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Synonyms: AM-111 | D-JNKI-1 | XG-102
Compound class:
Peptide or derivative
Comment: Brimapitide is a highly selective, non-competitive, long-acting inhibitor of c-jun N-terminal kinase (JNK). The peptide is an investigational drug for the intratympanic (i.t.) treatment of acute sensorineural hearing loss (ASNHL). Structurally the peptide consists of 20 amino acids from C-Jun-amino-terminal kinase-interacting protein 1 (JIP-1) fused to a carrier peptide derived from HIV-TAT48-57 (TAT) peptide PPRRRQRRKKRG. The peptide is constructed in a D-retro-inverso configuration to render it protease resistant. The TAT peptide mediates cell permeability. The sequence is claimed in patent US8080517 (SEQ ID NO: 11, D-JNKI1) [2]. The research codes XG-102 and AM-111 seem to be applied to this investigational agent.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| No information available. |
Summary of Clinical Use  |
| AM-111 has been granted orphan drug status in the European Union and the USA for the treatment of acute sensorineural hearing loss. Phase 2 clinical trial results for ths indication are published in [5]. A Phase 2I trial in patients with acute inner ear hearing loss is ongoing (NCT02561091). An additional Phase 2I trial (NCT02508337) evaluating Brimaptide's ability to reduce intraocular inflammation and pain following cataract surgery is also underway. |
| Mechanism Of Action and Pharmacodynamic Effects |
| Brimaptide is a cell-permeable peptide. It selectively prevents the protein-protein interaction between JNK and its targets, thereby blocking JNK MAPK mediated apoptosis of stress injured hair cells and neurons in the cochlea [1,3]. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT02508337 | Efficacy and Safety of XG-102 in Reduction of Post-cataract Surgery Intraocular Inflammation and Pain | Phase 3 Interventional | Xigen SA | ||
| NCT02561091 | AM-111 in the Treatment of Acute Inner Ear Hearing Loss | Phase 3 Interventional | Auris Medical, Inc. | ||
