Chemistry:Fasedienol

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Fasedienol (INN; developmental code names PH94B and Aloradine), also known as 4-androstadienol or as 4,16-androstadien-3β-ol, is a pherine which is under development by VistaGen Therapeutics[1][2] in a nasal spray formulation used as needed(PRN) for the acute treatment of social anxiety disorder.[3][4][5][6][7][8][9] It is also being investigated by VistaGen Therapeutics for the treatment of generalized anxiety disorder (GAD) and post-traumatic stress disorder (PTSD).[10][11] The pherine is a positional isomer of the endogenous pheromone androstadienol (5-androstadienol or 5,16-androstadien-3β-ol). As of 2020, it is in phase III clinical trials for social anxiety disorder.[12]

Fasedienol lacks affinity for steroid hormone receptors and has instead been found to directly activate isolated human vomeronasal receptor cells at nanomolar concentrations (EC50 = 200 nM).[8]

The closely related pheromone androstenol (5α-androst-16-en-3α-ol) has been found to act as a potent positive allosteric modulator of the GABAA receptor, and it has been proposed that this action may mediate its pheromone effects.[13] It produces anxiolytic-like effects in animals.[13] Androstadienol, androstadienone, and androstenone, all of which are also pheromones, have been found to be converted into androstenol, and as such, it may be responsible for their pheromone effects.[13] As fasedienol is very closely related structurally to androstadienol, it might be converted into androstenol similarly and hence potentiation of the GABAA receptor could contribute to its mechanism of action.[13]

Fasedienol failed to show effectiveness in phase 3 clinical trials.[14][15]

See also

References

  1. ↑ "VistaGen Therapeutics Acquires Worldwide License of Phase 3-Ready CNS Drug Candidate from Pherin Pharmaceuticals for As-Needed Treatment of Social Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/news-media/press-releases/detail/96/vistagen-therapeutics-acquires-worldwide-license-of-phase. 
  2. ↑ "VistaGen nabs phase 3-ready social anxiety drug from Pherin" (in en). 13 September 2018. https://www.fiercebiotech.com/biotech/vistagen-nabs-phase-3-ready-social-anxiety-med-from-pherin. 
  3. ↑ "FDA Grants Fast Track Designation to PH94B for Treatment of Social Anxiety Disorder". 10 December 2019. https://www.pharmacytimes.com/news/fda-grants-fast-track-designation-for-ph94b-for-treatment-of-social-anxiety-disorder. 
  4. ↑ "50 years of hurdles and hope in anxiolytic drug discovery". Nature Reviews. Drug Discovery 12 (9): 667–87. September 2013. doi:10.1038/nrd4075. PMID 23989795. PMC 4176700. http://ggriebel.chez-alice.fr/Pub127.pdf. 
  5. ↑ "The human vomeronasal system". Psychoneuroendocrinology 19 (5–7): 673–86. 1994. doi:10.1016/0306-4530(94)90049-3. PMID 7938363. 
  6. ↑ Rolls, Edmund T. (November 2013). Emotion and Decision Making Explained. Oxford University Press. pp. 356–. ISBN 978-0-19-965989-0. https://books.google.com/books?id=fZWcAQAAQBAJ&pg=PA356. 
  7. ↑ BioScan. Oryx Press. 2009. https://books.google.com/books?id=L_5PAQAAIAAJ. 
  8. ↑ 8.0 8.1 "Effect of an acute intranasal aerosol dose of PH94B on social and performance anxiety in women with social anxiety disorder". The American Journal of Psychiatry 171 (6): 675–82. June 2014. doi:10.1176/appi.ajp.2014.12101342. PMID 24700254. https://www.researchgate.net/publication/261511611. 
  9. ↑ "Acute Treatment of Social Phobia" US patent 8722652, published 13 November 2012, assigned to Pherin Pharmaceuticals, Inc.
  10. ↑ "Generalized Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/pipeline/ph94b/generalized-anxiety-disorder. 
  11. ↑ "Post-traumatic Stress Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/pipeline/ph94b/post-traumatic-stress-disorder. 
  12. ↑ "Positive Pilot Phase 3 Data Position VistaGen's PH94B Neuroactive Nasal Spray for Pivotal Phase 3 Development as a Novel, As-Needed Treatment for Social Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN)" (in en). https://www.vistagen.com/news-media/press-releases/detail/117/positive-pilot-phase-3-data-position-vistagens-ph94b. 
  13. ↑ 13.0 13.1 13.2 13.3 "The pheromone androstenol (5 alpha-androst-16-en-3 alpha-ol) is a neurosteroid positive modulator of GABAA receptors". The Journal of Pharmacology and Experimental Therapeutics 317 (2): 694–703. May 2006. doi:10.1124/jpet.105.098319. PMID 16415088. 
  14. ↑ Walters, Jessica (23 December 2025). "Fasedienol for Social Anxiety Disorder Does Not Demonstrate Significant Improvement in Phase 3 Study". https://www.psychiatrictimes.com/view/fasedienol-for-social-anxiety-disorder-does-not-demonstrate-significant-improvement-in-phase-3-study. 
  15. ↑ Kansteiner, Fraiser (17 December 2025). "Vistagen phase 3 study sees placebo surprise, putting future of social anxiety asset into question: analyst". https://www.fiercebiotech.com/biotech/vistagens-ph3-flop-puts-future-fasedienol-social-anxiety-question-william-blair. 



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