FLT-3 inhibitors can be expected in the future, and there is a new drug for acute myeloid leukemia!

2020/12/09

Leukemia, from the discoloration of hearing in the early years to the long-term survival of today, is still a serious illness but it is no longer impossible. Gleevec pioneered targeted drugs for leukemia. Although it is a miracle drug, it still cannot cure all diseases; and even in the field of leukemia diseases, such as acute myeloid leukemia, targeted drugs have not been produced until recent years. ; Among them, FLT-3 inhibitors are gradually showing their clinical value.

Acute myeloid leukemia (AML) accounts for about 70% of adult leukemias.

Since 2017, targeted drugs in the AML field have been produced successively, among which FLT-3 inhibitors account for a relatively large proportion, and dozens of drug candidates have entered clinical development.



FLT-3 inhibitors have been marketed traditional multi-target drugs

The first-generation FLT-3 inhibitors that have been marketed are all multi-target inhibitors. The representative varieties are Sorafenib (2005), Sunitinib (2006), and Panatinib (2013). , Cabozantinib (2013), the IC50 value of FLT-3 is between 1-60 nM; and in terms of sales, sorafenib and sunitinib are both major varieties with annual sales of more than 1 billion US dollars .


Since the first-generation drugs are multi-target drugs, there are some unavoidable side effects, such as diarrhea, anorexia, fatigue, nausea, rash, acne, joint pain, etc.; therefore, a more effective FLT-3 inhibitor It has been developed and approved for marketing, and its indications are mainly concentrated in acute myeloid leukemia.

New varieties of FLT-3 inhibitors marketed in the past 5 years



Midostaurin


Gilteritinib



Quizartinib


In summary, it is the target, indications and development of marketed drugs for FLT-3 inhibitors. In terms of targets, it is already a mature drug target; in terms of indications, it is now mainly focused on acute myeloid leukemia; marketed drugs have gradually shifted from multiple targets to highly active and selective inhibitors, which are fully in line with a drug target The logic of drug development. However, perhaps due to the scope of indications and the short time to market, the varieties on the market in recent years have not yet shown eye-catching market value. However, it is worth noting that there are dozens of drugs under research for this target, and the breadth and depth of development are expanding. The future potential is still worth looking forward to.