Routes Of Administration: | Oral |
Class: | Lysine-specific demethylase 1 (LSD1) inhibitor; Monoamine oxidase B (MAO-B) inhibitor |
Cas Number: | 1357362-02-7 |
Pubchem: | 66714983 |
Drugbank: | DB16446 |
Chemspiderid: | 68019508 |
Unii: | LZ82JLT4UP |
Chembl: | 4802155 |
Synonyms: | ORY-2001; ORY2001 |
Iupac Name: | 5-(1R,2S)-2-(4-phenylmethoxyphenyl)cyclopropylamino]methyl]-1,3,4-oxadiazol-2-amine| C=19 | H=20 | N=4 | O=2| SMILES = C1[C@H]([C@@H]1NCC2=NN=C(O2)N)C3=CC=C(C=C3)OCC4=CC=CC=C4| StdInChI = 1S/C19H20N4O2/c20-19-23-22-18(25-19)11-21-17-10-16(17)14-6-8-15(9-7-14)24-12-13-4-2-1-3-5-13/h1-9,16-17,21H,10-12H2,(H2,20,23)/t16-,17+/m0/s1| StdInChIKey = XBBRLCXCBCZIOI-DLBZAZTESA-N}} Vafidemstat (; 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. The drug is taken by mouth. 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. Conversely, no recent development has been reported for autism, dementia, Huntington's disease, Parkinson's disease, and telomeric 22q13 monosomy syndrome. It is being developed by Oryzon. 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).[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] References] |