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Gilteritinib: potent targeting of FLT3 mutations in AML.

08:00 EDT 24th March 2020 | BioPortfolio

Summary of "Gilteritinib: potent targeting of FLT3 mutations in AML."

Since the discovery of FMS-like tyrosine kinase-3 (FLT3)-activating mutations as genetic drivers in acute myeloid leukemia (AML), investigators have tried to develop tyrosine kinase inhibitors that could effectively target FLT3 and alter the disease trajectory. Giltertinib (formerly known as ASP2215) is a novel compound that entered the field late, but moved through the developmental process with remarkable speed. In many ways, this drug's rapid development was facilitated by the large body of knowledge gained over the years from efforts to develop other FLT3 inhibitors. Single-agent gilteritinib, a potent and selective oral FLT3 inhibitor, improved the survival of patients with relapsed or refractory FLT3-mutated AML compared with standard chemotherapy. This continues to validate the approach of targeting FLT3 itself and establishes a new backbone for testing combination regimens. This review will frame the preclinical and clinical development of gilteritinib in the context of the lessons learned from its predecessors.

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This article was published in the following journal.

Name: Blood advances
ISSN: 2473-9537
Pages: 1178-1191

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PubMed Articles [8260 Associated PubMed Articles listed on BioPortfolio]

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Medical and Biotech [MESH] Definitions

A cytoplasmic receptor and peroxin that contains a series of TETRACOTIPEPTIDE REPEATS and binds to PEROXISOME TARGETING SIGNAL 1 (SKL-type). It is essential for protein import into PEROXISOMES; mutations in the PEX5 gene are associated with PEROXISOMAL DISORDERS such as ZELLWEGER SYNDROME.

A cytoplasmic receptor and peroxin that contains a series of WD40 REPEATS and binds to PEROXISOME TARGETING SIGNAL 2. It is essential for protein import into PEROXISOMES; mutations in the human PEX7 gene are associated with PEROXISOMAL DISORDERS such as Type 1 CHONDRODYSPLASIA PUNCTATA, RHIZOMELIC.

Proteins that are essential for the assembly of PEROXISOMES. They recognize and transport cytoplasmic proteins that contain PEROXISOMAL TARGETING SIGNALS (PTS) to the peroxisome. Mutations in peroxin (PEX) genes are associated with several PEROXISOMAL DISORDERS.

Mutations in genes which lead to cell or organism death when occurring in combination with mutations in one or more other genes.

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