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denibulin
- Development stage
- Unknown
- Lead developer
- MediciNova
- Modality
- Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Denibulin is a novel small molecule antineoplastic agent that selectively targets and reversibly binds to the colchicine-binding site on tubulin. By inhibiting microtubule assembly, denibulin disrupts the cytoskeleton of tumor endothelial cells, leading to cell cycle arrest, blockage of cell division, and apoptosis. This mechanism also results in inadequate blood flow to tumors and a decrease in tumor cell proliferation. Denibulin hydrochloride was investigated in phase I clinical trials for the treatment of solid tumors; it was generally well tolerated and showed decreases in tumor vascular parameters. However, no recent development has been reported for this drug[8][10].
- Brand names
- ParaplatinHalaven
- Other names
- denibulin hydrochloride
02
Targets
TUBB (Tubulin (alpha and beta subunits))
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