Last reviewed · How we verify
Saphris (ASENAPINE)
Saphris works by blocking the action of serotonin at the 5-hydroxytryptamine receptor 2C.
Saphris (Asenapine) is a small molecule atypical antipsychotic developed by Forest Labs Inc and currently owned by Hisamitsu. It targets the 5-hydroxytryptamine receptor 2C to treat bipolar affective disorder, mixed bipolar I disorder, and schizophrenia. Saphris was FDA-approved in 2009 and is still under patent. Key safety considerations include its potential for sedation, dizziness, and increased risk of stroke. As a non-generic medication, it is not yet available from generic manufacturers.
At a glance
| Generic name | ASENAPINE |
|---|---|
| Sponsor | Hisamitsu |
| Drug class | Atypical Antipsychotic [EPC] |
| Target | 5-hydroxytryptamine receptor 2C |
| Modality | Small molecule |
| Therapeutic area | Neuroscience |
| Phase | FDA-approved |
| First approval | 2009 |
Mechanism of action
The mechanism of action of asenapine, as with other drugs having efficacy in schizophrenia and bipolar disorder, is unknown. It has been suggested that the efficacy of asenapine in schizophrenia is mediated through combination of antagonist activity at D2 and 5-HT2A receptors.
Approved indications
- Bipolar affective disorder, current episode manic
- Mixed bipolar I disorder
- Schizophrenia
Boxed warnings
- WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Asenapine is not approved for the treatment of patients with dementia-related psychosis [see Warnings and Precautions (5.1, 5.2)]. WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS See full prescribing information for complete boxed warning. Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Asenapine is not approved for the treatment of patients with dementia-related psychosis. ( 5.1 , 5.2 )
Common side effects
- Somnolence
- Akathisia
- Extrapyramidal symptoms (excluding akathisia)
- Vomiting
- Dizziness
- Oral hypoesthesia
- Constipation
- Weight increased
- Stomach discomfort
- Fatigue
- Irritability
- Increased appetite
Drug interactions
- High Risk QT Prolonging Agents
- azithromycin
- clarithromycin
- erythromycin
Key clinical trials
- Τhe Combination of Pharmacotherapy With RECOVERYTRSGR and RECOVERYTRSBDGR. (PHASE4)
- A Study to Assess Stroke Risk Among Users of Typical Versus Atypical Antipsychotics Stratified by Broad Age Group
- An Acceptability Study of Unflavored Asenapine Versus Raspberry Flavored Asenapine in Stable Patients With a Psychotic Disorder (P07010)(COMPLETED) (PHASE2)
- 9 Week Extension Study of Asenapine and Olanzapine in Treatment of Mania (P07007)(COMPLETED) (PHASE3)
- Efficacy and Safety of Asenapine With Placebo and Haloperidol (41023)(P05926)(COMPLETED) (PHASE3)
- 3-week Study of Asenapine, Olanzapine and Placebo for Treatment of Bipolar Mania (P07009) (PHASE3)
- 3-Week Study of Asenapine, Olanzapine and Placebo for Treatment of Bipolar Mania (P07008) (PHASE3)
- Efficacy and Safety of Asenapine Compared With Olanzapine in Patients With Persistent Negative Symptoms of Schizophrenia (25543)(COMPLETED)(P05817) (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Saphris CI brief — competitive landscape report
- Saphris updates RSS · CI watch RSS
- Hisamitsu portfolio CI