Esperoct 1500unit Inj 1 Vial
It is used to treat or prevent bleeding in people with hemophilia.
Drug Class
Hemostatic agent
Pharmacologic Class
Antihemophilic Factor (Recombinant), 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 genetic bleeding disorder. It works by replacing a missing protein in the blood called Factor VIII, which is essential for blood clotting. Because it's pegylated, it stays in the 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. Be sure to wash your hands before and after handling the medication.
Preparing the Medication
If the medication has been stored in the refrigerator, allow it to come to 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. This medication must be mixed before use, following the instructions provided by your doctor. Do not shake the vial after mixing.
Using the Mixed Medication
After mixing, use the medication within 4 hours if stored at room temperature. If necessary, the mixed medication can be stored in the refrigerator for up to 24 hours. Before using, check the solution for any signs of cloudiness, leakage, or particles. Do not use the medication if the solution has changed color or appears abnormal. Dispose of any unused portion of the opened vial after use.
Disposing of Needles and Supplies
Dispose of used 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. 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. Be sure to wash your hands before and after handling the medication.
Preparing the Medication
If the medication has been stored in the refrigerator, allow it to come to 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. This medication must be mixed before use, following the instructions provided by your doctor. Do not shake the vial after mixing.
Using the Mixed Medication
After mixing, use the medication within 4 hours if stored at room temperature. If necessary, the mixed medication can be stored in the refrigerator for up to 24 hours. Before using, check the solution for any signs of cloudiness, leakage, or particles. Do not use the medication if the solution has changed color or appears abnormal. Dispose of any unused portion of the opened vial after use.
Disposing of Needles and Supplies
Dispose of used 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. If you miss a dose, contact your doctor to determine the best course of action.
Lifestyle & Tips
- Adhere strictly to the prescribed dosing schedule for prophylaxis to prevent bleeding episodes.
- Maintain good dental hygiene to prevent gum bleeding.
- Avoid activities that carry a high risk of injury or bleeding.
- Carry identification indicating hemophilia A and Factor VIII deficiency.
- Learn proper infusion techniques if self-administering at home.
- Report any new or unusual bleeding, or signs of allergic reaction, immediately to your healthcare provider.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Prophylaxis: 50 units/kg every 4 days or 60 units/kg twice weekly. On-demand: Dose based on desired Factor VIII level and type of bleed (e.g., minor bleed: 20-40 units/kg, major bleed: 30-60 units/kg).
Dose Range:
20 - 60 mg
Condition-Specific Dosing:
prophylaxis:
50 units/kg every 4 days or 60 units/kg twice weekly
on_demand_minor_bleed:
20-40 units/kg to achieve 40-80% FVIII activity
on_demand_major_bleed:
30-60 units/kg to achieve 60-100% FVIII activity
Pediatric Dosing
Neonatal:
Not established (limited data in neonates, generally used in older infants/children)
Infant:
Prophylaxis: 50 units/kg every 4 days or 60 units/kg twice weekly. On-demand: Same as adult dosing based on bleed severity.
Child:
Prophylaxis: 50 units/kg every 4 days or 60 units/kg twice weekly. On-demand: Same as adult dosing based on bleed severity.
Adolescent:
Prophylaxis: 50 units/kg every 4 days or 60 units/kg twice weekly. On-demand: Same as adult dosing based on bleed severity.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
Not applicable, Factor VIII is not renally cleared
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Pharmacology
Mechanism of Action
Turoctocog alfa pegol is a recombinant coagulation Factor VIII (FVIII) that temporarily replaces the missing FVIII needed for effective hemostasis in patients with hemophilia A. FVIII acts as a cofactor for activated Factor IX (FIXa) in the intrinsic coagulation pathway, accelerating the activation of Factor X (FX) to Factor Xa (FXa). FXa, in turn, converts prothrombin to thrombin, which then converts fibrinogen to fibrin, forming a stable clot.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Not applicable (IV administration, peak activity achieved shortly after infusion)
FoodEffect:
Not applicable
Distribution:
Vd:
Approximately 0.05 L/kg (similar to plasma volume)
ProteinBinding:
Binds to von Willebrand factor (vWF)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours (terminal half-life, range 15.1-23.9 hours)
Clearance:
Approximately 2.6 mL/hr/kg
ExcretionRoute:
Degraded peptides are excreted via renal and biliary routes
Unchanged:
Not applicable (protein degradation)
Pharmacodynamics
OnsetOfAction:
Immediate (upon completion of infusion)
PeakEffect:
Within minutes of infusion completion
DurationOfAction:
Extended, allowing for less frequent dosing (up to 4 days for prophylaxis)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, including:
+ 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. While 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 do not go away, contact your doctor:
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, consult your doctor. For medical advice about side effects, you can also contact your doctor.
Reporting Side Effects
You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, including:
+ 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. While 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 do not go away, contact your doctor:
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, consult your doctor. For medical advice about side effects, you can also contact your doctor.
Reporting Side Effects
You can 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 allergic reaction: rash, hives, itching, facial swelling, shortness of breath, chest tightness, dizziness, fainting.
- Signs of inhibitor development: increased frequency or severity of bleeding, or if bleeding does not stop as expected after an infusion.
- Signs of bleeding: joint pain or swelling, muscle pain, unusual bruising, nosebleeds, blood in urine or stool, prolonged bleeding from minor cuts.
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 as a result of the allergy.
If you have an allergy to hamsters, discuss this with your doctor, as it may be relevant to your treatment.
* Potential interactions with other medications or health conditions. To ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of:
+ All prescription and over-the-counter (OTC) medications you are taking
+ Natural products and vitamins you are using
+ Any health problems you have
Carefully review your medications and health conditions with your doctor to confirm that it is safe to take this medication. Do not initiate, discontinue, or modify the dosage 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 as a result of the allergy.
