Esperoct 4000iu 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 bleeding disorder where blood doesn't clot properly). It works by replacing a missing protein called Factor VIII, which is needed for blood clotting. The 'pegylated' part means it's designed to stay in your body longer, so you might not need injections as often.
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 provide guidance 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.
To prepare the medication, follow the mixing instructions provided by your doctor. Avoid shaking 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 it if the solution has changed color. Dispose of any unused portion of the opened vial after use.
Disposal 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 of This Medication
Store unopened vials 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 provide guidance 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.
To prepare the medication, follow the mixing instructions provided by your doctor. Avoid shaking 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 it if the solution has changed color. Dispose of any unused portion of the opened vial after use.
Disposal 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 of This Medication
Store unopened vials 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
- Always carry your medication and medical identification (e.g., medical alert bracelet) indicating you have hemophilia A.
- Avoid activities that carry a high risk of injury or bleeding.
- Avoid medications that interfere with blood clotting, such as aspirin and NSAIDs (e.g., ibuprofen, naproxen), unless specifically advised by your doctor.
- Maintain good dental hygiene to prevent gum bleeding.
- Follow your doctor's instructions for regular infusions, even if you feel well, to prevent bleeding episodes.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Prophylaxis: 50 IU/kg every 4 days or 60 IU/kg twice weekly. On-demand: 20-60 IU/kg depending on bleed severity.
Dose Range:
20 - 60 mg
Condition-Specific Dosing:
Prophylaxis:
50 IU/kg every 4 days or 60 IU/kg twice weekly
Minor Hemorrhage (e.g., early hemarthrosis, minor muscle bleed):
20-40 IU/kg, target FVIII activity 40-80%
Moderate Hemorrhage (e.g., more extensive hemarthrosis, muscle bleed with swelling, significant trauma):
30-60 IU/kg, target FVIII activity 60-100%
Major Hemorrhage (e.g., life-threatening bleeds, major surgery):
40-60 IU/kg, target FVIII activity 80-120%
Pediatric Dosing
Neonatal:
Not established
Infant:
Dosing similar to adults for prophylaxis and on-demand treatment, based on FVIII levels and clinical response. Prophylaxis: 50 IU/kg every 4 days or 60 IU/kg twice weekly.
Child:
Dosing similar to adults for prophylaxis and on-demand treatment, based on FVIII levels and clinical response. Prophylaxis: 50 IU/kg every 4 days or 60 IU/kg twice weekly.
Adolescent:
Dosing similar to adults for prophylaxis and on-demand treatment, based on FVIII levels and clinical response. Prophylaxis: 50 IU/kg every 4 days or 60 IU/kg twice weekly.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended.
Dialysis:
No specific dose adjustment recommended. Monitor FVIII levels and clinical response.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended.
Pharmacology
Mechanism of Action
Turoctocog alfa pegol (Esperoct) is a recombinant DNA-derived, pegylated coagulation Factor VIII (FVIII) product. FVIII is an essential cofactor in the intrinsic coagulation pathway, where it binds to activated Factor IX (FIXa) and phospholipids, accelerating the conversion of Factor X (FX) to activated Factor X (FXa). FXa, in turn, converts prothrombin to thrombin, leading to the formation of a stable fibrin clot. In hemophilia A, FVIII is deficient or defective, leading to impaired clot formation. Esperoct temporarily replaces the missing FVIII, restoring hemostasis. The pegylation prolongs its half-life in circulation.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Immediate (intravenous administration)
FoodEffect:
Not applicable (intravenous administration)
Distribution:
Vd:
Approximately 0.1 L/kg
ProteinBinding:
Binds to von Willebrand factor (vWF)
CnssPenetration:
Limited
Elimination:
HalfLife:
Terminal half-life: Approximately 19 hours (range 12.5 to 27.7 hours)
Clearance:
Approximately 3.5 mL/hr/kg
ExcretionRoute:
Metabolites excreted via renal and hepatic pathways
Unchanged:
Not applicable (protein catabolism)
Pharmacodynamics
OnsetOfAction:
Immediate
PeakEffect:
Within minutes of administration
DurationOfAction:
Sustained FVIII activity for up to 4 days (prophylaxis regimen), due to prolonged half-life from pegylation.
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 guidance:
Irritation at the injection site
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can provide medical advice on managing side effects.
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 guidance:
Irritation at the injection site
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can provide medical advice on managing side effects.
Seek Immediate Medical Attention If You Experience:
- Signs of allergic reaction: rash, hives, itching, swelling of the face, lips, tongue, or throat, difficulty breathing, chest tightness, dizziness, faintness.
- Signs of inhibitor development: increased frequency of bleeding, bleeding that does not stop or respond to your usual dose of Esperoct.
- Signs of blood clots (rare): pain, swelling, warmth, or redness in an arm or leg; sudden chest pain; shortness of breath; sudden vision changes; slurred speech.
