Esperoct 2000unit Inj 1 Vial
It is used to treat or prevent bleeding in people with hemophilia.
Drug Class
Antihemophilic Agent
Pharmacologic Class
Recombinant Coagulation Factor VIII, Pegylated
Pregnancy Category
Category C
FDA Approved
Feb 2019
DEA Schedule
Not Controlled
Overview
What is this medicine?
Esperoct is a medicine used to treat and prevent bleeding in people with hemophilia A, a condition where your blood doesn't clot properly. It works by replacing a missing protein in your blood called Factor VIII, which is needed for normal blood clotting. Because it's pegylated, it stays in your body longer, allowing for less frequent injections.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered as an injection into a vein. If you will be self-administering the injection, your doctor or nurse will instruct you on the proper technique. Before and after handling the medication, wash your hands thoroughly.
If the medication has been stored in the refrigerator, allow it to reach room temperature before mixing. Do not heat the medication. You can warm it to room temperature by holding the vial in your hands until it feels as warm as your body temperature.
Before use, this medication must be mixed according to the instructions provided by your doctor. Do not shake the vial. After mixing, use the medication within 4 hours if stored at room temperature, or store it in the refrigerator for up to 24 hours if needed. Do not use the medication if the solution appears cloudy, is leaking, or contains particles. Also, do not use the medication if the solution has changed color.
After using the medication, discard any remaining balance in the opened vial. Dispose of needles and other sharp objects in a designated needle/sharp disposal box. Do not reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
Store unopened vials of this medication in the refrigerator, but do not freeze.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is administered as an injection into a vein. If you will be self-administering the injection, your doctor or nurse will instruct you on the proper technique. Before and after handling the medication, wash your hands thoroughly.
If the medication has been stored in the refrigerator, allow it to reach room temperature before mixing. Do not heat the medication. You can warm it to room temperature by holding the vial in your hands until it feels as warm as your body temperature.
Before use, this medication must be mixed according to the instructions provided by your doctor. Do not shake the vial. After mixing, use the medication within 4 hours if stored at room temperature, or store it in the refrigerator for up to 24 hours if needed. Do not use the medication if the solution appears cloudy, is leaking, or contains particles. Also, do not use the medication if the solution has changed color.
After using the medication, discard any remaining balance in the opened vial. Dispose of needles and other sharp objects in a designated needle/sharp disposal box. Do not reuse needles or other items. When the disposal box is full, follow local regulations for proper disposal. If you have any questions or concerns, consult your doctor or pharmacist.
Storage and Disposal
Store unopened vials of this medication in the refrigerator, but do not freeze.
Missed Dose
If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Adhere strictly to your prescribed dosing schedule, especially for prophylaxis, to prevent bleeding episodes.
- Learn to recognize the signs of bleeding and administer on-demand doses as instructed by your healthcare provider.
- Avoid activities that carry a high risk of injury or bleeding.
- Maintain good dental hygiene to prevent gum bleeding.
- Inform all healthcare providers (including dentists) that you have hemophilia and are on Factor VIII replacement therapy.
- Carry identification indicating your hemophilia status.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Routine Prophylaxis: 50 units/kg intravenously once weekly. May adjust to 65 units/kg once weekly or 50 units/kg every 5 days based on patient response. On-demand Treatment: Minor/Moderate bleeding: 20-40 units/kg IV. Major bleeding: 40-60 units/kg IV.
Dose Range:
20 - 65 mg
Condition-Specific Dosing:
routine_prophylaxis:
50 units/kg IV once weekly (adjust to 65 units/kg once weekly or 50 units/kg every 5 days)
on_demand_minor_moderate_bleeding:
20-40 units/kg IV
on_demand_major_bleeding:
40-60 units/kg IV
Pediatric Dosing
Neonatal:
Dosing established (refer to child dosing)
Infant:
Dosing established (refer to child dosing)
Child:
Routine Prophylaxis: 50 units/kg intravenously once weekly. May adjust to 65 units/kg once weekly or 50 units/kg every 5 days based on patient response. On-demand Treatment: Minor/Moderate bleeding: 20-40 units/kg IV. Major bleeding: 40-60 units/kg IV.
