Erzofri

Erzofri (paliperidone palmitate) is an injectable atypical antipsychotic used for the treatment of schizophrenia and schizoaffective disorder in adults.

• May be used as monotherapy or together with mood stabilizers or antidepressants in those with schizoaffective disorder.

Erzofri (paliperidone palmitate) works by being metabolized in the body to its active form, paliperidone. Paliperidone is the primary active metabolite of risperidone. While the exact mechanism of action (MOA) of paliperidone is not fully understood, it is believed to involve blocking dopamine D2 and serotonin 5-HT2A receptors in the brain. This dual action is thought to contribute to its effectiveness in treating schizophrenia.

Erzofri was FDA-approved on 26 July 2024 under the 505(b)(2) pathway. This pathway allows drug manufacturers to submit an application for a new drug based on previously approved drugs using existing data, such as clinical studies or information about similar drugs, to support the approval of their new product.

Do not receive Erzofri if you are allergic to paliperidone, risperidone, or any of the ingredients in Erzofri. See the end of this Erzofri Patient Information guide for a complete list of ingredients in Erzofri.

Before receiving Erzofri, tell your healthcare provider about all your medical conditions, including if you:

• have never taken paliperidone or risperidone before
• have had Neuroleptic Malignant Syndrome (NMS)
• have or had heart problems, including a heart attack, heart failure, abnormal heart rhythm, or long QT syndrome
• have or had low levels of potassium or magnesium in your blood
• have or had uncontrolled movements of your tongue, face, mouth, or jaw (tardive dyskinesia)
• have or had kidney or liver problems
• have or had high blood sugar, diabetes, or have a family history of diabetes
• have or had high levels of total cholesterol, LDL cholesterol, or triglycerides, or low levels of HDL cholesterol
• have Parkinson’s disease or a type of dementia called Lewy Body Dementia
• have or had problems with dizziness or fainting or are being treated for high blood pressure
• have or had a low white blood cell count
• have or had seizures or epilepsy
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

It is not known if Erzofri is safe and effective in children.

Pregnancy

It is not known if Erzofri will harm your unborn baby. If you become pregnant during treatment, talk to your healthcare provider about registering with the National Pregnancy Registry for Atypical Antipsychotics. You can register by calling 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/.

Babies born to women who are treated with Erzofri during their third trimester of pregnancy may experience symptoms such as tremors, irritability, excessive sleepiness, eye twitching, muscle spasms, decreased appetite, difficulty breathing, or abnormal movement of arms and legs. Let your healthcare provider know if these symptoms occur.

Breastfeeding

Erzofri can pass into your breast milk. Talk to your healthcare provider about the best way to feed your baby if you receive Erzofri.

The most common side effects of Erzofri include:

• injection site reactions
• feeling restless or like you need to move
• sleepiness or drowsiness
• dizziness
• abnormal muscle movements including tremors (shaking), shuffling, uncontrolled involuntary movements, and abnormal movements of your eyes.

Serious side effects and warnings

Erzofri carries a Boxed Warning for an increased risk of death in elderly patients with dementia-related psychosis.

Erzofri increases the risk of death and cardiovascular problems (such as a stroke) in elderly people who have lost touch with reality (psychosis) due to confusion and memory loss (dementia). Erzofri should not be used to treat people with dementia-related psychosis.

Erzofri may also cause the following serious side effects.

Neuroleptic Malignant Syndrome (NMS). This a rare reaction to antipsychotic drugs, such as Erzofri that can lead to death. Call your healthcare provider right away or go to your nearest emergency room right away if you get any of the following signs or symptoms:

• high fever
• sweating
• stiff muscles
• changes in your breathing, pulse, heart rate, or blood pressure
• confusion.

Problems with your heartbeat. These heart problems can cause death. Call your healthcare provider right away if you get any of these symptoms:

• passing out or feeling like you will pass out
• dizziness
• feeling as if your heart is pounding or missing beats.

