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.