Eplivanserin/volinanserin

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Eplivanserin/volinanserin
Eplivanserin structure.svg
Volinanserin.svg
Eplivanserin (top) and
volinanserin (bottom)
Combination of
Eplivanserin Serotonin 5-HT2A receptor antagonist
Volinanserin Serotonin 5-HT2A receptor antagonist
Clinical data
Other namesVolinanserin/eplivanserin
Drug class Serotonin 5-HT2A receptor antagonist
Pharmacokinetic data
Onset of action Volinanserin: 1–2.5 hours (Tmax Tooltip time to peak levels) [1]
Eplivanserin: 2–6 hours (Tmax Tooltip time to peak levels) [2]
Elimination half-life Volinanserin: 6.6 hours [3] [1]
Eplivanserin: 50 hours [2]

Eplivanserin/volinanserin is a combination of eplivanserin and volinanserin, both of which are selective serotonin 5-HT2A receptor antagonists, which is under development for the treatment of psychiatric and neurological disorders. [4] [5] One of its indications is to block the hallucinogenic effects of serotonergic psychedelics, for instance to abort psychedelic experiences early or to allow for take-home medications without hallucinations but with potentially retained therapeutic benefits. [5] [6] Its route of administration is unspecified. [4] The elimination half-life of volinanserin is 6.6 hours [3] [1] and of eplivanserin is 50 hours. [2] As of January 2024, eplivanserin/volinanserin has entered clinical trials for neurological and psychiatric disorders, but its exact clinical phase is unknown. [4]

Contents

See also

References

  1. 1 2 3 Gründer G, Yokoi F, Offord SJ, Ravert HT, Dannals RF, Salzmann JK, Szymanski S, Wilson PD, Howard DR, Wong DF (September 1997). "Time course of 5-HT2A receptor occupancy in the human brain after a single oral dose of the putative antipsychotic drug MDL 100,907 measured by positron emission tomography". Neuropsychopharmacology. 17 (3): 175–185. doi:10.1016/S0893-133X(97)00044-4. PMID   9272484.
  2. 1 2 3 "Method of treating sleep disorders using eplivanserin". Google Patents. 10 November 2009. Eplivanserin is well absorbed (>70%). Conventional dosage, between 1 and 10 mg, leads to a maximal plasma concentration that is reached between 2 and 6 hours; the half-life time of eplivanserin or pharmaceutically acceptable salts or esters thereof is relatively long, with an average value of 50 hours.
  3. 1 2 Teegarden BR, Al Shamma H, Xiong Y (2008). "5-HT(2A) inverse-agonists for the treatment of insomnia". Curr Top Med Chem. 8 (11): 969–976. doi:10.2174/156802608784936700. PMID   18673166. The plasma half-life for Volinanserin is ~6.6 hr and according to Gründer et al. [82] the receptor occupancy half-life greatly exceeds this.
  4. 1 2 3 "Eplivanserin/volinanserin". AdisInsight. 15 January 2024. Retrieved 15 January 2026.
  5. 1 2 Cornall, Jim (15 March 2024). "Reformulating psychedelics for neurodegenerative diseases". Labiotech.eu. Retrieved 15 January 2026. Eplivanserin and Volinanserin as hallucination blockers: Eplivanserin and Volinanserin are selective serotonin 2A receptor blockers [that] Terran Biosciences is using to remove hallucinations from psychedelics. This could lead to a take-home medication without the trip. Terran Biosciences is also using them as standalone compounds to end trips early in situations where a physician is giving psychedelic-assisted psychotherapy. "That's something we think will be needed by all psychedelic treatment centers in the future. Everyone is going to need a way to tailor the duration of their trips and to end bad trips. And with these compounds, we hope to provide that solution."
  6. ↑ "Sam Clark: Founder and CEO of Terran Biosciences". Buzzsprout. 31 October 2024. Retrieved 15 January 2026. So these scientists said, what would happen if we combine the psychedelic with a selective serotonin receptor blocker? And they did that, and they found that in animal models, it was able to remove the behavioral effects of the trip but maintain the therapeutic efficacy. So then we move that into a human study where we showed that psychedelic without the trip still maintain all of the functional changes on the brain measured with functional MRI. And so we had partnered with Sanofi, where we exclusively licensed their large neural programs, Eplivanserin and Volinanserin. These are two of the most selective serotonin 2a receptor antagonists known. They had already been tested in 15,000 patients over 100 clinical trials, we got the exclusive worldwide rights to develop those compounds. We're combining them with our psychedelics now and pushing those forward towards the clinic, where we hope to develop a take home psychedelic without the trip, where you can get the antidepressant or anti anxiety benefits without having to experience a trip. We're not anti tripitarian. It can absolutely benefit certain people, but we believe that without the trip, you have the potential to benefit all those extra people who can't afford the trip, or can't take the time for it, or scared by it, or don't want it, and really improve the market at lower costs so that we can democratize access for as many people as possible.
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