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ESTABLISHED

EFFICACY & SAFETY

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Efficacy Safety Efficacy Safety
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Efficacy Safety Efficacy Safety

ERZOFRI® OFFERS THE ESTABLISHED EFFICACY OF ONCE-MONTHLY PALIPERIDONE PALMITATE LAI1,2

The efficacy of ERZOFRI® in the treatment of adult patients with schizophrenia has been established based on adequate and well-controlled studies of paliperidone palmitate monthly IM injections, the results of which are described here.1,2

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Efficacy Safety Efficacy Safety

For the treatment of schizophrenia1,2

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Time to relapse - schizophrenia1,2
Kaplan-Meier plot of cumulative proportion of subjects with relapse over time

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  • *90% (n=141/156) of patients treated with paliperidone palmitate LAI remained relapse-free at the interim analysis compared to 66% (n=103/156) treated with placebo (P<0.0001). Median time to relapse for placebo group is 163 days.
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Efficacy Safety Efficacy Safety

ERZOFRI® OFFERS THE ESTABLISHED TOLERABILITY OF ONCE-MONTHLY PALIPERIDONE PALMITATE1,2

The safety of ERZOFRI® in the treatment of adult patients with schizophrenia has been established based on adequate and well-controlled studies of paliperidone palmitate monthly IM injections, the results of which are described here.1,2

Safety in schizophrenia – long-term maintenance study1,2

 

Adverse events occurring in ≥2% of patients in the long-term schizophrenia maintenance trial2

Placebo
(n=203)		 Monthly paliperidone
palmitate LAI (n=205)
Weight increase 1% 7%
Nasopharyngitis 3% 4%
Headache 3% 3%
Blood glucose increase 1% 3%
Gastroenteritis viral <1% 2%
Tremor <1% 2%

In the pivotal schizophrenia trials for monthly paliperidone palmitate LAI, the most common adverse reactions (incidence ≥5% and occurring at least twice as often as placebo) were injection-site reactions, somnolence/ sedation, dizziness, akathisia, and extrapyramidal disorder.1

 

IM=intramuscular; LAI=long-acting injectable; PANSS=Positive and Negative Syndrome Scale.

 

Clinical Trial Efficacy in

Schizoaffective Disorder
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INDICATIONS AND USAGE:

INDICATIONS AND USAGE: ERZOFRI® (paliperidone palmitate) extended-release injectable suspension for intramuscular use is an atypical antipsychotic indicated for the treatment of:

  • schizophrenia in adults
  • schizoaffective disorder in adults as monotherapy and as an adjunct to mood stabilizers or antidepressants

IMPORTANT SAFETY INFORMATION FOR ERZOFRI

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. ERZOFRI is not approved for use in patients with dementia-related psychosis.

CONTRAINDICATIONS

ERZOFRI is contraindicated in patients with known hypersensitivity to paliperidone, risperidone, or to any excipients in ERZOFRI.

WARNINGS AND PRECAUTIONS

  • Cerebrovascular Adverse Reactions, Including Stroke, in Elderly Patients with Dementia-Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g., stroke, transient ischemic attacks) including fatalities.
  • Neuroleptic Malignant Syndrome (NMS): NMS, a potentially fatal symptom complex, has been reported in association with antipsychotic drugs. Manage with immediate discontinuation and close monitoring.
  • QT Prolongation: Avoid use with drugs that also increase QT interval and in patients with risk factors for prolonged QT interval and patients with a history of cardiac arrhythmias.
  • Tardive Dyskinesia (TD): TD, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements, may develop in patients treated with antipsychotic drugs. ERZOFRI should be prescribed in a manner that is most likely to minimize occurrence of TD. Chronic antipsychotic treatment should generally be reserved for patients: (1) who suffer from a chronic illness that is known to respond to antipsychotic drugs and (2) for whom alternative, equally effective, but potentially less harmful treatments are not available or appropriate. In patients who require chronic treatment, use the lowest dose and shortest duration of treatment producing a satisfactory clinical response. Periodically reassess the need for continued treatment.

    If signs and symptoms of TD appear in a patient treated with ERZOFRI, drug discontinuation should be considered. However, some patients may require treatment with ERZOFRI despite the presence of the syndrome.

