overcome resistance to FLT3 inhibitors. These properties give giritinib unique advantages in the treatment of FLT3 mutant AML.

In clinical studies, giritinib has shown significant efficacy in patients with FLT3 mutant relapsed or refractory AML. In multiple studies, the overall survival (OS) and complete response rate (CR) of the gilitinib group were superior to traditional salvage chemotherapy regimens. For example, the COMMODORE study showed that the median OS of the geritinib group was 9.6 months, which was significantly higher than the 5.0 months of the chemotherapy group. These results demonstrate the superiority of giritinib in the treatment of FLT3 mutant AML.

In addition, the safety of giritinib has also been widely recognized. In clinical trials, giritinib was well tolerated. Common adverse reactions include abnormal liver function, anemia, febrile neutropenia, etc. Most of them are mild to moderate and can be recovered after stopping the drug or adjusting the dose. The incidence of these adverse reactions is low and can be tolerated by most patients, ensuring its clinical application.

The approval history of gilitinib also reflects its success inimportant role in the treatment of AML. In November 2018, the U.S. FDA approved giritinib for the treatment of adult patients with FLT3-mutant relapsed or refractory AML, becoming the first approved monotherapy regimen. Since then, giritinib has been approved in many countries and regions, including China, Europe and Japan. These approvals mark the widespread use of gilitinib worldwide.

To sum up, giritinib has become the preferred treatment option for patients with FLT3 mutant AML due to its efficient inhibitory effect onFLT3 mutation, good safety and significant clinical efficacy. With in-depth research on its mechanism of action and clinical application, giritinib is expected to play a more important role in the treatment of AML.

Reference materials:https://www.xospata.com/