Chemistry:Vafidemstat
Vafidemstat (INN; developmental code name ORY-2001) is a dual inhibitor of the enzymes lysine-specific demethylase 1 (LSD1; KDM1A) and monoamine oxidase B (MAO-B) which is under development for the treatment of a variety of medical conditions, including aggression, Alzheimer's disease, borderline personality disorder, multiple sclerosis, acute respiratory disease in COVID-19 infection, and schizophrenia.[1][2][3] It is or was also being developed for several other indications, but no recent development has been reported for these uses.[1] The drug is taken by mouth.[1]
As of October 2024, vafidemstat is in phase 2 clinical trials for aggression, Alzheimer's disease, borderline personality disorder, multiple sclerosis, COVID-19 acute respiratory disease, and schizophrenia.[1] Conversely, no recent development has been reported for autism, dementia, Huntington's disease, Parkinson's disease, and telomeric 22q13 monosomy syndrome.[1] It is being developed by Oryzon.[1][2]
Other LSD1 inhibitors that are under development for medical use include bomedemstat (IMG-7289), iadademstat (ORY-1001), phenelzine (Nardil), pulrodemstat (CC-90011), seclidemstat (SP-2577), and tranylcypromine (Parnate).[3][4] Another drug, zavondemstat (QC8222, TACH101), is a pan-inhibitor of lysine-specific demethylase 4 (LSD4; KDM4).[5][6][7] Vafidemstat contains the chemical structure of (1S,2R)-tranylcypromine within its own structure.[8]
See also
- List of investigational aggression drugs
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 "Vafidemstat - Oryzon Genomics". 9 October 2024. https://adisinsight.springer.com/drugs/800045069.
- ↑ 2.0 2.1 "Delving into the Latest Updates on Vafidemstat with Synapse". 1 November 2024. https://synapse.patsnap.com/drug/d1efe73e113c423ab01f4f69ebc37cc3.
- ↑ 3.0 3.1 "LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials". Front Pharmacol 14. 2023. doi:10.3389/fphar.2023.1120911. PMID 36817147.
- ↑ "Lysine-specific demethylase 1 as a therapeutic cancer target: observations from preclinical study". Expert Opin Ther Targets 27 (12): 1177–1188. 2023. doi:10.1080/14728222.2023.2288277. PMID 37997756.
- ↑ Chandhasin, C., Perabo, F., Dai, Y., DiMascio, L., Mehta, R. K., Hassan, M. K., & Nyati, M. K. (2024). 245 (PB233): Histone methylation changes of H3K9 and H3K36 in PBMCs as pharmacodynamic biomarkers for Zavondemstat (TACH101), a paninhibitor of KDM4 histone lysine demethylase. European Journal of Cancer, 211, 114763.
- ↑ "Delving into the Latest Updates on Zavondemstat with Synapse". 1 November 2024. https://synapse.patsnap.com/drug/4a42923b95bf4d3e974dc927c3557e63.
- ↑ "Use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances, 2024". World Health Organization. 2024. p. 184. https://iris.who.int/bitstream/handle/10665/379226/9789240099388-eng.pdf#page=190. "-stat- or enzyme inhibitors -stat [...] -demstat lysine-specific histone demethylase inhibitors (a) bomedemstat (122), iadademstat (119), pulrodemstat (124), seclidemstat (118), vafidemstat (119), zavondemstat (128)"
- ↑ "Vafidemstat". https://pubchem.ncbi.nlm.nih.gov/compound/66714983.
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