Ulotaront

Also called SEP-363856

Acts on TAAR1, a receptor that regulates dopamine release, without blocking dopamine receptors. Promising in phase 2, it failed in two phase 3 trials; a third has finished.

At a glance

Type
Medicine: TAAR1 and serotonin 5-HT1A receptor agonist
Used for
Tested in adults with acute schizophrenia
Status
In trials, after two phase 3 trials found no benefit in 2023
Evidence
EarlyHow evidence is rated
Administration
Tablets, once a day
Common side effects
Sleepiness, digestive complaints, anxiety
In Europe
In trials in the United States and Japan
Clinical summaryFor health professionals

What it is

Ulotaront acts on TAAR1, a receptor that regulates how much dopamine nerve cells release, and on the serotonin 5-HT1A receptor. It does not block dopamine receptors.1,2

How it works

In a brain-scan study, 22 people with schizophrenia took ulotaront or a placebo for two weeks alongside their antipsychotic. Ulotaront reduced how much dopamine the striatum produces, and those in whom it fell more had a larger fall in hallucinations and delusions.3 It therefore acts on the step that brain scans have found raised in schizophrenia, the production of dopamine, rather than on its receptor, as explained in Beyond dopamine (opens in a new tab).

How well it works

In a four-week phase 2 trial of 245 people, symptoms fell by 17.2 points on ulotaront and 9.7 on placebo.2

Two six-week phase 3 trials, with 435 and 464 people, did not confirm it: no dose did better than placebo. The makers attributed this partly to an unusually large improvement on placebo, possibly linked to the COVID-19 pandemic.1 A new phase 3 trial with 538 people has finished enrolling, and its results are expected after October 2026.4 A related medicine from Roche, ralmitaront, did not beat placebo, and its trial in negative symptoms was stopped early.5,6

Side effects

In the phase 2 trial, sleepiness and digestive complaints were the most common side effects, and one person taking ulotaront died suddenly of a heart problem.2 Across trials, anxiety was about twice as common on the 75 mg dose as on placebo.7

What we don’t know yet

  • Whether the new phase 3 trial confirms a benefit.
  • Whether acting on dopamine production, rather than on its receptor, helps people whom antipsychotics have not helped.

Sources

  1. Sumitomo Pharma, Otsuka Pharmaceutical. Sumitomo Pharma and Otsuka announce topline results from Phase 3 DIAMOND 1 and DIAMOND 2 clinical studies evaluating ulotaront in schizophrenia. 31 July 2023.
    otsuka-us.com (opens in a new tab)
  2. Koblan KS, Kent J, Hopkins SC, et al. A Non–D2-Receptor-Binding Drug for the Treatment of Schizophrenia. New England Journal of Medicine. 2020;382(16):1497–1506.
    DOI (opens in a new tab)PubMed (opens in a new tab)
  3. Howes OD, Vano LJ, Petty AE, et al. TAAR1 Regulates Presynaptic Dopamine Function: Evidence From Preclinical Studies and a Phase 1b Trial in Patients With Schizophrenia. Biological Psychiatry. 2026;100(2):199–207.
    DOI (opens in a new tab)PubMed (opens in a new tab)
  4. Otsuka Pharmaceutical Development & Commercialization. A trial of the efficacy and safety of SEP-363856 in acutely psychotic participants with schizophrenia (NCT06894212). 2026.
    clinicaltrials.gov (opens in a new tab)
  5. Hoffmann-La Roche. A trial of the efficacy and the safety of RO6889450 (ralmitaront) vs placebo in patients with an acute exacerbation of schizophrenia or schizoaffective disorder (NCT04512066). 2026.
    clinicaltrials.gov (opens in a new tab)
  6. Hoffmann-La Roche. A study to assess the effects of RO6889450 (ralmitaront) in participants with schizophrenia or schizoaffective disorder and negative symptoms (NCT03669640). 2026.
    clinicaltrials.gov (opens in a new tab)
  7. Hsu YC, Hung TY, Chen YCB, et al. Trajectory of efficacy and safety across ulotaront dose levels in schizophrenia: a systematic review and dose–response meta-analysis. International Journal of Neuropsychopharmacology. 2025;28(9):pyaf059.
    DOI (opens in a new tab)PubMed (opens in a new tab)

Not medical advice. Talk to a doctor before starting or changing any treatment. Disclaimer

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Page last reviewed: 5 November 2026Next review due: May 2027

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