Adolescent:
Routine Prophylaxis: 50 units/kg intravenously once weekly. May adjust to 65 units/kg once weekly or 50 units/kg every 5 days based on patient response. On-demand Treatment: Minor/Moderate bleeding: 20-40 units/kg IV. Major bleeding: 40-60 units/kg IV.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended.
Dialysis:
Not applicable; Factor VIII is not significantly cleared by dialysis.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended.
Pharmacology
Mechanism of Action
Esperoct is a recombinant, pegylated Factor VIII (FVIII) product. It temporarily replaces the deficient endogenous Factor VIII, which is an essential cofactor for activated Factor IX (FIXa) in the activation of Factor X (FX) to Factor Xa (FXa). Activated Factor X (FXa) converts prothrombin into thrombin, which in turn converts fibrinogen into fibrin, leading to clot formation. Pegylation extends the half-life of the Factor VIII molecule.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Immediate (IV administration)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
Approximately 0.05-0.07 L/kg (similar to plasma volume)
ProteinBinding:
Binds to von Willebrand factor (vWF) in plasma, which stabilizes FVIII.
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours (terminal half-life, significantly prolonged due to pegylation compared to non-pegylated FVIII)
Clearance:
Approximately 2.5-3.5 mL/hr/kg
ExcretionRoute:
Primarily via proteolytic degradation and cellular uptake; not renally or hepatically excreted in an unchanged form.
Unchanged:
Not applicable (protein degradation)
Pharmacodynamics
OnsetOfAction:
Immediate (upon intravenous administration)
PeakEffect:
Immediate (upon intravenous administration)
DurationOfAction:
Extended (due to pegylation, allowing for once-weekly dosing in prophylaxis)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Chest pain
Dizziness or fainting
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or persist, contact your doctor for advice:
Irritation at the injection site
Important Note
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, don't hesitate to reach out to your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Chest pain
Dizziness or fainting
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or persist, contact your doctor for advice:
Irritation at the injection site
Important Note
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, don't hesitate to reach out to your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of bleeding: unusual bruising, prolonged bleeding from cuts, nosebleeds, blood in urine or stools, joint pain or swelling, severe headache, vision changes.
- Signs of allergic reaction: rash, hives, itching, facial swelling, difficulty breathing, chest tightness, dizziness, fainting.
- Signs of inhibitor development: bleeding that does not stop or respond to your usual dose of Esperoct.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are allergic to hamsters, as this may be relevant to your treatment.
Any other medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions.
Any existing health problems you have, as they may affect the safety and efficacy of this medication.
To ensure your safety, it is vital to discuss all your medications and health issues with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other drugs and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are allergic to hamsters, as this may be relevant to your treatment.
Any other medications you are taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions.
Any existing health problems you have, as they may affect the safety and efficacy of this medication.
To ensure your safety, it is vital to discuss all your medications and health issues with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other drugs and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Regular blood tests and other laboratory assessments should be conducted as directed by your doctor to monitor your condition.
If you experience unexplained bruising, bleeding, or if bleeding does not stop after taking this medication, contact your doctor immediately, as this may indicate that your current dose is not effective.
Before traveling, consult with your doctor and ensure you have an adequate supply of this medication to last throughout your trip.
If you are pregnant, planning to become pregnant, or are breastfeeding, discuss this with your doctor to carefully weigh the benefits and risks of this medication to both you and your baby.
Regular blood tests and other laboratory assessments should be conducted as directed by your doctor to monitor your condition.
If you experience unexplained bruising, bleeding, or if bleeding does not stop after taking this medication, contact your doctor immediately, as this may indicate that your current dose is not effective.
Before traveling, consult with your doctor and ensure you have an adequate supply of this medication to last throughout your trip.
If you are pregnant, planning to become pregnant, or are breastfeeding, discuss this with your doctor to carefully weigh the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- While overdose is unlikely to cause acute toxicity, very high levels of Factor VIII could theoretically increase the risk of thrombotic events (blood clots).