  • Metabolic Changes: Atypical antipsychotic drugs have caused metabolic changes, including hyperglycemia, diabetes mellitus, dyslipidemia, and body weight gain that may increase the cardiovascular/cerebrovascular risk.
    • Hyperglycemia and Diabetes Mellitus: Monitor for hyperglycemia/diabetes mellitus, dyslipidemia, and weight gain. Patients with an established diagnosis of diabetes mellitus who are started on atypical antipsychotics should be monitored regularly for worsening glucose control. Patients with risk factors for diabetes mellitus (e.g., obesity, family history of diabetes) who are starting treatment with atypical antipsychotics should undergo fasting blood glucose testing at the beginning of treatment and periodically during treatment. Any patient treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Patients who develop symptoms of hyperglycemia during treatment with atypical antipsychotics should undergo fasting blood glucose testing. In some cases, hyperglycemia resolved when the atypical antipsychotic was discontinued; however, some patients required continuation of anti-diabetic treatment despite discontinuation of the suspect drug.
    • Dyslipidemia: Undesirable alterations in lipids have been observed in patients treated with atypical antipsychotics.
    • Weight Gain: Weight gain has been observed with atypical antipsychotic use. Clinical monitoring of weight is recommended.
  • Orthostatic Hypotension and Syncope: Paliperidone may induce orthostatic hypotension and syncope in some patients because of its alpha-adrenergic blocking activity. Use ERZOFRI with caution in patients with known cardiovascular disease (e.g., heart failure, history of myocardial infarction or ischemia, conduction abnormalities), cerebrovascular disease, or conditions that predispose the patient to hypotension (e.g., dehydration, hypovolemia, and treatment with antihypertensive medications). Monitoring of orthostatic vital signs should be considered in patients who are vulnerable to hypotension.
  • Falls: Somnolence, postural hypotension, motor and sensory instability have been reported with the use of antipsychotics, including paliperidone palmitate, which may lead to falls, and consequently, fractures or other fall-related injuries.
  • Leukopenia, Neutropenia, and Agranulocytosis: In clinical trial and/or postmarketing experience, events of leukopenia and neutropenia have been reported temporally related to antipsychotic agents, including once-a-month paliperidone palmitate. Agranulocytosis has also been reported. Possible risk factors for leukopenia/neutropenia include pre-existing low white blood cell count (WBC)/absolute neutrophil count (ANC) and history of drug-induced leukopenia/neutropenia. In patients with a history of a clinically significant low WBC/ANC or a drug-induced leukopenia/neutropenia, perform a complete blood count (CBC) frequently during the first few months of therapy. In such patients, consider discontinuation of ERZOFRI at the first sign of a clinically significant decline in WBC in the absence of other causative factors. Monitor patients with clinically significant neutropenia for fever or other symptoms or signs of infection and treat promptly if such symptoms or signs occur. Discontinue ERZOFRI in patients with severe neutropenia (absolute neutrophil count <1000/mm3) and follow their WBC until recovery.
  • Hyperprolactinemia: Paliperidone elevates prolactin levels and the elevation persists during chronic administration. Paliperidone has a prolactin-elevating effect similar to that seen with risperidone, a drug that is associated with higher levels of prolactin than other antipsychotic drugs.  Long-standing hyperprolactinemia, when associated with hypogonadism may lead to decreased bone density in both female and male subjects.
  • Potential for Cognitive and Motor Impairment: Somnolence, sedation, and dizziness were reported as adverse reactions in subjects treated with another once-a-month paliperidone palmitate extended-release injectable suspension. Antipsychotics, including ERZOFRI, have the potential to impair judgement, thinking, or motor skills. Patients should be cautioned about performing activities requiring mental alertness, such as operating hazardous machinery or operating a motor vehicle, until they are reasonably certain that paliperidone therapy does not adversely affect them.
  • Seizures: Like other antipsychotic drugs, ERZOFRI should be used cautiously in patients with a history of seizures or other conditions that potentially lower the seizure threshold.
  • Dysphagia: Esophageal dysmotility and aspiration have been associated with antipsychotic drug use. ERZOFRI and other antipsychotic drugs should be used cautiously in patients at risk for aspiration.
  • Priapism: Drugs with alpha-adrenergic blocking effects have been reported to induce priapism.
  • Disruption of Body Temperature Regulation: Disruption of the body’s ability to reduce core body temperature has been attributed to antipsychotic agents. Appropriate care is advised when prescribing ERZOFRI to patients who will be experiencing conditions which may contribute to an elevation in core body temperature, e.g. exercising strenuously, exposure to extreme heat, receiving concomitant medication with anticholinergic activity, or being subject to dehydration.

ADVERSE REACTIONS

The most common adverse reactions (incidence ≥5% and occurring at least twice as often as placebo) were injection site reactions, somnolence/sedation, dizziness, akathisia, and extrapyramidal disorder.

USE IN SPECIFIC POPULATIONS

Pregnancy Exposure Registry: There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to atypical antipsychotics, including ERZOFRI, during pregnancy. Healthcare providers are encouraged to register patients by contacting the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or online at https://womensmentalhealth.org/clinicaland-research-programs/pregnancyregistry/.

Risk Summary: Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery. Overall, available data from published epidemiologic studies of pregnant women exposed to paliperidone have not established a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes. There are risks to the mother associated with untreated schizophrenia and with exposure to antipsychotics, including ERZOFRI, during pregnancy.

Lactation: Infants exposed to ERZOFRI through breastmilk should be monitored for excess sedation, failure to thrive, jitteriness, and extrapyramidal symptoms (tremors and abnormal muscle movements).

Fertility: Treatment with ERZOFRI may result in an increase in serum prolactin levels, which may lead to a reversible reduction in fertility in females of reproductive potential.

Renal Impairment: Use of ERZOFRI is not recommended in patients with moderate or severe renal impairment (creatinine clearance <50 mL/min).

Patients with Parkinson’s Disease or Lewy Body Dementia: Patients with Parkinson’s Disease or Dementia with Lewy Bodies can experience increased sensitivity to ERZOFRI. Manifestations can include confusion, obtundation, postural instability with frequent falls, extrapyramidal symptoms, and clinical features consistent with neuroleptic malignant syndrome.

Please see full Prescribing Information for ERZOFRI® including BOXED WARNING.