Esperoct 3000unit Inj, 1 Vial
It is used to treat or prevent bleeding in people with hemophilia.
Drug Class
Coagulation Factor
Pharmacologic Class
Antihemophilic Factor (Recombinant), Pegylated
Pregnancy Category
Not available
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 the blood does not clot properly. It works by replacing a missing protein called Factor VIII, which is essential for 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
- Follow your prescribed dosing schedule carefully, whether for prophylaxis or on-demand treatment.
- Learn how to properly prepare and administer the injection at home, or ensure a healthcare professional administers it.
- Keep a detailed record of all infusions, including date, time, dose, and reason for infusion (e.g., prophylaxis, bleeding event).
- Report any bleeding episodes, even minor ones, to your healthcare provider.
- Avoid activities that carry a high risk of injury or bleeding.
- Inform all healthcare providers (including dentists) that you have hemophilia A and are using Esperoct.
- Wear a medical alert identification (e.g., bracelet or necklace) indicating your condition.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Prophylaxis: 50 units/kg intravenously every 4 days or 65 units/kg intravenously twice weekly. On-demand treatment: 20-50 units/kg intravenously, adjusted based on bleeding severity.
Dose Range:
20 - 65 mg
Condition-Specific Dosing:
prophylaxis:
50 units/kg IV every 4 days or 65 units/kg IV twice weekly
on_demand_minor_bleeding:
20-30 units/kg IV
on_demand_major_bleeding:
30-50 units/kg IV
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Prophylaxis (0 to <12 years): 65 units/kg intravenously twice weekly. On-demand treatment: 20-50 units/kg intravenously, adjusted based on bleeding severity.
Adolescent:
Prophylaxis (>=12 years): 50 units/kg intravenously every 4 days or 65 units/kg intravenously twice weekly. On-demand treatment: 20-50 units/kg intravenously, adjusted based on bleeding severity.
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 clinical response and Factor VIII levels.
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 is a recombinant DNA-derived, pegylated human coagulation Factor VIII (FVIII) that temporarily replaces the missing coagulation FVIII needed for effective hemostasis in patients with hemophilia A. FVIII acts as a cofactor for activated Factor IX (FIXa) in the activation of Factor X (FX) to Factor Xa (FXa), which ultimately leads to the conversion of prothrombin to thrombin and the formation of a fibrin clot.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Immediate (intravenous administration)
FoodEffect:
Not applicable (intravenous administration)
Distribution:
Vd:
Approximately 4.8 L (adults)
ProteinBinding:
Not highly protein bound; circulates bound to von Willebrand factor (vWF)
CnssPenetration:
Limited
Elimination:
HalfLife:
Terminal half-life: Approximately 19 hours (adults), 14.5 hours (adolescents), 13.6 hours (children 6 to <12 years), 12.6 hours (children 0 to <6 years).
Clearance:
Approximately 0.26 L/hour (adults)
ExcretionRoute:
Primarily via proteolytic degradation; no specific excretion route.
Unchanged:
Not applicable (protein degradation)
Pharmacodynamics
OnsetOfAction:
Immediate (upon intravenous administration)
PeakEffect:
Immediate (upon intravenous administration)
DurationOfAction:
Extended due to pegylation, allowing for less frequent dosing (e.g., every 4 days or twice weekly).
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
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. 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 guidance:
Irritation at the injection site
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. 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 allergic reaction: rash, hives, itching, redness, swelling of the face, eyes, lips, or tongue, difficulty breathing, wheezing, chest tightness, dizziness, lightheadedness, fainting.
- Signs of inhibitor development: increased bleeding, bleeding that does not stop with treatment, or a lack of expected response to Esperoct.
- Signs of blood clots (rare): pain, swelling, warmth, or redness in an arm or leg; sudden chest pain; shortness of breath.
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 evaluations should be performed 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 dose is not effective, and your doctor may need to adjust your treatment.
Before traveling, consult with your doctor to 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, notify your doctor. It is crucial to discuss the potential benefits and risks of this medication to both you and your baby, and your doctor will help you make an informed decision.
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 dose is not effective, and your doctor may need to adjust your treatment.
Before traveling, consult with your doctor to 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, notify your doctor. It is crucial to discuss the potential benefits and risks of this medication to both you and your baby, and your doctor will help you make an informed decision.
