Esperoct 1000unit Inj 1 Vial
It is used to treat or prevent bleeding in people with hemophilia.
Drug Class
Antihemophilic Agent
Pharmacologic Class
Coagulation Factor VIII, 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. Hemophilia A is a genetic bleeding disorder where the blood doesn't clot properly because of a missing or faulty protein called Factor VIII. Esperoct replaces this missing protein, helping your blood to clot normally and stop bleeding.
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.
Preparing the Medication
This medication must be mixed before use. 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. If necessary, the mixed solution can be stored in the refrigerator for up to 24 hours.
Important Safety Precautions
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 use, discard any remaining medication from 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. 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.
Preparing the Medication
This medication must be mixed before use. 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. If necessary, the mixed solution can be stored in the refrigerator for up to 24 hours.
Important Safety Precautions
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 use, discard any remaining medication from 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. 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 (preventing bleeds) or on-demand treatment.
- Learn how to properly prepare and administer the injection, or ensure a caregiver is trained.
- Keep a detailed record of all infusions, including date, time, dose, and reason for infusion.
- Avoid activities that carry a high risk of injury or bleeding.
- Wear a medical alert bracelet or carry an identification card indicating you have hemophilia A.
- Maintain good dental hygiene to prevent gum bleeding.
- Discuss any planned surgeries or dental procedures with your healthcare provider well in advance.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Prophylaxis: 50 units/kg every 4 days or 65 units/kg twice weekly. On-demand treatment: 20-50 units/kg depending on bleed severity.
Dose Range:
20 - 65 mg
Condition-Specific Dosing:
prophylaxis:
50 units/kg every 4 days or 65 units/kg twice weekly
minor_bleed:
20-30 units/kg (target FVIII 40-60% of normal)
moderate_bleed:
30-40 units/kg (target FVIII 60-80% of normal)
major_bleed:
40-50 units/kg (target FVIII 80-100% of normal)
Pediatric Dosing
Neonatal:
Not established (limited data in infants <1 year)
Infant:
Dosing should be individualized based on clinical response and FVIII levels. Prophylaxis: 50 units/kg every 4 days or 65 units/kg twice weekly (for children ≥1 year).
Child:
Prophylaxis: 50 units/kg every 4 days or 65 units/kg twice weekly. On-demand treatment: Same as adult dosing based on bleed severity.
Adolescent:
Same as adult dosing.
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; 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 (turoctocog alfa pegol) is a recombinant DNA-derived coagulation Factor VIII (FVIII) concentrate that has been pegylated. It temporarily replaces the missing coagulation FVIII that is necessary 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 conversion of Factor X (FX) to activated Factor X (FXa). FXa, in turn, converts prothrombin to thrombin, which then converts fibrinogen to fibrin, leading to clot formation.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Immediate (IV administration)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
Approximately 40-60 mL/kg
ProteinBinding:
Not highly protein bound; circulates bound to von Willebrand factor (vWF)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 19 hours (terminal half-life, extended due to pegylation)
Clearance:
Approximately 2.5-3.5 mL/hr/kg
ExcretionRoute:
Primarily via proteolytic degradation and cellular uptake; not renally or hepatically excreted as intact protein.
Unchanged:
Not applicable (protein degradation)
Pharmacodynamics
OnsetOfAction:
Immediate (upon intravenous administration)
PeakEffect:
Immediate (within minutes of administration)
DurationOfAction:
Extended, allowing for less frequent dosing (up to 4 days for prophylaxis) due to pegylation.
Safety & Warnings
Side Effects
Important Side Effects to Report to Your Doctor Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. Seek immediate medical attention if you experience any of the following symptoms, which may indicate a serious allergic reaction:
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. However, many people do not experience any side effects or only have mild ones. If you experience any of the following side effects or any other symptoms that concern you or do not go away, contact your doctor:
Irritation at the injection site
Note: This is not an exhaustive list of all possible side effects. If you have questions or concerns about side effects, consult your doctor. For medical advice about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. Seek immediate medical attention if you experience any of the following symptoms, which may indicate a serious allergic reaction:
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. However, many people do not experience any side effects or only have mild ones. If you experience any of the following side effects or any other symptoms that concern you or do not go away, contact your doctor:
Irritation at the injection site
Note: This is not an exhaustive list of all possible side effects. If you have questions or concerns about side effects, consult your doctor. For medical advice about side effects, contact 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 an allergic reaction: rash, hives, itching, redness, swelling of the face, lips, tongue, or throat, difficulty breathing, chest tightness, wheezing, dizziness, lightheadedness, fainting.
- Signs of bleeding: unusual bruising, prolonged bleeding from cuts, nosebleeds, blood in urine or stools, severe headaches, joint pain or swelling, stomach pain.
- Signs of inhibitor development (if your treatment seems less effective): increased frequency or severity of bleeding episodes, or bleeding that doesn't stop with your usual dose.
