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Identification
- Summary
Susoctocog alfa is a recombinant Factor VIII used to treat and prevent bleeding in hemophilia A.
- Brand Names
- Obizur
- Generic Name
- Susoctocog alfa
- DrugBank Accession Number
- DB11606
- Background
Intravenous susoctocog alfa is a recombinant, B-domain deleted, porcine sequence antihaemophilic factor VIII (FVIII) product that has recently been approved for the treatment of bleeding episodes in adults with acquired haemophilia A (AHA). AHA is a rare bleeding disorder that results in a prolonged clotting time as measured by the activated partial thromboplastin time (aPTT) assay, a conventional in vitro test for biological activity of factor VIII. Patients with AHA have normal Factor VIII genes for coagulation pathways but develop inhibitory autoantibodies directed against Factor VIII. These autoantibodies neutralize circulating human factor VIII and create a functional deficiency of this procoagulant protein. Susoctocog alfa serves to temporarily restore the inhibited endogenous Factor VIII for effective hemostasis.
In a global, prospective, controlled, multi-center Phase 2/3 open-label clinical trial, all patients responded to susoctocog alfa treatment within 24 hours 2. Susoctocog alfa is a glycoprotein containing a 90 kDa heavy chain and a 80 kDa light chain with the naturally-occuring B domain replaced with a twenty-four amino acid linker.
Susoctocog alfa was approved by the FDA in October 2014 and is marketed under the brand name Obizur for intravenous injection. It is the first recombinant porcine FVIII treatment approved for AHA that allows physicians to manage the treatment's efficacy and safety by measuring factor VIII activity levels in addition to clinical assessments 2. The recombinant porcine sequence allows less susceptibility to inactivation by circulating human factor VIII antibodies.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Blood factors - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 170000.0 Da (Approximate, B-Domain deleted)
- Sequences
- Not Available
- Synonyms
- Antihemophilic factor (recombinant) porcine sequence
- ANTIHEMOPHILIC FACTOR (RECOMBINANT), PORCINE SEQUENCE
- Antihemophilic factor porcine, B-domain truncated recombinant
- Porcine recombinant factor VIII B-domain truncated
- RECOMBINANT DNA DERIVED B-DOMAIN DELETED PORCINE BLOODCOAGULATION FACTOR VIII ANALOGUE, PRODUCED IN BHK21 CELLS: DES-(753-1418)-BLOOD-COAGULATION FACTOR VIII (PROCOAGULANT COMPONENT) SUS SCROFA, GLYCOSYLATED
- Susoctocog alfa
Pharmacology
- Indication
Indicated for the treatment of bleeding episodes in adults with acquired hemophilia A.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Bleeding •••••••••••• - Contraindications & Blackbox Warnings
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Following susoctocog alfa administration, the activated partial thromboplastin time (aPTT) is expected to normalize indicating restored biological activity of factor VIII and normal clotting time 3. In a prospective, open-label clinical trail involving 28 subjects with acquired haemophilia A, all subjects had a positive response to treatment for the initial bleeding episodes at 24 hours after dosing where bleeding was either stopped or substantially reduced 3.
- Mechanism of action
Factor VIII circulates in the plasma as a hemostatically active protein complex that consists of factor VIII and a large carrier protein von Willebrand factor via a non-covalent binding interaction. This protein complex remains inactive until the coagulation cascade is activated which in turn activates factor VIII to be released from factor VIII/von Willebrand factor complex. Activated factor VIII acts as a cofactor for factor IX-mediated conversion of factor X to activated factor X. Activated factor X is critical in converting prothrombin into thrombin and sequentially, thrombin converts fibrinogen to fibrin for the formation of a blood clot Label.
Acquired haemophilia is a rare bleeding disorder where patients with normal Factor VIII genes spontaneously develop inhibitory autoantibodies directed against Factor VIII. These autoantibodies are IgG1 and IgG4 autoantibodies that bind to the A2, A3 and C2 domains of the FVIII molecules to inactivate them 1. The autoantibodies neutralize circulating human factor VIII and create a functional deficiency of this procoagulant protein. Susoctocog alfa serves to temporarily restore the inhibited endogenous Factor VIII for effective hemostasis. Circulating inhibitory autoantibodies have minimal or no cross-reactivity against susoctocog alfa Label.