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 allergic reaction you experienced, including any symptoms that occurred.
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, tell your doctor and pharmacist about:
+ All prescription and over-the-counter (OTC) medications you are taking
+ Any natural products or vitamins you are using
+ Existing health problems or conditions
It is crucial to verify that it is safe to take this medication with your other medications 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 allergic reaction you experienced, including any symptoms that occurred.
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, tell your doctor and pharmacist about:
+ All prescription and over-the-counter (OTC) medications you are taking
+ Any natural products or vitamins you are using
+ Existing health problems or conditions
It is crucial to verify that it is safe to take this medication with your other medications 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 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.
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.
Overdose Information
Overdose Symptoms:
- No specific symptoms of overdose are known for Factor VIII products. Very high levels of Factor VIII could theoretically increase the risk of thrombosis, though this is rare.
What to Do:
In case of suspected overdose, contact your healthcare provider or emergency services immediately. Management is supportive. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Monitoring
Baseline Monitoring
Baseline Factor VIII activity levels
Rationale: To establish pre-treatment levels and guide initial dosing.
Timing: Prior to initiation of therapy.
Inhibitor (neutralizing antibody) screening
Rationale: To detect pre-existing inhibitors to Factor VIII, which can render treatment ineffective.
Timing: Prior to initiation of therapy.
Routine Monitoring
Factor VIII activity levels
Frequency: Regularly, especially during initial treatment, before and after surgery, or for severe bleeds. Periodically during prophylaxis.
Target: Dependent on clinical situation (e.g., 40-80% for minor bleeds, 80-120% for major bleeds/surgery).
Action Threshold: If levels are not within target range or clinical response is inadequate, adjust dose or frequency.
Inhibitor (neutralizing antibody) titers (Bethesda assay)
Frequency: Regularly (e.g., every 3-6 months, or if clinical response to treatment is suboptimal).
Target: Negative (<0.6 Bethesda Units/mL)
Action Threshold: If inhibitor titers are detected or increase, consider alternative treatments or immune tolerance induction.
Clinical response to treatment
Frequency: Continuously during treatment of bleeding episodes and periodically during prophylaxis.
Target: Cessation of bleeding, prevention of bleeding episodes.
Action Threshold: Persistent bleeding or new bleeding episodes indicate need for dose adjustment or investigation for inhibitors.
Symptom Monitoring
- Signs of bleeding (e.g., joint pain/swelling, muscle pain, bruising, blood in urine/stool, nosebleeds)
- Signs of allergic or hypersensitivity reactions (e.g., rash, hives, itching, facial swelling, shortness of breath, chest tightness, dizziness, faintness)
- Signs of inhibitor development (e.g., increased frequency of bleeding, bleeding that does not respond to usual doses of Esperoct)
Special Patient Groups
Pregnancy
Esperoct is a Category C drug. There are no adequate and well-controlled studies of Esperoct in pregnant women. Animal reproduction studies have not been conducted. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Risk unknown, use only if clearly needed.
Second Trimester:
Risk unknown, use only if clearly needed.
Third Trimester:
Risk unknown, use only if clearly needed.
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. Caution should be exercised when administering Esperoct to a nursing woman.
Infant Risk:
Not available, potential risk unknown.
Pediatric Use
Esperoct is approved for use in pediatric patients with hemophilia A, including neonates, infants, children, and adolescents. Dosing is based on body weight and Factor VIII activity levels, similar to adults. Clinical studies have shown efficacy and safety in this population.
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 a prolonged half-life compared to conventional recombinant Factor VIII products, allowing for less frequent dosing (e.g., every 4 days or twice weekly for prophylaxis).
- Always confirm the specific Factor VIII activity unit (IU) and concentration before reconstitution and administration.
- Patients should be educated on proper aseptic technique for self-administration and signs/symptoms of bleeding and adverse reactions.
- Regular monitoring for Factor VIII inhibitors is crucial, especially in previously untreated patients (PUPs) or if there's a loss of efficacy.
- The dose and frequency should be individualized based on the patient's Factor VIII levels, clinical response, and type of bleeding or surgical procedure.
Alternative Therapies
- Other recombinant Factor VIII products (e.g., Advate, Eloctate, Adynovate, Jivi, Nuwiq, Recombinate, Xyntha)
- Plasma-derived Factor VIII products (e.g., Hemofil M, Koate-DVI)
- Emicizumab (Hemlibra) - a bispecific antibody mimicking FVIIIa, for prophylaxis in patients with or without inhibitors
- Bypassing agents (e.g., FEIBA, Novoseven RT) - for patients with Factor VIII inhibitors
- Gene therapy (e.g., Roctavian) - for severe hemophilia A
Cost & Coverage
Average Cost:
Highly variable, typically several thousand to tens of thousands of USD per vial depending on strength and quantity. 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's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.