Emrusolmin

Emrusolmin
Clinical data
Other names	Anle138b, TEV-56286
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name 5-(1,3-benzodioxol-5-yl)-3-(3-bromophenyl)-1H-pyrazole;
CAS Number	882697-00-9;
PubChem CID	44608289;
DrugBank	DB13927;
UNII	E7WRA77JET;
KEGG	D80685;
ChEBI	CHEBI:232606;
ChEMBL	ChEMBL4748063;
Chemical and physical data
Formula	C16H11BrN2O2
Molar mass	343.180 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1OC2=C(O1)C=C(C=C2)C3=CC(=NN3)C4=CC(=CC=C4)Br;
	InChI InChI=InChI=1S/C16H11BrN2O2/c17-12-3-1-2-10(6-12)13-8-14(19-18-13)11-4-5-15-16(7-11)21-9-20-15/h1-8H,9H2,(H,18,19); Key:RCQIIBJSUWYYFU-UHFFFAOYSA-N;

Emrusolmin (development code Anle138b) is an experimental drug for the treatment of neurodegenerative diseases. It is an inhibitor of protein aggregation, particularly preventing the aggregation of α-synuclein which is implicated in the development of Parkinson's disease.^[1]^[2]^[3] Other proteins it inhibits the aggregation of include tau^[4] which is associated with Alzheimer's disease (AD) and tauopathy, and amyloid beta^[5] which is associated with AD.

It is currently in clinical trials for Parkinson's disease and multiple system atrophy.^[6]

References

^ Wagner J, Ryazanov S, Leonov A, Levin J, Shi S, Schmidt F, et al. (2013). "Anle138b: A novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease". Acta Neuropathologica. 125 (6): 795–813. doi:10.1007/s00401-013-1114-9. PMC 3661926. PMID 23604588.
^ Dervişoğlu R, Antonschmidt L, Nimerovsky E, Sant V, Kim M, Ryazanov S, et al. (2023). "Anle138b interaction in α-synuclein aggregates by dynamic nuclear polarization NMR". Methods. 214: 18–27. doi:10.1016/j.ymeth.2023.04.002. PMID 37037308.
^ Antonschmidt L, Matthes D, DervişOğLu R, Frieg B, Dienemann C, Leonov A, et al. (2022). "The clinical drug candidate anle138b binds in a cavity of lipidic α-synuclein fibrils". Nature Communications. 13 (1): 5385. doi:10.1038/s41467-022-32797-w. PMC 9474542. PMID 36104315.
^ Wagner J, Krauss S, Shi S, Ryazanov S, Steffen J, Miklitz C, et al. (2015). "Reducing tau aggregates with anle138b delays disease progression in a mouse model of tauopathies". Acta Neuropathologica. 130 (5): 619–631. doi:10.1007/s00401-015-1483-3. PMC 4612332. PMID 26439832.
^ Martinez Hernandez A, Urbanke H, Gillman AL, Lee J, Ryazanov S, Agbemenyah HY, et al. (2018). "The diphenylpyrazole compound anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology". EMBO Molecular Medicine. 10: 32–47. doi:10.15252/emmm.201707825. PMID 29208638.
^ "Emrusolmin - Modag". AdisInsight. Springer Nature Switzerland AG.

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[1] Wagner J, Ryazanov S, Leonov A, Levin J, Shi S, Schmidt F, et al. (2013). "Anle138b: A novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease". Acta Neuropathologica. 125 (6): 795–813. doi:10.1007/s00401-013-1114-9. PMC 3661926. PMID 23604588.

[2] Dervişoğlu R, Antonschmidt L, Nimerovsky E, Sant V, Kim M, Ryazanov S, et al. (2023). "Anle138b interaction in α-synuclein aggregates by dynamic nuclear polarization NMR". Methods. 214: 18–27. doi:10.1016/j.ymeth.2023.04.002. PMID 37037308.

[3] Antonschmidt L, Matthes D, DervişOğLu R, Frieg B, Dienemann C, Leonov A, et al. (2022). "The clinical drug candidate anle138b binds in a cavity of lipidic α-synuclein fibrils". Nature Communications. 13 (1): 5385. doi:10.1038/s41467-022-32797-w. PMC 9474542. PMID 36104315.

[4] Wagner J, Krauss S, Shi S, Ryazanov S, Steffen J, Miklitz C, et al. (2015). "Reducing tau aggregates with anle138b delays disease progression in a mouse model of tauopathies". Acta Neuropathologica. 130 (5): 619–631. doi:10.1007/s00401-015-1483-3. PMC 4612332. PMID 26439832.

[5] Martinez Hernandez A, Urbanke H, Gillman AL, Lee J, Ryazanov S, Agbemenyah HY, et al. (2018). "The diphenylpyrazole compound anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology". EMBO Molecular Medicine. 10: 32–47. doi:10.15252/emmm.201707825. PMID 29208638.

[6] "Emrusolmin - Modag". AdisInsight. Springer Nature Switzerland AG.

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