What to Do:
In case of suspected overdose, seek immediate medical attention. Management is supportive and may involve monitoring for signs of thrombosis. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Monitoring
Baseline Monitoring
Factor VIII activity levels
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation of therapy.
Factor VIII inhibitor levels (Bethesda assay)
Rationale: To screen for pre-existing inhibitors, which can render the treatment ineffective.
Timing: Prior to initiation of therapy.
Routine Monitoring
Factor VIII activity levels
Frequency: Periodically, especially when adjusting dose or in response to bleeding episodes.
Target: Target levels vary based on clinical situation (e.g., >1% for prophylaxis, higher for bleeding events).
Action Threshold: If levels are not therapeutic or if bleeding occurs despite adequate dosing, consider inhibitor development or pharmacokinetic variability.
Factor VIII inhibitor levels (Bethesda assay)
Frequency: Regularly (e.g., every 3-6 months, or more frequently in the first year of treatment, or if clinical response is suboptimal).
Target: <0.6 Bethesda Units (BU)/mL
Action Threshold: If inhibitor levels are ≥0.6 BU/mL, treatment may be ineffective, and alternative therapies (e.g., bypassing agents) may be required.
Clinical response (bleeding episodes, joint health)
Frequency: Ongoing
Target: Reduction in bleeding frequency, resolution of bleeding episodes.
Action Threshold: Persistent or recurrent bleeding may indicate inadequate dosing, inhibitor development, or other complications.
Symptom Monitoring
- Signs of bleeding (e.g., joint pain/swelling, bruising, nosebleeds, blood in urine/stools, prolonged bleeding from cuts)
- Signs of allergic reaction (e.g., rash, hives, itching, facial swelling, shortness of breath, chest tightness, dizziness, fainting)
- Signs of inhibitor development (e.g., lack of response to previously effective doses of Esperoct)
Special Patient Groups
Pregnancy
Use only if clearly needed. There are no adequate and well-controlled studies of Esperoct in pregnant women. Animal reproduction studies have not been conducted. It is not known whether Esperoct can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity.
Trimester-Specific Risks:
First Trimester:
Limited data; theoretical risk is low as Factor VIII is a naturally occurring protein.
Second Trimester:
Limited data.
Third Trimester:
Limited data; Factor VIII levels naturally increase during pregnancy, but replacement may still be needed for bleeding events or delivery.
Lactation
It is not known whether Esperoct is excreted in human milk. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Esperoct and any potential adverse effects on the breastfed infant from Esperoct or from the underlying maternal condition. Factor VIII is a large protein, making significant transfer into breast milk unlikely.
Infant Risk:
Low risk of adverse effects to the breastfed infant.
Pediatric Use
Esperoct is approved for use in pediatric patients of all ages with hemophilia A. Dosing is weight-based and similar to adults. Close monitoring of Factor VIII activity and inhibitor development is crucial, especially in previously untreated patients (PUPs).
Geriatric Use
Clinical studies of Esperoct did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Esperoct offers extended half-life compared to conventional Factor VIII products, allowing for less frequent (e.g., once-weekly) prophylactic dosing.
- It is important to monitor for the development of Factor VIII inhibitors, especially in previously untreated patients (PUPs) or those with a history of inhibitor development to other Factor VIII products.
- The dose should be individualized based on the patient's Factor VIII levels, clinical response, and pharmacokinetic parameters if available.
- Patients should be educated on self-administration techniques and signs of bleeding or allergic reactions.
- This product is for intravenous administration only.
Alternative Therapies
- Other recombinant Factor VIII products (e.g., Advate, Eloctate, Adynovate, Jivi, Hemlibra (emicizumab - non-factor VIII bypassing agent), Alprolix, Nuwiq, Xyntha, Kogenate, Recombinate)
- Plasma-derived Factor VIII products
- Bypassing agents (e.g., FEIBA, NovoSeven RT) for patients with inhibitors
- Gene therapy (e.g., Roctavian) for eligible patients
Cost & Coverage
Average Cost:
Highly variable, typically several thousand to tens of thousands of USD per vial depending on unit strength. per vial
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high co-pays or co-insurance)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.