Overdose Information
Overdose Symptoms:
- While overdose is unlikely to cause acute toxicity, very high doses could theoretically increase the risk of thrombotic events (blood clots).
What to Do:
In case of suspected overdose, contact your healthcare provider or emergency services immediately. Call 911 or the Poison Control Center at 1-800-222-1222. Management would be supportive and focused on monitoring for and treating any thrombotic complications.
Drug Interactions
Monitoring
Baseline Monitoring
Factor VIII activity levels
Rationale: To establish baseline FVIII 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 impact treatment efficacy.
Timing: Prior to initiation of therapy.
Routine Monitoring
Factor VIII activity levels
Frequency: Periodically, especially after dose adjustments, during bleeding episodes, or if clinical response is suboptimal.
Target: Dependent on clinical situation (e.g., >1% for prophylaxis, higher for bleeding events).
Action Threshold: Suboptimal FVIII levels or unexpected bleeding may indicate need for dose adjustment or inhibitor testing.
Inhibitor (neutralizing antibody) screening
Frequency: Regularly (e.g., every 3-6 months for the first few years, then annually) or if there is a lack of expected clinical response.
Target: Negative (Bethesda units <0.6 BU/mL)
Action Threshold: Positive inhibitor titer (>=0.6 BU/mL) requires further investigation and may necessitate alternative treatment strategies.
Signs and symptoms of allergic reactions
Frequency: During and immediately after infusion, and with subsequent doses.
Target: Absence of symptoms
Action Threshold: Presence of rash, urticaria, pruritus, facial swelling, dyspnea, chest tightness, or anaphylaxis requires immediate discontinuation and supportive care.
Symptom Monitoring
- Frequency and severity of bleeding episodes
- Signs of allergic or hypersensitivity reactions (e.g., rash, hives, itching, facial swelling, difficulty breathing, chest tightness, dizziness, faintness)
- Signs of inhibitor development (e.g., increased bleeding, lack of response to treatment)
Special Patient Groups
Pregnancy
There are no adequate and well-controlled studies of Esperoct in pregnant women. Animal reproduction studies have not been conducted. Use during pregnancy only if clearly needed and the potential benefits outweigh the potential risks. The clinical experience with Factor VIII products suggests that they are generally safe during pregnancy when indicated for hemophilia A.
Trimester-Specific Risks:
First Trimester:
Risk unknown; use only if clearly indicated.
Second Trimester:
Risk unknown; use only if clearly indicated.
Third Trimester:
Risk unknown; use only if clearly indicated.
Lactation
It is unknown whether turoctocog alfa pegol is excreted in human milk. However, Factor VIII is a normal component of human plasma. 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. Generally considered compatible with breastfeeding.
Infant Risk:
Low risk; Factor VIII is a large protein and unlikely to be absorbed intact by the infant.
Pediatric Use
Esperoct is approved for use in pediatric patients, including neonates, infants, children, and adolescents with hemophilia A. Dosing is weight-based and adjusted according to age group and clinical need. Clinical studies included pediatric patients down to 0 years of age.
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. No specific dose adjustment is generally required for elderly patients, but dosing should be individualized based on clinical response and Factor VIII levels.
Clinical Information
Clinical Pearls
- Esperoct is a pegylated Factor VIII product, which provides an extended half-life compared to conventional Factor VIII products, allowing for less frequent intravenous infusions (e.g., every 4 days or twice weekly for prophylaxis).
- Individualize dosing based on the patient's Factor VIII levels, the severity of the bleeding episode, and the patient's clinical response.
- Always confirm the Factor VIII activity level using a one-stage clotting assay, as chromogenic assays may not accurately reflect in vivo activity for pegylated products.
- Patients should be monitored for the development of Factor VIII inhibitors, especially during the first 50 exposure days, as this can lead to a lack of efficacy.
- Ensure proper aseptic technique during preparation and administration to minimize the risk of infection.
- Do not mix Esperoct with other medicinal products or diluents other than the provided sterile water for injection.
Alternative Therapies
- Other recombinant Factor VIII products (e.g., Advate, Eloctate, Adynovate, Jivi, Hemlibra [emicizumab - a bispecific antibody mimicking FVIIIa], Alprolix, Nuwiq, Xyntha)
- 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 dollars per vial depending on unit strength. per vial
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to step therapy)
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 details. 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 for clarification. 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 information about the medication taken, the amount, and the time it occurred.