Harman Patil (Editor)

Quizartinib

Updated on
Edit
Like
Comment
Share on FacebookTweet on TwitterShare on LinkedInShare on Reddit
Quizartinib fileselleckchemcomdownloadsstructAC220chemic

Dr levis discusses the ideal use of quizartinib in flt3 itd aml


Quizartinib (AC220) is a small molecule receptor tyrosine kinase inhibitor that is currently under development by Ambit Biosciences for the treatment of acute myeloid leukaemia. Its molecular target is FLT3, also known as CD135 which is a proto-oncogene.

Contents

Flt3 mutations are among the most common mutations in acute myeloid leukaemia due to internal tandem duplication of Flt3. The presence of this mutation is a marker of adverse outcome.

Quizartinib ac220 is a second generation


Mechanism

Specifically, Quizartinib selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs).

Mutations cause constitutive action of Flt3 resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis.

Clinical trials

It reported good results in 2012 from a phase II clinical trial for refractory AML - particularly in patients who went on to have a stem cell transplant.

As of 2017 it has completed 5 clinical trials and another 7 are active.

References

Quizartinib Wikipedia