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elraglusib
- Development stage
- Phase 2
- Lead developer
- Actuate Therapeutics
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Elraglusib is a maleimide-based, small molecule inhibitor of glycogen synthase kinase-3 beta (GSK-3β), developed by Actuate Therapeutics for the treatment of various cancers. It acts as an ATP-competitive inhibitor of GSK3, leading to downregulation of nuclear factor kappa B (NF-kappaB) and decreased expression of its target genes, including cyclin D1, Bcl-2, XIAP, and Bcl-xL. This results in inhibition of tumor cell survival pathways and chemoresistance. Elraglusib also mediates anti-tumor immunity through regulation of immune checkpoints and immune cell function. It has demonstrated antitumor activity across several solid tumors such as melanoma, Ewing sarcoma, colorectal cancer, pancreatic cancer (including metastatic pancreatic ductal adenocarcinoma), soft tissue sarcoma, bone sarcomas, myelofibrosis, and hematologic malignancies[1][2][4][5][7].
- Other names
- elraglusibElraglusib [USAN]UNII-ND1SOF0DLUUNII-ND-1SOF0DLUUNII-ND 1SOF0DLU
02
Targets
GSK3 (Glycogen synthase kinase 3 beta)
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