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| {{cs1 config|name-list-style=vanc|display-authors=6}} | |||
| {{Infobox drug | {{Infobox drug | ||
| | drug_name = | | drug_name = | ||
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| | type = <!-- empty --> | | type = <!-- empty --> | ||
| | image = Emrusolmin.svg | | image = Emrusolmin.svg | ||
| | |
| width = 200px | ||
| ⚫ | | alt = | ||
| | caption = | | caption = | ||
| | image2 = | |||
| | width2 = | |||
| | alt2 = | |||
| | caption2 = | |||
| | imageL = | |||
| | widthL = | |||
| | altL = | |||
| | imageR = | |||
| | widthR = | |||
| | altR = | |||
| | captionLR = | |||
| <!-- Clinical data --> | <!-- Clinical data --> | ||
| | pronounce = | | pronounce = | ||
| Line 11: | Line 26: | ||
| | Drugs.com = | | Drugs.com = | ||
| | MedlinePlus = | | MedlinePlus = | ||
| | licence_CA = | |||
| | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> | |||
| | licence_EU = | |||
| | DailyMedID = | |||
| | licence_US = | |||
| | pregnancy_AU = | |||
| | pregnancy_AU_comment = | | pregnancy_AU_comment = | ||
| | pregnancy_category= | | pregnancy_category= | ||
| | dependency_liability = | |||
| | addiction_liability = | |||
| | routes_of_administration = | | routes_of_administration = | ||
| | class = | |||
| <!-- Legal status --> | |||
| | ATCvet = | | ATCvet = | ||
| | ATC_prefix = <!-- 'none' if uncategorised --> | | ATC_prefix = <!-- 'none' if uncategorised --> | ||
| Line 38: | Line 62: | ||
| | legal_UN_comment = | | legal_UN_comment = | ||
| | legal_status = Investigational | | legal_status = Investigational | ||
| <!-- Pharmacokinetic data --> | <!-- Pharmacokinetic data --> | ||
| | bioavailability = | | bioavailability = | ||
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| | duration_of_action= | | duration_of_action= | ||
| | excretion = | | excretion = | ||
| <!-- Identifiers --> | <!-- Identifiers --> | ||
| | |
| CAS_number = 882697-00-9 | ||
| | CAS_supplemental = | |||
| | CAS_number = 882697-00-9 | |||
| | PubChem = 44608289 | | PubChem = 44608289 | ||
| | PubChemSubstance = | |||
| ⚫ | | |
||
| | IUPHAR_ligand = | |||
| | DrugBank = DB13927 | | DrugBank = DB13927 | ||
| | ChemSpiderID = | |||
| | UNII = E7WRA77JET | |||
| | KEGG = D80685 | |||
| | ChEBI = 232606 | |||
| | ChEMBL = 4748063 | |||
| | NIAID_ChemDB = | |||
| | PDB_ligand = | |||
| | synonyms = Anle138b, TEV-56286 | |||
| <!-- Chemical and physical data --> | <!-- Chemical and physical data --> | ||
| | IUPAC_name = 5-(1,3- |
| IUPAC_name = <nowiki>5-(1,3-benzodioxol-5-yl)-3-(3-bromophenyl)-1H-pyrazole</nowiki> | ||
| | C |
| C=16 | H=11 | Br=1 | N=2 | O=2 | ||
| | molecular_weight = | |||
| | |
| SMILES = C1OC2=C(O1)C=C(C=C2)C3=CC(=NN3)C4=CC(=CC=C4)Br | ||
| | Jmol = | |||
| | StdInChI = 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) | |||
| | StdInChI_comment = | |||
| | StdInChIKey = RCQIIBJSUWYYFU-UHFFFAOYSA-N | |||
| | density = | |||
| | density_notes = | |||
| | melting_point = | |||
| | melting_high = | |||
| | melting_notes = | |||
| | boiling_point = | |||
| | boiling_notes = | |||
| | solubility = | |||
| | sol_units = | |||
| | specific_rotation = | |||
| }} | }} | ||
| '''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 ] which is implicated in the development of ].<ref>{{cite journal | doi = 10.1007/s00401-013-1114-9 | title = Anle138b: A novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease | date = 2013 | last1 = Wagner | first1 = Jens | last2 = Ryazanov | first2 = Sergey | last3 = Leonov | first3 = Andrei | last4 = Levin | first4 = Johannes | last5 = Shi | first5 = Song | last6 = Schmidt | first6 = Felix | last7 = Prix | first7 = Catharina | last8 = Pan-Montojo | first8 = Francisco | last9 = Bertsch | first9 = Uwe | last10 = Mitteregger-Kretzschmar | first10 = Gerda | last11 = Geissen | first11 = Markus | last12 = Eiden | first12 = Martin | last13 = Leidel | first13 = Fabienne | last14 = Hirschberger | first14 = Thomas | last15 = Deeg | first15 = Andreas A. | last16 = Krauth | first16 = Julian J. | last17 = Zinth | first17 = Wolfgang | last18 = Tavan | first18 = Paul | last19 = Pilger | first19 = Jens | last20 = Zweckstetter | first20 = Markus | last21 = Frank | first21 = Tobias | last22 = Bähr | first22 = Mathias | last23 = Weishaupt | first23 = Jochen H. | last24 = Uhr | first24 = Manfred | last25 = Urlaub | first25 = Henning | last26 = Teichmann | first26 = Ulrike | last27 = Samwer | first27 = Matthias | last28 = Bötzel | first28 = Kai | last29 = Groschup | first29 = Martin | last30 = Kretzschmar | first30 = Hans | journal = Acta Neuropathologica | volume = 125 | issue = 6 | pages = 795–813 | pmid = 23604588 | pmc = 3661926 |
'''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 ] which is implicated in the development of ].<ref>{{cite journal | doi = 10.1007/s00401-013-1114-9 | title = Anle138b: A novel oligomer modulator for disease-modifying therapy of neurodegenerative diseases such as prion and Parkinson's disease | date = 2013 | last1 = Wagner | first1 = Jens | last2 = Ryazanov | first2 = Sergey | last3 = Leonov | first3 = Andrei | last4 = Levin | first4 = Johannes | last5 = Shi | first5 = Song | last6 = Schmidt | first6 = Felix | last7 = Prix | first7 = Catharina | last8 = Pan-Montojo | first8 = Francisco | last9 = Bertsch | first9 = Uwe | last10 = Mitteregger-Kretzschmar | first10 = Gerda | last11 = Geissen | first11 = Markus | last12 = Eiden | first12 = Martin | last13 = Leidel | first13 = Fabienne | last14 = Hirschberger | first14 = Thomas | last15 = Deeg | first15 = Andreas A. | last16 = Krauth | first16 = Julian J. | last17 = Zinth | first17 = Wolfgang | last18 = Tavan | first18 = Paul | last19 = Pilger | first19 = Jens | last20 = Zweckstetter | first20 = Markus | last21 = Frank | first21 = Tobias | last22 = Bähr | first22 = Mathias | last23 = Weishaupt | first23 = Jochen H. | last24 = Uhr | first24 = Manfred | last25 = Urlaub | first25 = Henning | last26 = Teichmann | first26 = Ulrike | last27 = Samwer | first27 = Matthias | last28 = Bötzel | first28 = Kai | last29 = Groschup | first29 = Martin | last30 = Kretzschmar | first30 = Hans | journal = Acta Neuropathologica | volume = 125 | issue = 6 | pages = 795–813 | pmid = 23604588 | pmc = 3661926 }}</ref><ref>{{cite journal | doi = 10.1016/j.ymeth.2023.04.002 | title = Anle138b interaction in α-synuclein aggregates by dynamic nuclear polarization NMR | date = 2023 | last1 = Dervişoğlu | first1 = Rıza | last2 = Antonschmidt | first2 = Leif | last3 = Nimerovsky | first3 = Evgeny | last4 = Sant | first4 = Vrinda | last5 = Kim | first5 = Myeongkyu | last6 = Ryazanov | first6 = Sergey | last7 = Leonov | first7 = Andrei | last8 = Fuentes-Monteverde | first8 = Juan Carlos | last9 = Wegstroth | first9 = Melanie | last10 = Giller | first10 = Karin | last11 = Mathies | first11 = Guinevere | last12 = Giese | first12 = Armin | last13 = Becker | first13 = Stefan | last14 = Griesinger | first14 = Christian | last15 = Andreas | first15 = Loren B. | journal = Methods | volume = 214 | pages = 18–27 | pmid = 37037308 }}</ref><ref>{{cite journal | doi = 10.1038/s41467-022-32797-w | title = The clinical drug candidate anle138b binds in a cavity of lipidic α-synuclein fibrils | date = 2022 | last1 = Antonschmidt | first1 = Leif | last2 = Matthes | first2 = Dirk | last3 = DervişOğLu | first3 = Rıza | last4 = Frieg | first4 = Benedikt | last5 = Dienemann | first5 = Christian | last6 = Leonov | first6 = Andrei | last7 = Nimerovsky | first7 = Evgeny | last8 = Sant | first8 = Vrinda | last9 = Ryazanov | first9 = Sergey | last10 = Giese | first10 = Armin | last11 = Schröder | first11 = Gunnar F. | last12 = Becker | first12 = Stefan | last13 = De Groot | first13 = Bert L. | last14 = Griesinger | first14 = Christian | last15 = Andreas | first15 = Loren B. | journal = Nature Communications | volume = 13 | issue = 1 | page = 5385 | pmid = 36104315 | pmc = 9474542 }}</ref> Other proteins it inhibits the aggregation of include ]<ref>{{cite journal | doi = 10.1007/s00401-015-1483-3 | title = Reducing tau aggregates with anle138b delays disease progression in a mouse model of tauopathies | date = 2015 | last1 = Wagner | first1 = Jens | last2 = Krauss | first2 = Sybille | last3 = Shi | first3 = Song | last4 = Ryazanov | first4 = Sergey | last5 = Steffen | first5 = Julia | last6 = Miklitz | first6 = Carolin | last7 = Leonov | first7 = Andrei | last8 = Kleinknecht | first8 = Alexander | last9 = Göricke | first9 = Bettina | last10 = Weishaupt | first10 = Jochen H. | last11 = Weckbecker | first11 = Daniel | last12 = Reiner | first12 = Anne M. | last13 = Zinth | first13 = Wolfgang | last14 = Levin | first14 = Johannes | last15 = Ehninger | first15 = Dan | last16 = Remy | first16 = Stefan | last17 = Kretzschmar | first17 = Hans A. | last18 = Griesinger | first18 = Christian | last19 = Giese | first19 = Armin | last20 = Fuhrmann | first20 = Martin | journal = Acta Neuropathologica | volume = 130 | issue = 5 | pages = 619–631 | pmid = 26439832 | pmc = 4612332 }}</ref> which is associated with ] (AD) and ], and ]<ref>{{cite journal | doi = 10.15252/emmm.201707825 | title = The diphenylpyrazole compound anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology | date = 2018 | last1 = Martinez Hernandez | first1 = Ana | last2 = Urbanke | first2 = Hendrik | last3 = Gillman | first3 = Alan L. | last4 = Lee | first4 = Joon | last5 = Ryazanov | first5 = Sergey | last6 = Agbemenyah | first6 = Hope Y. | last7 = Benito | first7 = Eva | last8 = Jain | first8 = Gaurav | last9 = Kaurani | first9 = Lalit | last10 = Grigorian | first10 = Gayane | last11 = Leonov | first11 = Andrei | last12 = Rezaei-Ghaleh | first12 = Nasrollah | last13 = Wilken | first13 = Petra | last14 = Arce | first14 = Fernando Teran | last15 = Wagner | first15 = Jens | last16 = Fuhrman | first16 = Martin | last17 = Caruana | first17 = Mario | last18 = Camilleri | first18 = Angelique | last19 = Vassallo | first19 = Neville | last20 = Zweckstetter | first20 = Markus | last21 = Benz | first21 = Roland | last22 = Giese | first22 = Armin | last23 = Schneider | first23 = Anja | last24 = Korte | first24 = Martin | last25 = Lal | first25 = Ratnesh | last26 = Griesinger | first26 = Christian | last27 = Eichele | first27 = Gregor | last28 = Fischer | first28 = Andre | journal = EMBO Molecular Medicine | volume = 10 | pages = 32–47 | pmid = 29208638 }}</ref> which is associated with AD. | ||
| It is currently in clinical trials for Parkinson's disease and ].<ref>{{cite web | url = https://adisinsight.springer.com/drugs/800046788 | title = Emrusolmin - Modag | publisher = AdisInsight }}</ref> | It is currently in clinical trials for Parkinson's disease and ].<ref>{{cite web | url = https://adisinsight.springer.com/drugs/800046788 | title = Emrusolmin - Modag | publisher = AdisInsight }}</ref> | ||
Revision as of 19:10, 24 December 2024
Pharmaceutical compound
 | |
| Clinical data | |
|---|---|
| Other names | Anle138b, TEV-56286 |
| Legal status | |
| Legal status |
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| Identifiers | |
IUPAC name
| |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C16H11BrN2O2 |
| Molar mass | 343.180 g·mol |
| 3D model (JSmol) | |
SMILES
| |
InChI
| |
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. Other proteins it inhibits the aggregation of include tau which is associated with Alzheimer's disease (AD) and tauopathy, and amyloid beta which is associated with AD.
It is currently in clinical trials for Parkinson's disease and multiple system atrophy.
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.
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