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 the medications you are taking, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Any health problems you have, as they may affect the safety and efficacy of this medication.
Remember to check with your doctor before starting, stopping, or changing the dose of any medication to ensure it is safe to take with this drug and your existing health conditions.
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 the medications you are taking, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Any health problems you have, as they may affect the safety and efficacy of this medication.
Remember to check with your doctor before starting, stopping, or changing the dose of any medication to ensure it is safe to take with this drug and your existing health conditions.
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:
- While overdose is unlikely to cause acute toxicity, very high levels of Factor VIII could theoretically increase the risk of thrombotic events (blood clots), though this is rare in hemophilia patients.
- Symptoms might include signs of abnormal clotting, such as chest pain, shortness of breath, or swelling/pain in a limb.
What to Do:
In case of suspected overdose, contact your healthcare provider or emergency services immediately. Management would be supportive and aimed at monitoring for and treating any thrombotic complications. Call 1-800-222-1222 (Poison Control Center) for advice.
Drug Interactions
Monitoring
Baseline Monitoring
Factor VIII (FVIII) activity levels
Rationale: To establish baseline FVIII levels and guide initial dosing.
Timing: Prior to initiation of therapy.
FVIII inhibitor screen (Bethesda assay)
Rationale: To detect pre-existing FVIII inhibitors, which can render treatment ineffective.
Timing: Prior to initiation of therapy, especially in previously untreated patients (PUPs).
Routine Monitoring
Factor VIII (FVIII) activity levels
Frequency: Periodically, especially when adjusting dose, during major bleeding episodes, or prior to surgery.
Target: Varies based on clinical situation (e.g., 40-60% for minor bleeds, 80-100% for major bleeds/surgery).
Action Threshold: If FVIII levels are not within expected range for the dose administered, consider inhibitor development or pharmacokinetic variability.
FVIII inhibitor screen (Bethesda assay)
Frequency: Regularly (e.g., every 3-6 months) or if clinical response to treatment 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.
Signs and symptoms of hypersensitivity/allergic reactions
Frequency: During and immediately after infusion.
Target: Absence of symptoms
Action Threshold: If symptoms (e.g., rash, urticaria, dyspnea, chest tightness, hypotension) occur, discontinue infusion and provide supportive care.
Symptom Monitoring
- Signs of bleeding (e.g., joint pain/swelling, bruising, prolonged bleeding from cuts, blood in urine/stools, nosebleeds, headaches)
- Signs of allergic reaction (e.g., rash, hives, itching, swelling of face/lips/tongue, difficulty breathing, chest tightness, dizziness, fainting)
- Signs of inhibitor development (e.g., increased frequency or severity of bleeding, lack of response to usual doses of Esperoct)
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 only if clearly needed and the potential benefits outweigh the potential risks to the fetus. Hemophilia A is a genetic disorder, and management during pregnancy should be carefully considered.
Trimester-Specific Risks:
First Trimester:
Risk unknown. Factor VIII does not cross the placenta in significant amounts.
Second Trimester:
Risk unknown.
Third Trimester:
Risk unknown. Close monitoring of FVIII levels may be necessary, especially near delivery.
Lactation
It is unknown 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 and unlikely to be absorbed intact by the infant.
Infant Risk:
Low risk, but caution advised due to lack of data.
Pediatric Use
Approved for use in pediatric patients 1 year and older. Dosing is individualized based on weight, FVIII levels, and clinical response. Children may require higher doses or more frequent administration due to higher clearance rates compared to adults, though pegylation helps extend half-life. Inhibitor development is a significant concern, 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. Dosing should be individualized based on clinical response and FVIII levels. No specific dose adjustments are generally required based on age alone, but age-related comorbidities should be considered.
Clinical Information
Clinical Pearls
- Esperoct offers 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 activity levels and monitor for inhibitor development, especially if the clinical response to treatment is suboptimal.
- Patients should be educated on the signs of allergic reactions and inhibitor development, and instructed to seek immediate medical attention if these occur.
- Proper storage (refrigerated or at room temperature for a limited period) and reconstitution are crucial for product efficacy and safety.
- This product is for intravenous administration only. Do not administer subcutaneously or intramuscularly.
Alternative Therapies
- Other recombinant Factor VIII products (e.g., Advate, Eloctate, Adynovate, Jivi, Nuwiq, Recombinate, 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 [Hemlibra])
- Desmopressin (DDAVP) for mild hemophilia A
Cost & Coverage
Average Cost:
Highly variable, typically several thousand to tens of thousands of dollars per vial depending on unit strength and quantity. Factor products are among the most expensive drugs. per 1000 units 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 promptly. To ensure safe and effective treatment, 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 for more information. If you have any questions or concerns about your 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 details about the medication taken, the amount, and the time it happened.