![Esperoct® [antihemophilic factor (recombinant), glycopegylated-exei] logo](/content/dam/novonordisk/novomedlink/logos/bleeding-disorders/esperoct.svg)
Extend half-life beyond the standard
In open-label clinical trials, Esperoct® achieved a longer half-life across age groups when compared to standard half-life (SHL) Factor VIII products.1
Extend half-life beyond the standard
In open-label clinical trials, Esperoct® achieved a longer half-life across age groups when compared to standard half-life (SHL) Factor VIII products.1
Longer half-life compared to SHL FVIII products
In patients ≥18 years of age
In pathfinder 1, a phase 1 study with adult patients, Esperoct® achieved a 60% longer half-life compared to SHL FVIII products.1
Keep them covered longer
Compared to other extended half-life (EHL) products, Esperoct® achieved an unprecedented 22-hour half-life in adults.2,a,b
in adults with site-directed glycoPEGylation2
aIn a phase 3, open-label study, safety, efficacy, and pharmacokinetics (PK) of Esperoct® were evaluated in previously treated patients (PTPs) aged ≥12 years with severe hemophilia A. Single-dose PK studies were performed in 42 adults after receiving Esperoct® 50 IU/kg (includes adult patients from pathfinder 2 Phase 3 trial and Phase 1 PK trials).2,3
bMean half-life in adults, compared with other EHL FVIII products; the mean half-life in adults is 19.7 hours for Eloctate®, 14.7 for Adynovate®, and 17.9-18.6 for Jivi®.4-6
In patients <12 years of age
In pathfinder 5, a phase 3 open-label study with pediatric previously treated patients, Esperoct® achieved an 85% longer half-life compared to SHL FVIII products.7
Compared with SHL FVIII products
Keep them covered longer
In pathfinder 5, a phase 3 study of children (aged <12 years), Esperoct® achieved a 14.3-hour mean half-life.2,8
mean half-life in children1,8
Achieve high trough levels in hemophilia A
The pharmacokinetics (PK) of Esperoct® were evaluated in previously treated patients with severe hemophilia A. Esperoct® achieved high factor levels in adolescents, adults, and children.2,c
cFor children aged 6-11 years, trough level is 2%.
In patients aged 12 to 70 years
In the pathfinder 2 open-label study, Esperoct® achieved factor levels ≥3% for the entire dosing interval and in PK modeling data ≥5% for 90% of the time.2
In patients aged 0 to <12 years
In the pathfinder 5 open-label study, Esperoct® achieved factor levels ≥2% for the entire dosing interval for children aged 6 to 11 years, and in PK modeling data, ≥5% for 72% of the dosing interval for children aged 0 to <12 years.2
Aged 6-11 years
Aged 0 to <12 years
dSteady-state FVIII activity profiles were estimated in 143 patients using a one-compartment model with first-order elimination with PK parameters of clearance and volume of distribution.2
eSteady-state FVIII activity profiles were estimated in 22 children using a one-compartment model with first-order elimination, including PK parameters of clearance and volume of distribution.2
Study designs
pathfinder 1 phase 1 clinical trial (Tiede, et al):
A phase 1, open-label study evaluated the safety and pharmacokinetic properties of Esperoct® in 26 PTPs. Patients received a single dose of 25, 50, or 75 IU/kg of their previous SHL product (pdFVIII or rFVIII), followed by the same dose of Esperoct®. To allow for comparison, all results were adjusted to a 50 IU/kg dose of each product.1
pathfinder 2 phase 3 clinical trial (Giangrande, et al):
In a phase 3, open-label study, safety, efficacy, and PK of Esperoct® were evaluated in previously treated patients (PTPs) aged ≥12 years with severe hemophilia A. Single-dose PK studies were performed in 42 adults after receiving Esperoct® 50 IU/kg (includes adult patients from pathfinder 2 Phase 3 trial and Phase 1 PK trials); 175 PTPs received routine prophylaxis (50 IU/kg Q4D) for 76 weeks. Steady state trough FVIII activity was measured in 143 adults and 23 adolescents (12-<18 years). Mean trough level for adults was 3.0 IU/dL, and mean trough level for adolescents (12-<18 years) was 2.7 IU/dL.2,3
