Newly clarified efficacy and role of giritinib fumarate

Patients with FLT3 mutationsacute myeloid leukemia (AML) whose disease has recurred or failed to improve after prior treatment have a poor prognosis and limited treatment options. Gilteritinib has been shown to extend patients' lives compared with other cancer treatments. The side effects of giritinib are expected for this class of drugs and are considered manageable. Inhibition of giritinib on the receptor tyrosine kinaseAXL, which is known to regulate the activity of FLT3 in acute myeloid leukemia.

Ina phase 1/2 clinical trial, giditinib showed a composite complete response of 41%, an overall response rate of 52%, a median duration of response of 20 weeks, and a median overall survival of 31 weeks. In preclinical trials, giditinib had an IC50 of 5 nM against wild-type receptors and an IC50 of 0.7-1.8 nM against ITD mutations, and its inhibitory effect on TKD mutations was comparable to other therapies. Another important result in vivo is high-level localization in xenograft tumors, indicating high selectivity.

The original drug of giritinib has been launched in China, but it has not yet been included in the medical insurance. The price of each box of 40mg*42 tablets may be more than 20,000 yuan, and the price of the Hong Kong version of the original drug is about 90,000 yuan per box. The price of the European version of the original drug, 40mg*84 tablets, per box listed overseas is around RMB 210,000 (the price may fluctuate due to exchange rates), which is very expensive. Generic drugs of giritinib are currently produced and sold overseas, and their drug ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of 40mg*84 tablets per box produced by a Laos pharmaceutical factory is more than 4,000 yuan (the price may fluctuate due to the exchange rate).