Drug intelligence / Profile preview

GSK3145095

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK3145095 is an orally available small-molecule inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1). It was developed as a potential antineoplastic and immunomodulatory agent. By inhibiting RIPK1-mediated signaling pathways, GSK3145095 may reduce the recruitment and migration of immunosuppressive myeloid-derived suppressor cells in the tumor microenvironment. This action can enhance the activity of effector immune cells such as natural killer cells and cytotoxic T lymphocytes against cancer cells. RIPK1 plays a key role in inflammation and cell death responses to tissue damage or pathogen recognition; it is overexpressed in certain cancers and associated with oncogenesis and immune evasion. The drug was primarily investigated for advanced solid tumors including pancreatic ductal adenocarcinoma but its development was discontinued after Phase I/II trials[1][2][4][7].

Other names
1622849-43-7UNII-B4D3WPS7JYUNII-B-4D3WPS7JYUNII-B 4D3WPS7JY5-benzyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide
02

Targets

RIPK1 (Receptor-interacting serine/threonine-protein kinase 1)

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