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Review
. 2019 Sep 11:7:19.
doi: 10.1186/s40364-019-0170-2. eCollection 2019.

Gilteritinib: a novel FLT3 inhibitor for acute myeloid leukemia

Juanjuan Zhao  1 , Yongping Song  1 , Delong Liu  1   2
Affiliations
Review

Gilteritinib: a novel FLT3 inhibitor for acute myeloid leukemia

Juanjuan Zhao et al. Biomark Res. .

Erratum in

Abstract

FMS-like tyrosine kinase 3- internal tandem duplication (FLT3-ITD) remains as one of the most frequently mutated genes in acute myeloid leukemia (AML), especially in those with normal cytogenetics. The FLT3-ITD and FLT3-TKD (tyrosine kinase domain) mutations are biomarkers for high risk AML and are associated with drug resistance and high risk of relapse. Multiple FLT3 inhibitors are in clinical development, including lestaurtinib, tandutinib, quizartinib, midostaurin, gilteritinib, and crenolanib. Midostaurin and gilteritinib have been approved by FDA for Flt3 mutated AML. Gilteritinib (ASP2215, Xospata) is a small molecule dual inhibitor of FLT3/AXL. The ADMIRAL study showed that longer overall survival and higher response rate are associated with gilteritinib in comparison with salvage chemotherapy for relapse /refractory (R/R) AML. These data from the ADMIRAL study may lead to the therapy paradigm shift and establish gilteritinib as the new standard therapy for R/R FLT3-mutated AML. Currently, multiple clinical trials are ongoing to evaluate the combination of gilteritinib with other agents and regimens. This study summarized clinical trials of gilteritinib for AML.

Keywords: FLT3; FLT3 inhibitor; Gilteritinib; Tyrosine kinase inhibitor.

PubMed Disclaimer

Conflict of interest statement

DL serves on the Xospata speaker bureau of Astellas. Astellas was not involved in this publication.

Figures

Fig. 1
Fig. 1
The ADMIRAL study scheme. The ADMIRAL study is an open-label multicenter randomized phase 3 study for adults with relapsed and/or refractory AML with FLT3 mutations. The randomization between gilteritinib and one of the four salvage chemotherapy regimens was 2:1. To date, the accrual has been completed with 371 patients randomized. MEC: mitoxantrone, etoposide, cyclophosphamide; FLAG-IDA: fludarabine, cytarabine, GCSF, idarubicin; CR/CRh: complete remission with partial hematologic recovery; OS: overall survival
See this image and copyright information in PMC

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