Tisolagiline

Tisolagiline
Clinical data
Other names	KDS-2010; KDS2010; SeReMABI
Drug class	Reversible monoamine oxidase B (MAO-B) inhibitor
Identifiers
	IUPAC name (2S)-2-[[4-[4-(trifluoromethyl)phenyl]phenyl]methylamino]propanamide;
CAS Number	1894207-44-3 ;
PubChem CID	132023446 ;
ChemSpider	128942408 ;
UNII	PCH79KLX33 ;
ChEMBL	ChEMBL5314546 ;
Chemical and physical data
Formula	C17H17F3N2O
Molar mass	322.331 g·mol−1
3D model (JSmol)	Interactive image ;
	SMILES C[C@@H](C(=O)N)NCC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F;
	InChI InChI=1S/C17H17F3N2O/c1-11(16(21)23)22-10-12-2-4-13(5-3-12)14-6-8-15(9-7-14)17(18,19)20/h2-9,11,22H,10H2,1H3,(H2,21,23)/t11-/m0/s1; Key:XCUXYNYVUMLDKH-NSHDSACASA-N;

Last updated February 24, 2025

Tisolagiline (INN Tooltip 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 2 3 4 "KDS 2010". AdisInsight. 6 February 2025. Retrieved 24 February 2025.
1 2 3 "Delving into the Latest Updates on KDS-2010 with Synapse". Synapse. 23 January 2025. Retrieved 24 February 2025.
↑ 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.
↑ 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).

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[AdisInsight-1] 1 2 3 4 "KDS 2010". AdisInsight. 6 February 2025. Retrieved 24 February 2025.

[Synapse-2] 1 2 3 "Delving into the Latest Updates on KDS-2010 with Synapse". Synapse. 23 January 2025. Retrieved 24 February 2025.

[NamSaJu2022-3] 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.

[DuarteCuadradoLeón2021-4] 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).

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