Target Actions Organism Avon Willebrand factor bindingHumans - Absorption
The time to reach peak plasma concentrations (Tmax) is approximately 26 minutes or 0.42 hour following intravenous administration of 5000U susoctocog alfa in patients with acquired haemophilia in a non-bleeding state Label.
- Volume of distribution
Following intravenous dose of 5000U to patients with acquired haemophilia in a non-bleeding state, the volume of distribution at steady state was 30.7 U/% 3.
- Protein binding
Circulating susoctocog alfa binds to endogenous von Willebrand factor endogenously present in the circulation Label.
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
The terminal half-life ranges from 2-17 hours in a non-bleeding state. Following intravenous dose of 5000U to patients with acquired haemophilia in a non-bleeding state, the terminal half life was approximately 3.8 hours 3.
- Clearance
Following intravenous dose of 5000U to patients with acquired haemophilia in a non-bleeding state, the clearance rate was approximately 4.80 U/% * t 3.
- Adverse Effects
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Long-term studies in animals to evaluate the carcinogenic potential, genotoxicity and effects on fertility have not been performed with susoctocog alfa. In repeated-dose studies, the incidence and severity of glomerulopathy observed in monkeys intravenously administered susoctocog alfa at doses of 75, 225 and 750 U/kg/day tended to increase over time 3.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The therapeutic efficacy of Susoctocog alfa can be decreased when used in combination with Abciximab. Acenocoumarol The therapeutic efficacy of Susoctocog alfa can be decreased when used in combination with Acenocoumarol. Alpha-1-proteinase inhibitor Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Susoctocog alfa. Alteplase The therapeutic efficacy of Susoctocog alfa can be decreased when used in combination with Alteplase. Aminocaproic acid The risk or severity of adverse effects can be increased when Aminocaproic acid is combined with Susoctocog alfa. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Obizur Injection, powder, for solution 500 U Intravenous Baxalta Innovations Gmb H 2016-09-08 Not applicable EU 
Obizur Injection, powder, lyophilized, for solution; Kit 500 [USP'U]/1mL Intravenous Takeda Pharmaceuticals America, Inc. 2014-10-23 Not applicable US 
Obizur Injection, powder, for solution 500 U Intravenous Baxalta Innovations Gmb H 2016-09-08 Not applicable EU Obizur Injection, powder, for solution 500 U Intravenous Baxalta Innovations Gmb H 2016-09-08 Not applicable EU Obizur Powder, for solution 500 unit / mL Intravenous Takeda 2016-11-30 Not applicable Canada 
Categories
- ATC Codes
- B02BD14 — Susoctocog alfa
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 6892UQT2GK
- CAS number
- 1339940-90-7
References
- General References
- External Links
- PubChem Substance
- 347911216
- 1592899
- Wikipedia
- Susoctocog_alfa
- FDA label
- Download (356 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Not Yet Recruiting Not Available Hemophilia A, Acquired 1 somestatus stop reason just information to hide Not Available Recruiting Not Available Hemophilia A, Acquired 1 somestatus stop reason just information to hide 3 Terminated Treatment Hemophilia A 1 somestatus stop reason just information to hide 2, 3 Completed Treatment Hemophilia A, Acquired 1 somestatus stop reason just information to hide Not Available Completed Not Available Hemophilia A, Acquired 2 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 500 U Injection, powder, for solution Intravenous; Parenteral 500 U Injection, powder, lyophilized, for solution; kit Intravenous 500 [USP'U]/1mL Powder, for solution Intravenous 500 unit / mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binding
- General Function
- Important in the maintenance of hemostasis, it promotes adhesion of platelets to the sites of vascular injury by forming a molecular bridge between sub-endothelial collagen matrix and platelet-surface receptor complex GPIb-IX-V. Also acts as a chaperone for coagulation factor VIII, delivering it to the site of injury, stabilizing its heterodimeric structure and protecting it from premature clearance from plasma
- Specific Function
- Collagen binding
- Gene Name
- VWF
- Uniprot ID
- P04275
- Uniprot Name
- von Willebrand factor
- Molecular Weight
- 309261.83 Da
Drug created at June 22, 2016 16:51 / Updated at July 07, 2023 12:10