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| Other names | KDS-2010; KDS2010; SeReMABI |
| Drug class | Reversiblemonoamine oxidase B (MAO-B)inhibitor |
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| Formula | C17H17F3N2O |
| Molar mass | 322.331 g·mol−1 |
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Tisolagiline (INNTooltip International Nonproprietary Name; developmental code namesKDS-2010,SeReMABI) is apotent, highlyselective, andreversiblemonoamine oxidase B (MAO-B)inhibitor which is under development for the treatment ofAlzheimer's disease andobesity.[1][2][3][4] It is takenby mouth.[1] Tisolagiline is being developed by NEUROBiOGEN and Scilex Bio.[1][2] As of December 2024, it is inphase 2clinical trials for Alzheimer's disease and obesity.[1][2]
4.4. KDS2010 A recently developed KDS2010, which is ~12,500-fold more selective to MAOB than MAOA, differentiates the role of MAOB from MAOA and reports that MAOB does not contribute to DA degradation [39]. KDS2010 is a potent (IC50 = 7.6 nM), and selective MAOB inhibitor named shows no known off-target effect (no other enzymes or channels causing >40% inhibition) or toxicity for 4 weeks of repeated dosing in non-human primates [16,41]. KDS2010 was turned out to be highly effective for alleviating the PD-related motor symptoms and PD-like pathology, including reactive astrogliosis, excessive astrocytic GABA, and nigrostriatal DAergic neuronal loss in multiple rodent models of PD [41]. Its clinical efficacy is still waiting to be tested in future studies.
KDS2010 is a novel compound highly potent and selective reversible MAO-B inhibitor (Fig. 2). It has demonstrated learning and memory improvements, promotion of synaptic transmission, and reduction of astrogliosis and astrocytic GABA levels in APP/presenilin 1 mice (Park et al. 2019).
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