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Deramciclane came out of EGIS Pharmaceuticals in Hungary as a non-benzodiazepine anxiolytic working through 5-HT2A/2C receptors instead of GABA-A, and Orion Pharma partnered on it to run one of the largest clinical programs in Orion's 20-year research history. Early dose-finding data in generalized anxiety disorder actually looked encouraging; the 60 mg/day arm cleared the psychic-anxiety subscale of the HAM-A against placebo. That promise collapsed when the larger Phase III studies read out; Orion announced in 2003 that deramciclane simply lacked sufficient efficacy in GAD, closing out a program that had consumed years of investment on a hopeful mechanistic bet.
- significant improvement on the HAM-A psychic anxiety factor at 30 and 60 mg/day in the dose-finding study
- non-sedating, non-benzodiazepine mechanism with no muscle-relaxant effect
- headache was the most commonly reported adverse event across dose groups
- The deramciclane GAD program was described as one of the largest clinical trial efforts in Orion Pharma's 20-year research history at the time, which makes its 2003 discontinuation an especially costly one.
Mechanism
Inverse / at 5-HT2C receptors, with additional affinity; intended to relieve anxiety without the sedation, dependence, or muscle-relaxant effects of -A benzodiazepine anxiolytics.
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
Deramciclane is an investigational non-benzodiazepine anxiolytic (a 5-HT2A antagonist and 5-HT2C inverse agonist) that was well tolerated across clinical trials spanning roughly 0.2 to 150 mg, with all reported adverse events being mild-to-moderate and none severe. The most common side effects were headache, dizziness, tiredness, and generally transient events; notably, side effects were not found to be dose-dependent.
Trials showed no meaningful changes in liver enzymes, ECGs, blood pressure, or HDL/LDL cholesterol, and unlike benzodiazepines it produced no withdrawal effects after long-term dosing. The main caveat is that development was discontinued after it failed to beat placebo in Phase 3, so its human exposure is limited to trial settings and long-term real-world safety was never established. It is a weak CYP2D6 inhibitor, which flags a theoretical interaction consideration with drugs cleared by that enzyme.
History
Developed by EGIS Pharmaceuticals (Hungary) with Orion Pharma (Finland); a placebo-controlled, double-blind dose-finding study in GAD showed a positive signal at 60 mg/day. Orion discontinued the larger Phase III GAD program in 2003, citing lack of efficacy.
Subjective profileweighing the evidence above
A non-benzodiazepine anxiolytic that showed just enough early promise to justify a major trial program, then failed to hold up at scale.
Resources
This entry is here for reference.
Research
- 1.Deramciclane in the treatment of generalized anxiety disorder: a placebo-controlled, double-blind, dose-finding study
- 2.Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation
2 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
Why did Orion give up on deramciclane?
Despite promising Phase II dose-finding results in generalized anxiety disorder, the larger Phase III program failed to show sufficient efficacy, and Orion discontinued development in 2003.
How is deramciclane different from a benzodiazepine?
It works through serotonin 2A/2C receptors rather than GABA-A, so it was designed to avoid the sedation, muscle relaxation, and dependence risk associated with benzodiazepines.
Limitations of the evidence
- Phase III trials ultimately failed to confirm the efficacy suggested by earlier dose-finding data
Adverse effects
- headache was the most commonly reported adverse event across dose groups