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kukoamine B
- Development stage
- Phase 2
- Lead developer
- Tianjin Chase Sun Pharmaceutical
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Kukoamine B is a small molecule spermine alkaloid originally isolated from the traditional Chinese herb Lycium chinense. It acts as a novel dual inhibitor of both lipopolysaccharide (LPS) and CpG DNA, which are key pathogenic molecules involved in the induction of sepsis. Kukoamine B directly binds to LPS and CpG DNA, neutralizing them and preventing their interaction with immune cell receptors such as Toll-like receptor 4 (TLR4) and Toll-like receptor 9 (TLR9). This action inhibits downstream pro-inflammatory signaling without affecting cell viability or other signal pathways in macrophages. Kukoamine B has demonstrated antioxidant and anti-inflammatory properties in preclinical studies, showing protective effects against severe sepsis in animal models. It is currently being developed for intravenous treatment of sepsis, with clinical trials reaching Phase II status[1][3][5][8].
- Other names
- kukoamine B mesilate地骨皮乙素
02
Targets
CpG DNANMDAR (Glutamate receptor ionotropic, NMDA)
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