Vafidemstat

Last updated

Vafidemstat
Vafidemstat.svg
Clinical data
Other namesORY-2001; ORY2001
Routes of
administration 		Oral [1] [2]
Drug class Lysine-specific demethylase 1 (LSD1) inhibitor; Monoamine oxidase B (MAO-B) inhibitor [1]
Identifiers
  • 5-[[[(1R,2S)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,3,4-oxadiazol-2-amine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C19H20N4O2
Molar mass 336.395 g·mol−1
3D model (JSmol)
  • C1[C@H]([C@@H]1NCC2=NN=C(O2)N)C3=CC=C(C=C3)OCC4=CC=CC=C4
  • InChI=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
  • Key:XBBRLCXCBCZIOI-DLBZAZTESA-N

Vafidemstat (INN Tooltip International Nonproprietary Name; 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] [3] [2] 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] [3]

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). [2] [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

References

  1. 1 2 3 4 5 6 7 8 "Vafidemstat - Oryzon Genomics". AdisInsight. 9 October 2024. Retrieved 6 November 2024.
  2. 1 2 3 Noce B, Di Bello E, Fioravanti R, Mai A (2023). "LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials". Front Pharmacol. 14 1120911. doi: 10.3389/fphar.2023.1120911 . PMC   9932783 . PMID   36817147.
  3. 1 2 "Delving into the Latest Updates on Vafidemstat with Synapse". Synapse. 1 November 2024. Retrieved 6 November 2024.
  4. ↑ Johnson JD, Alejo S, Jayamohan S, Sareddy GR (2023). "Lysine-specific demethylase 1 as a therapeutic cancer target: observations from preclinical study". Expert Opin Ther Targets. 27 (12): 1177–1188. doi:10.1080/14728222.2023.2288277. PMC   10872912 . PMID   37997756.
  5. ↑ 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.
  6. ↑ "Delving into the Latest Updates on Zavondemstat with Synapse". Synapse. 1 November 2024. Retrieved 6 November 2024.
  7. ↑ World Health Organization (2024). "Use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances, 2024" (PDF). World Health Organization. p. 184. Retrieved 21 October 2024. -stat- or enzyme inhibitors -stat [...] -demstat lysine-specific histone demethylase inhibitors (a) bomedemstat (122), iadademstat (119), pulrodemstat (124), seclidemstat (118), vafidemstat (119), zavondemstat (128)
  8. ↑ "Vafidemstat". PubChem. Retrieved 7 November 2024.
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