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TOP-1288
- Development stage
- Phase 2
- Lead developer
- Topivert Pharma
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Rectal
01
Overview
TOP-1288 is a small molecule investigational drug developed as a narrow spectrum kinase inhibitor (NSKI) for the treatment of ulcerative colitis. It acts by inhibiting multiple protein kinases involved in inflammatory signaling pathways, including p38α (MAPK14), Src kinase, and Syk kinase. This multi-targeted inhibition leads to potent suppression of pro-inflammatory cytokine release from various immune and epithelial cells. The drug is designed for topical action in the colon with minimal systemic exposure to improve safety and tolerability compared to systemically acting therapies. Clinical studies have shown that TOP-1288 achieves high concentrations in colonic tissue with negligible systemic levels and demonstrates efficacy comparable to cyclosporine A in preclinical models of colitis[1][2][3][4][5][6][8].
- Other names
- UNII-19ZTZ9YC4OUNII19ZTZ9YC4OUNII 19ZTZ9YC4O
02
Targets
SRC (Proto-oncogene tyrosine-protein kinase Src)SYK (Spleen Tyrosine Kinase)MAPK14 (p38 mitogen-activated protein kinase alpha)
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