Tisolagiline (INNTooltip International Nonproprietary Name; developmental code names KDS-2010, SeReMABI) is a potent, highly selective, and reversible monoamine oxidase B (MAO-B) inhibitor which is under development for the treatment of Alzheimer's disease and obesity.[1][2][3][4] It is taken by mouth.[1] Tisolagiline is being developed by NEUROBiOGEN and Scilex Bio.[1][2] As of December 2024, it is in phase 2 clinical trials for Alzheimer's disease and obesity.[1][2]

References

  1. ^ a b c d "KDS 2010". AdisInsight. 6 February 2025. Retrieved 24 February 2025.
  2. ^ a b c "Delving into the Latest Updates on KDS-2010 with Synapse". Synapse. 23 January 2025. Retrieved 24 February 2025.
  3. ^ Nam MH, Sa M, Ju YH, Park MG, Lee CJ (April 2022). "Revisiting the Role of Astrocytic MAOB in Parkinson's Disease". International Journal of Molecular Sciences. 23 (8): 4453. doi:10.3390/ijms23084453. PMC 9028367. PMID 35457272. 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.
  4. ^ Duarte P, Cuadrado A, León R (2021). "Monoamine Oxidase Inhibitors: From Classic to New Clinical Approaches". Handbook of Experimental Pharmacology. 264: 229–259. doi:10.1007/164_2020_384. ISBN 978-3-030-68509-6. PMID 32852645. 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).
Allikas: http://en.wikipedia.org/wiki/Tisolagiline
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