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Identification
- Summary
Eculizumab is a recombinant humanized monoclonal antibody used to reduce the risk of hemolysis in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).
- Brand Names
- Soliris
- Generic Name
- Eculizumab
- DrugBank Accession Number
- DB01257
- Background
Eculizumab is a monoclonal antibody that targets complement protein C5.7,1 Binding to this protein prevents the activation of a complement terminal complex, which is used to treat a number of autoimmune conditions.7,1,2
Eculizumab was granted FDA approval on 16 March 2007.7 In Q1 2023, the EMA's Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion of two formulations of eculizumab indicated for the treatment of paroxysmal nocturnal hemoglobinuria.9,10
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- 148000.0 Da
- Sequences
- Not Available
- Synonyms
- Eculizumab
- External IDs
- 5G1.1
- H5G1-1
- H5G1.1
- H5G11
Pharmacology
- Indication
Eculizumab is indicated in the US to treat paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis, atypical hemolytic uremic syndrome to inhibit complement-mediated thrombotic microangiopathy, and neuromyelitis optica spectrum disorder (NMOSD).6,2 It is also indicated in EU to treat PNH in both adult and pediatric patients.11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Generalized myasthenia gravis •••••••••••• ••••• •••••••••••••••••• •••••••• •••••••• •••••••• ••••••••• Treatment of Neuromyelitis optica spectrum disorder •••••••••••• ••••• •••••••••••••• • •••••••• •••••••• ••••••••• Treatment of Paroxysmal nocturnal haemoglobinuria (pnh) •••••••••••• •••••• ••••••••• ••••••••• Management of Paroxysmal nocturnal hemoglobinuria •••••••••••• ••••••••• Management of Thrombotic microangiopathies •••••••••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Eculizumab is a monoclonal antibody that prevents the activation of terminal complement in some autoimmune conditions.7,1,2 Eculizumab has a long duration of action.7 Patients taking this medication should be vaccinated against Neisseria meningiditis as serious meningococcal infections have occurred in the past.7,2
- Mechanism of action
Eculizumab is a monoclonal antibody that targets complement protein C5, preventing cleavage to C5a and C5b, and the formation of the terminal complement complex C5b-9.7,1,2 Inhibition of this complex prevents complement mediated intravascular hemolysis in paroxysmal nocturnal hemoglobunuria, complement mediated microangiopathy in atypical hemolytic uremic syndrome, and immune mediated inflammation and damage of the central nervous system in neuromyelitis optica spectrum disorder.7,6,2
Target Actions Organism AComplement C5 antibodyHumans - Absorption
Eculizumab is administered by intravenous infusion so the bioavailability is 100%.7 This drug reaches a Cmax of 194±76µg/mL and Ctrough of 97±60µg/mL.7 The AUC was calculated to be 24,467.6µg*h/mL.4
- Volume of distribution
The volume of distribution of eculizumab is 5-8L.7
- Protein binding
Though protein binding data is scarce, eculizumab is unlikely to be protein bound as it is a monoclonal antibody.
