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AKN-028
- Development stage
- Discontinued
- Lead developer
- Accelerated Innovation Europe
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
AKN-028 is an orally bioavailable small molecule tyrosine kinase inhibitor developed for the treatment of acute myeloid leukemia (AML). It potently inhibits FMS-like tyrosine kinase 3 (FLT3) and stem cell factor receptor (KIT), targeting both wild-type and mutated forms. By inhibiting these kinases, AKN-028 blocks tumor cell proliferation in cancers overexpressing these receptors. Preclinical studies show that AKN-028 induces dose-dependent cytotoxicity and apoptosis in AML cells regardless of FLT3 mutation status. The drug also causes cell cycle arrest and downregulates Myc-associated genes. In animal models, it demonstrated high oral bioavailability and antileukemic effects with low toxicity. Clinical development has reached phase II trials for AML[1][4][5][6][7].
- Other names
- N2-(1H-Indol-5-yl)-6-(pyridin-4-yl)pyrazine-2,3-diamine1175017-90-9UNII-Y66IS3CS0RUNII-Y-66IS3CS0RUNII-Y 66IS3CS0RY66IS3CS0RY-66IS3CS0RY 66IS3CS0R
02
Targets
CLK1 (CDC-like kinase 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)RSK (RSK family)FGFR2 (Keratinocyte growth factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)
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