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crenolanib + azacitidine
- Development stage
- Unknown
- Lead developer
- AROG Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
Crenolanib + azacitidine is a combination therapy consisting of **crenolanib**, a potent and selective type I FLT3 kinase inhibitor, and **azacitidine**, a hypomethylating agent (epigenetic modulator). Crenolanib inhibits both FLT3-ITD and FLT3-TKD mutations, which drive poor prognosis and therapeutic resistance in acute myeloid leukemia (AML)[2][4]. Azacitidine modulates DNA methylation, promoting the differentiation and apoptosis of malignant cells[2]. The combination targets leukemia-initiating cells (LICs) in **FLT3-mutant AML**, overcoming protective stromal microenvironment mechanisms that confer resistance to FLT3 inhibitors alone, regardless of concurrent mutations (TET2, DNMT3A, NPM1)[1][2]. Early-phase (preclinical and translational) results indicate synergistic activity in FLT3-ITD AML, providing rationale for combination use in treatment-resistant or newly diagnosed AML. No specific proprietary brand name is associated; drugs are typically supplied as independent products by respective manufacturers.
- Other names
- crenolanib + AZAcrenolanib plus azacitidine
02
Targets
DNMT1 (DNA (cytosine-5)-methyltransferase 1)FLT3 (Fms related receptor tyrosine kinase 3)
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