If you have an allergy to hamsters, discuss this with your doctor, as it may be relevant to your treatment.
* Potential interactions with other medications or health conditions. To ensure safe treatment, provide your doctor and pharmacist with a comprehensive list of:
+ All prescription and over-the-counter (OTC) medications you are taking
+ Natural products and vitamins you are using
+ Any health problems you have
Carefully review your medications and health conditions with your doctor to confirm that it is safe to take this medication. Do not initiate, discontinue, or modify the dosage 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 or bleeding, or if bleeding does not stop after taking this medication, contact your doctor immediately. This could be an indication that your current dosage is not effective.
Before traveling, consult with your doctor to ensure you have an adequate supply of this medication for the duration of your trip.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
If you experience unexplained bruising or bleeding, or if bleeding does not stop after taking this medication, contact your doctor immediately. This could be an indication that your current dosage is not effective.
Before traveling, consult with your doctor to ensure you have an adequate supply of this medication for the duration of your trip.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- While overdose is rare, extremely high levels of Factor VIII could theoretically increase the risk of thrombosis (blood clot formation), though this is not commonly reported with Factor VIII products.
What to Do:
In case of suspected overdose, contact a healthcare professional or poison control center immediately. Management would be supportive and aimed at monitoring for and treating any thrombotic events if they occur. Call 1-800-222-1222.
Drug Interactions
Monitoring
Baseline Monitoring
Factor VIII activity levels
Rationale: To establish baseline and guide initial dosing, especially for on-demand treatment.
Timing: Prior to initiation of therapy or as needed for dose adjustments.
Inhibitor (neutralizing antibody) screening (Bethesda assay)
Rationale: To detect the presence of inhibitors, which can render Factor VIII ineffective.
Timing: Prior to initiation of therapy, and regularly thereafter (e.g., every 3-6 months, or if bleeding control is poor).
Routine Monitoring
Factor VIII activity levels
Frequency: Periodically, especially when initiating prophylaxis, changing dose, or if bleeding control is suboptimal. Also, before and after major surgery.
Target: Depends on clinical situation (e.g., prophylaxis trough >1-3%, major bleed >60-100%)
Action Threshold: If levels are lower than expected for the dose, consider inhibitor development or pharmacokinetic variability.
Inhibitor (neutralizing antibody) screening
Frequency: Every 3-6 months, or if there is an unexpected lack of clinical response to treatment.
Target: Negative (<0.6 Bethesda Units/mL)
Action Threshold: Positive inhibitor titer requires specialized management by a hematologist.
Clinical response (bleeding episodes)
Frequency: Continuously
Target: Reduction or cessation of bleeding episodes
Action Threshold: Increased frequency or severity of bleeding may indicate need for dose adjustment, inhibitor testing, or re-evaluation of treatment plan.
Symptom Monitoring
- Signs of bleeding (e.g., joint pain/swelling, bruising, nosebleeds, blood in urine/stool)
- Signs of allergic reaction (e.g., rash, hives, itching, facial swelling, shortness of breath, chest tightness, dizziness)
- Signs of inhibitor development (e.g., increased bleeding frequency, poor response to Factor VIII infusions)
Special Patient Groups
Pregnancy
Esperoct is a Category C drug. There are no adequate and well-controlled studies of Esperoct in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Hemophilia A is rare in women, but treatment may be necessary for bleeding complications.
Trimester-Specific Risks:
First Trimester:
Potential risk to fetus cannot be ruled out; use only if clearly needed.
Second Trimester:
Potential risk to fetus cannot be ruled out; use only if clearly needed.
Third Trimester:
Potential risk to fetus cannot be ruled out; use only if clearly needed.
Lactation
It is unknown whether Esperoct is excreted in human milk. Since many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Given its large protein nature, systemic absorption by the infant is unlikely.
Infant Risk:
Low risk of systemic effects in the infant due to large molecular size and likely degradation in the infant's GI tract if ingested.
Pediatric Use
Esperoct has been studied and is approved for use in pediatric patients, including infants (0-12 months), children (1-11 years), and adolescents (12-17 years) with hemophilia A. Dosing is weight-based and similar to adults.
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 is a pegylated Factor VIII, offering an extended half-life compared to conventional Factor VIII products, allowing for less frequent prophylactic infusions (e.g., every 4 days or twice weekly).
- Always confirm the patient's Factor VIII deficiency and rule out inhibitors before initiating therapy.
- Monitor for inhibitor development, especially in previously untreated patients (PUPs) and during the first 50 exposure days.
- Patients should be educated on the signs of allergic reactions and inhibitor development, and instructed to seek immediate medical attention if these occur.
- Dosing is individualized based on the patient's weight, severity of Factor VIII deficiency, location and extent of bleeding, and clinical response.
- Reconstitute Esperoct using the provided diluent and administration set, and administer intravenously. Do not mix with other medicinal products.
Alternative Therapies
- Other recombinant Factor VIII products (e.g., Advate, Eloctate, Adynovate, Jivi, Nuwiq, Xyntha)
- Plasma-derived Factor VIII products (e.g., Humate-P, Alphanate)
- Bypassing agents for patients with inhibitors (e.g., FEIBA, NovoSeven RT)
- Non-factor replacement therapies (e.g., Emicizumab)
- Gene therapy for hemophilia A (e.g., Roctavian)
Cost & Coverage
Average Cost:
Highly variable, typically several thousand to tens of thousands of dollars per vial depending on unit strength and quantity. Annual cost can be hundreds of thousands to over a million dollars. per 1500 unit vial
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to high deductibles/copays)
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 is a good idea to check with your pharmacist. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.