Fasedienol Explained

Fasedienol (; 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 (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 = 200nM).

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. 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. 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.

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Notes and References

  1. Web site: 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). VistaGen Therapeutics, Inc.. en. 2019-12-19. 2019-12-19. https://web.archive.org/web/20191219174743/https://www.vistagen.com/news-media/press-releases/detail/96/vistagen-therapeutics-acquires-worldwide-license-of-phase. dead.
  2. Web site: Al Idrus A . 13 September 2018 . VistaGen nabs phase 3-ready social anxiety drug from Pherin. FierceBiotech. en. 2019-12-19.
  3. Web site: Murphy J . 10 December 2019 . FDA Grants Fast Track Designation to PH94B for Treatment of Social Anxiety Disorder. Pharmacy Times. 2019-12-19.
  4. Griebel G, Holmes A . 50 years of hurdles and hope in anxiolytic drug discovery . Nature Reviews. Drug Discovery . 12 . 9 . 667–87 . September 2013 . 23989795 . 4176700 . 10.1038/nrd4075 .
  5. Monti-Bloch L, Jennings-White C, Dolberg DS, Berliner DL . 36129626 . The human vomeronasal system . Psychoneuroendocrinology . 19 . 5–7 . 673–86 . 1994 . 7938363 . 10.1016/0306-4530(94)90049-3 .
  6. Book: Rolls, Edmund T. . vanc . Emotion and Decision Making Explained. November 2013. Oxford University Press. 978-0-19-965989-0. 356–.
  7. Book: BioScan. 2009. Oryx Press.
  8. Liebowitz MR, Salman E, Nicolini H, Rosenthal N, Hanover R, Monti L . 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 . 24700254 . 10.1176/appi.ajp.2014.12101342 . 38510058 .
  9. US . 8722652 . patent . Acute Treatment of Social Phobia . 13 November 2012 . 9 September 2005 . 9 September 2005 . Louis Monti-Bloch . Pherin Pharmaceuticals, Inc..
  10. Web site: Generalized Anxiety Disorder :: VistaGen Therapeutics, Inc. (VTGN). VistaGen Therapeutics, Inc.. en. 2019-12-19. 2019-12-19. https://web.archive.org/web/20191219174741/https://www.vistagen.com/pipeline/ph94b/generalized-anxiety-disorder. dead.
  11. Web site: Post-traumatic Stress Disorder :: VistaGen Therapeutics, Inc. (VTGN). VistaGen Therapeutics, Inc.. en. 2019-12-19.
  12. Web site: 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). VistaGen Therapeutics, Inc.. en. 2019-12-19. 2019-12-19. https://web.archive.org/web/20191219174742/https://www.vistagen.com/news-media/press-releases/detail/117/positive-pilot-phase-3-data-position-vistagens-ph94b. dead.
  13. Kaminski RM, Marini H, Ortinski PI, Vicini S, Rogawski MA . 95393004 . 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 . 16415088 . 10.1124/jpet.105.098319 .

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