Ocaperidone
dopaminergic · positive symptoms (d2/5-ht2 dual antagonism, preclinical/early data) class / dopaminergicdata + articles · 1 listed
newest 1992spec sheet6 rows
Ocaperidone was a Janssen Pharmaceutica benzisoxazole compound from the same chemical family that produced risperidone, sharing its dual dopamine D2 and serotonin 5-HT2 antagonism but pushed to a far higher level of receptor potency. Janssen's own pharmacology described it as expected to deliver haloperidol-level control of positive symptoms while keeping the lower extrapyramidal side-effect burden and improved tolerability associated with risperidone-style balanced D2/5-HT2 blockade. It never became a marketed drug; risperidone (and later Janssen's own paliperidone) filled that commercial niche, and ocaperidone's rights eventually passed to Neuro3D and then to Evotec after a series of licensing moves in the 2000s, with no clinical program ever reaching the public record beyond early pharmacological characterization.
- very high receptor potency at both D2 and 5-HT2 targets in preclinical characterization
- shared the balanced D2/5-HT2 antagonism mechanism credited with risperidone's improved side-effect profile over first-generation antipsychotics
- expected haloperidol-level control of positive symptoms per Janssen's own pharmacology profile
- Ocaperidone's development rights changed hands twice after Janssen, first to Neuro3D and then to Evotec in 2007, yet no clinical trial results for it have ever been published.
Mechanism
Potent dual at receptors and 5-HT2 receptors, structurally related to risperidone within the benzisoxazole antipsychotic class.
Safetyrisks and cautions, not medical advice
Extrapyramidal side effects are the reported reason this one stopped, and the irony is thick: the whole preclinical case for ocaperidone was that its separation between antipsychotic action and catalepsy matched risperidone's, which was supposed to mean fewer movement problems rather than more. Drug pipeline databases record Phase II testing abandoned around 2010 because the movement side effects were unacceptable at doses that controlled symptoms. That account has never appeared in a peer-reviewed paper and no figures of any kind were released, so the direction of the finding is far clearer than its size.
History
Developed by Janssen Pharmaceutica in the early 1990s; characterized pharmacologically as a highly potent D2/5-HT2 antagonist but never marketed, with rights later licensed to Neuro3D and then acquired by Evotec in 2007; no clinical development beyond early-stage work is publicly documented.
Subjective profileweighing the evidence above
A potent risperidone cousin that got out-competed by its own sibling compounds before it ever reached the clinic in any documented way.
Resources
This entry is here for reference.
Research
1 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
Is ocaperidone related to risperidone?
Yes, both are benzisoxazole compounds developed by Janssen sharing the same dual dopamine D2 and serotonin 5-HT2 antagonist mechanism; risperidone made it to market and ocaperidone did not.
Why did ocaperidone never get marketed?
No official reason was ever published. It was likely overtaken commercially by risperidone and paliperidone from the same research program, which offered Janssen a cleaner and better-documented path to market.
Limitations of the evidence
- no published human efficacy or safety data exists
Notes and cautions
- commercially overtaken by risperidone and paliperidone from the same chemical lineage
- development history after licensing to Neuro3D/Evotec is not publicly documented