Uncontrolled body movements (tardive dyskinesia). Erzofri may cause movements that you cannot control in your face, tongue, or other body parts. Tardive dyskinesia may not go away, even if you stop taking Erzofri. Tardive dyskinesia may also start after you stop taking Erzofri

Problems with your metabolism such as:

High blood sugar (hyperglycemia) and diabetes. Increases in blood sugar can happen in some people who are treated with Erzofri. Extremely high blood sugar can lead to coma or death. If you have diabetes or risk factors for diabetes such as being overweight, or a family history of diabetes, your healthcare provider should check your blood sugar before you start treatment and during your treatment.

• Call your healthcare provider if you get any of these symptoms of high blood sugar during treatment with Erzofri, such as feeling very thirsty, needing to urinate more than usual, feeling very hungry, feeling weak or tired, feeling sick to your stomach, feeling confused, or your breath smells fruity

Increased fat levels (cholesterol and triglycerides) in your blood. Your healthcare provider may check your cholesterol and triglyceride levels during treatment with Erzofri.

Weight gain. You and your healthcare provider should check your weight regularly during treatment with Erzofri.

Decreased blood pressure (orthostatic hypotension) and fainting. You may feel lightheaded or faint when you rise too quickly from a sitting or lying position.

Falls. Erzofri may make you sleepy or dizzy, may cause a decrease in your blood pressure when changing position (orthostatic hypotension), and can slow your thinking and motor skills which may lead to falls that can cause fractures or other injuries.

Low white blood cell counts. Your healthcare provider may do blood tests during treatment with Erzofri.

Increased prolactin levels in your blood (hyperprolactinemia). Erzofri may cause a rise in the blood levels of a hormone called prolactin that may cause side effects including missed menstrual periods, a reversible reduction in fertility in females who can become pregnant, leakage of milk from the breasts, development of breasts in men, or problems with erection.

Other serious side effects may include

• sleepiness, drowsiness, feeling tired, difficulty thinking and doing normal activities.
• seizures (convulsions)
• difficulty swallowing that can cause food or liquid to get into your lungs
• prolonged or painful erection lasting more than 4 hours (priapism). Call your healthcare provider or go to your nearest emergency room right away if you have an erection that lasts more than 4 hours

Problems with control of your body temperature so that you feel too warm. See “What should I avoid while receiving Erzofri?”

Tell your healthcare provider if you have any side effect that bothers you or does not go away. These are not all of the possible side effects of Erzofri. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Erzofri is given as an injection by your healthcare provider into the muscle (intramuscularly) of your arm or your buttocks 1 time every month. Your first Erzofri injection will be in your arm.

Your healthcare provider will tell you how much Erzofri you will receive and when you will receive it.

If you miss a dose of Erzofri, call your healthcare provider right away to schedule your next injection.

Do not drive, operate heavy machinery, or do other dangerous activities until you know how Erzofri affects you.

• Erzofri may affect your ability to make decisions, think clearly, or react quickly.

Avoid getting too hot or becoming dehydrated.

• Do not exercise too much.
• Do not wear too much clothing or heavy clothing
• In hot weather, stay inside in a cool place if possible.
• Stay out of the sun.
• Drink plenty of water.

Avoid alcohol during treatment with Erzofri

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Erzofri and certain other medicines may affect each other causing possible serious side effects or affecting the way each other works.

An additive effect may occur when other drugs that lower blood pressure are co-administered with Erzofri. This may be noticed especially when going from a sitting or lying position to standing.

Avoid using strong inducers of CYP3A4 and/or P-gp (such as phenytoin, barbituates, rifampin, or St John's Wort) during Erzofri administration. Use paliperidone extended-release tablets instead.

Know the medicines you take. Keep a list of them to show to your healthcare provider or pharmacist when you get a new medicine.

Erzofri ingredients

Active ingredient: paliperidone palmitate

Inactive ingredients: citric acid monohydrate, dibasic sodium phosphate anhydrous, monobasic sodium phosphate monohydrate, polyethylene glycol 4000, polysorbate 20, and sodium hydroxide.

Available as an extended-release injectable suspension in the following strengths:

• 39 mg/0.25 mL
• 78 mg/0.5 mL
• 117 mg/0.75 mL
• 156 mg/mL
• 234 mg/1.5 mL
• 351 mg/2.25 mL.

Shandong Luye Pharmaceutical Co., Ltd., makes Erzofri.