- Metabolism
Eculizumab is a monoclonal antibody and is expected to be metabolized to small peptides and amino acids.4,5
- Route of elimination
Monoclonal antibodies are not eliminated in the urine, and only a small amount is excreted in bile.5 Most monoclonal antibodies are catabolized in lysosomes to amino acids.5
- Half-life
- Clearance
Pharmacokinetic properties in healthy patients have not been determined.4 In patients with rhematoid arthritis, there is an average clearance of 0.26mL/kg/h.4
- Adverse Effects
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Overdoses of eculizumab are unlikely as it is administered under specialist supervision.8 In case of overdose, contact local poison control.8
- 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 softwareAbatacept The risk or severity of adverse effects can be increased when Eculizumab is combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Eculizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Eculizumab. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Eculizumab. Aducanumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Aducanumab. - 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 Bekemv Injection, solution, concentrate 300 mg Intravenous Amgen Technology (Ireland) Uc 2023-05-16 Not applicable EU 
Epysqli Injection, solution, concentrate 10 mg/ml Intravenous Samsung Bioepis Nl B.V. 2023-06-09 Not applicable EU Soliris Injection, solution, concentrate 300 mg Intravenous Alexion Europe Sas 2016-09-08 Not applicable EU Soliris Solution 10 mg / mL Intravenous Alexion Pharma Gmbh 2009-05-25 Not applicable Canada 
Soliris Injection, solution, concentrate 300 mg/30mL Intravenous Alexion Pharmaceuticals Inc. 2007-04-02 Not applicable US 
Categories
- ATC Codes
- L04AJ01 — Eculizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Complement C5 inhibitors
- Complement Inactivating Agents
- Globulins
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Immunotherapy
- Proteins
- Selective Immunosuppressants
- Serum Globulins
- 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
- Humans and other mammals
Chemical Identifiers
- UNII
- A3ULP0F556
- CAS number
- 219685-50-4
References
- General References
- Thomas TC, Rollins SA, Rother RP, Giannoni MA, Hartman SL, Elliott EA, Nye SH, Matis LA, Squinto SP, Evans MJ: Inhibition of complement activity by humanized anti-C5 antibody and single-chain Fv. Mol Immunol. 1996 Dec;33(17-18):1389-401. [Article]
- Dmytrijuk A, Robie-Suh K, Cohen MH, Rieves D, Weiss K, Pazdur R: FDA report: eculizumab (Soliris) for the treatment of patients with paroxysmal nocturnal hemoglobinuria. Oncologist. 2008 Sep;13(9):993-1000. doi: 10.1634/theoncologist.2008-0086. Epub 2008 Sep 10. [Article]
- Rother RP, Rollins SA, Mojcik CF, Brodsky RA, Bell L: Discovery and development of the complement inhibitor eculizumab for the treatment of paroxysmal nocturnal hemoglobinuria. Nat Biotechnol. 2007 Nov;25(11):1256-64. [Article]
- Wijnsma KL, Ter Heine R, Moes DJAR, Langemeijer S, Schols SEM, Volokhina EB, van den Heuvel LP, Wetzels JFM, van de Kar NCAJ, Bruggemann RJ: Pharmacology, Pharmacokinetics and Pharmacodynamics of Eculizumab, and Possibilities for an Individualized Approach to Eculizumab. Clin Pharmacokinet. 2019 Jul;58(7):859-874. doi: 10.1007/s40262-019-00742-8. [Article]
- Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29. [Article]
- FDA: Eculizumab New Indication [Link]
- FDA Approved Drug Products: Eculizumab Intravenous Infusion [Link]
- Alexion Pharma: Soliris Product Monograph [Link]
- CHMP Summary of Positive Opinion: Bekemv (eculizumab) [Link]
- CHMP Summary of Positive Opinion: Epysqli (eculizumab) [Link]
- EMA Approved Drug Products: Epysqli (Eculizumab) solution for infusion [Link]
- FDA Approved Drug Products: SOLIRIS (eculizumab) injection, for intravenous use [Link]
- External Links
- PubChem Substance
- 46505429
- 591781
- ChEMBL
- CHEMBL1201828
- Therapeutic Targets Database
- DAP000967
- PharmGKB
- PA164776637
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Eculizumab
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 data4 Completed Treatment Atypical Hemolytic Uremic Syndrome(aHUS) 1 somestatus stop reason just information to hide 4 Completed Treatment Paroxysmal Hemoglobinuria 1 somestatus stop reason just information to hide 4 Completed Treatment Paroxysmal Nocturnal Hemoglobinuria (PNH) 1 somestatus stop reason just information to hide 3 Active Not Recruiting Treatment Atypical Hemolytic Uremic Syndrome(aHUS) 1 somestatus stop reason just information to hide 3 Active Not Recruiting Treatment Paroxysmal Nocturnal Hemoglobinuria (PNH) 3 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Alexion Pharmaceuticals Inc.