pathfinder 5 phase 3 clinical trial (Meunier, et al):
In a phase 3 study of children (aged <12 years) a single-dose PK comparison was performed in 27 children between previous SHL products and Esperoct® at the same administered dose prior to the start of routine prophylaxis. Half-life comparison is based on estimated terminal half-life ratio using a population-based method. During the main phase, 68 children received prophylaxis at an average dose of approximately 65 IU/kg twice weekly for 26 weeks.7
Based on single-dose PK parameters (one-stage clotting assay) in 22 children, geometric mean terminal half-life was 14.7 hours in the younger cohort (0-5 years) and 13.8 hours in the older cohort (6-11 years). Steady state trough FVIII activity was measured in 34 children (6-11 years of age).7,8
Fixed dosing for all patients means no calculating desired FVIII activity levels.2
PEGylation technology
Esperoct® extends half-life through PEGylation.2
Selected Important Safety Information for Esperoct®
Contraindications
- Do not use in patients who have known hypersensitivity to Esperoct® or its components, including hamster proteins
Warnings and Precautions
- Hypersensitivity reactions, including anaphylaxis, may occur. Should hypersensitivity reactions occur, discontinue Esperoct® and administer appropriate treatment
Indications and Usage
Esperoct® [antihemophilic factor (recombinant), glycopegylated-exei] is indicated for use in adults and children with hemophilia A for on-demand treatment and control of bleeding episodes, perioperative management of bleeding, and routine prophylaxis to reduce the frequency of bleeding episodes
- Esperoct® is not indicated for the treatment of von Willebrand disease
Important Safety Information
Contraindications
- Do not use in patients who have known hypersensitivity to Esperoct® or its components, including hamster proteins
Warnings and Precautions
- Hypersensitivity reactions, including anaphylaxis, may occur. Should hypersensitivity reactions occur, discontinue Esperoct® and administer appropriate treatment
- Development of neutralizing antibodies (inhibitors) has occurred. Perform an assay that measures Factor VIII inhibitor concentration if bleeding is not controlled with the recommended dose of Esperoct® or if the expected plasma Factor VIII activity levels are not attained
Adverse Reactions
- The most frequently reported adverse reactions in clinical trials (≥1%) were rash, redness, itching (pruritus), and injection site reactions
Please click here for Esperoct® Prescribing Information.
References:
- Tiede A, Brand B, Fischer R, et al. Enhancing the pharmacokinetic properties of recombinant factor VIII: first-in-human trial of glycoPEGylated recombinant factor VIII in patients with hemophilia A. J Thromb Haemost. 2013;11(4):670-678.
- Esperoct [package insert]. Plainsboro, NJ: Novo Nordisk Inc; 2019.
- Giangrande P, Andreeva T, Chowdary P, et al. Clinical evaluation of glycoPEGylated recombinant FVIII: efficacy and safety in severe haemophilia A. Thromb Haemost. 2017;117(2):252-261.
- Eloctate® [package insert]. Cambridge, MA: Biogen Idec Inc.; 2020.
- Adynovate® [package insert]. Westlake Village, CA: Baxter Healthcare Corporation; 2021.
- Jivi® [package insert]. Whippany, NJ: Bayer HealthCare LLC; 2018.
- Meunier S, Alamelu J, Ehrenforth S, et al. Safety and efficacy of a glycoPEGylated rFVIII (turoctocog alpha pegol, N8-GP) in paediatric patients with severe haemophilia A. Thromb Haemost. 2017;117:1705-1713.
- Data on file. Novo Nordisk Inc; Plainsboro, NJ.