- Ben Venue Laboratories Inc.
- Dosage Forms
Form Route Strength Injection, solution, concentrate Intravenous 300 mg Injection, solution, concentrate 300 mg/30ml Solution, concentrate Intravenous 10 mg Solution, concentrate Intravenous 1000000 mg Injection, solution, concentrate Intravenous 10 mg/ml Injection, solution, concentrate Intravenous 300 mg/30mL Injection, solution, concentrate Intravenous; Parenteral 300 MG Solution Intravenous 10 mg / mL Solution, concentrate Intravenous 300 mg Injection, solution, concentrate Parenteral 300 mg/30ml Solution Intravenous 300 mg - Prices
Unit description Cost Unit Soliris 300 mg/30 ml vial 210.0USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2189015 No 2010-04-13 2015-04-30 Canada
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Activation of C5 by a C5 convertase initiates the spontaneous assembly of the late complement components, C5-C9, into the membrane attack complex. C5b has a transient binding site for C6. The C5b-C6 complex is the foundation upon which the lytic complex is assembled
- Specific Function
- Chemokine activity
- Gene Name
- C5
- Uniprot ID
- P01031
- Uniprot Name
- Complement C5
- Molecular Weight
- 188303.705 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Singer AL, Locke JE, Stewart ZA, Lonze BE, Hamilton JP, Scudiere JR, Anders RA, Rother RP, Brodsky RA, Cameron AM: Successful liver transplantation for Budd-Chiari syndrome in a patient with paroxysmal nocturnal hemoglobinuria treated with the anti-complement antibody eculizumab. Liver Transpl. 2009 May;15(5):540-3. doi: 10.1002/lt.21714. [Article]
- Kelly R, Richards S, Hillmen P, Hill A: The pathophysiology of paroxysmal nocturnal hemoglobinuria and treatment with eculizumab. Ther Clin Risk Manag. 2009;5:911-21. Epub . [Article]
- Dmytrijuk A, Robie-Suh K, Cohen MH, Rieves D, Weiss K, Pazdur R: FDA report: eculizumab (Soliris) for the treatment of patients with paroxysmal nocturnal hemoglobinuria. Oncologist. 2008 Sep;13(9):993-1000. doi: 10.1634/theoncologist.2008-0086. Epub 2008 Sep 10. [Article]
- Rother RP, Rollins SA, Mojcik CF, Brodsky RA, Bell L: Discovery and development of the complement inhibitor eculizumab for the treatment of paroxysmal nocturnal hemoglobinuria. Nat Biotechnol. 2007 Nov;25(11):1256-64. [Article]
- Luzzatto L, Risitano AM, Notaro R: Paroxysmal nocturnal hemoglobinuria and eculizumab. Haematologica. 2010 Apr;95(4):523-6. doi: 10.3324/haematol.2009.017848. [Article]
- Hillmen P, Young NS, Schubert J, Brodsky RA, Socie G, Muus P, Roth A, Szer J, Elebute MO, Nakamura R, Browne P, Risitano AM, Hill A, Schrezenmeier H, Fu CL, Maciejewski J, Rollins SA, Mojcik CF, Rother RP, Luzzatto L: The complement inhibitor eculizumab in paroxysmal nocturnal hemoglobinuria. N Engl J Med. 2006 Sep 21;355(12):1233-43. [Article]
- Hillmen P, Muus P, Duhrsen U, Risitano AM, Schubert J, Luzzatto L, Schrezenmeier H, Szer J, Brodsky RA, Hill A, Socie G, Bessler M, Rollins SA, Bell L, Rother RP, Young NS: Effect of the complement inhibitor eculizumab on thromboembolism in patients with paroxysmal nocturnal hemoglobinuria. Blood. 2007 Dec 1;110(12):4123-8. Epub 2007 Aug 16. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at May 16, 2007 16:57 / Updated at June 20, 2023 09:00