Eculizumab
- Atc Codes:L04AA25
- CAS Codes:219685-50-4
- PHARMGKB ID:219685-50-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Soliris; Belgium: Soliris; Bulgaria: Soliris; Denmark: Soliris; Estonia: Soliris; Finland: Soliris; France: Soliris; Germany: Soliris; Greece: Soliris; Ireland: Soliris; Italy: Soliris; Malta: Soliris; Poland: Soliris; Portugal: Soliris; Romania: Soliris; Slovakia: Soliris; Slovenia: Soliris; Spain: Soliris; Sweden: Soliris; UK: Soliris.
North America
USA: Soliris.
Drug combinations
Chemistry
Eculizumab: Mw: approx. 150000.01. Immunoglobulin, anti-(human complement C~5α~-chain)(human-mouse monoclonal 5G~1.1~ heavy chain), disulfide with human-mouse monoclonal 5G~1.1~ light chain, dimer. CAS-219685-50-4 (2002).
Pharmacologic Category
Miscellaneous Therapeutic Agents; Complement Inhibitors; Monoclonal Antibody. (ATC-Code: L04AA25).
Mechanism of action
A recombinant humanized IgG~2~/4κ monoclonal antibody. Eculizumab binds specifically and with high affinity to the complement protein C~5~, preventing activation of terminal complement components. Prevents the cleavage of complement protein C~5~ into C~5α~ and C~5β~, thereby blocking subsequent formation of the C~5β~-C~9~ terminal complement complex (also referred to as the membrane attack complex). Terminal complement-mediated intravascular hemolysis is a key clinical feature of paroxysmal nocturnal hemoglobinuria.
Therapeutic use
Treatment of paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis (designated an orphan drug by the FDA for use in this condition).
Pregnancy and lactiation implications
Animal studies have demonstrated fetal abnormalities. Human IgG is known to cross the placenta, therefore, eculizumab (a recombinant IgG molecule) may also do so. There are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if clearly needed. It is not known if eculizumab is excreted in human milk. Human IgG is excreted in breast milk, and therefore, eculizumab may also be so. Use with caution during lactation.
Unlabeled use
Contraindications
Hypersensitivity to eculizumab or any component of the formulation. Active, severe N. meningitidis infection. Patients not currently vaccinated against N. meningitidis.
Warnings and precautions
Infusion reactions, including anaphylaxis or hypersensitivity, may occur. The risk for meningococcal (Neisseria meningitidis) infections (septicemia and/or meningitis) is increased (use caution in any concurrent systemic infection). Discontinuation of treatment may increase risk for serious hemolysis. Eculizumab increases susceptibility to infections caused by encapsulated bacteria, particularly meningococcal infections. Serious infections (e.g. meningococcal sepsis) reported in some patients receiving eculizumab. Use caution in other systemic infections. High risk of venous thrombosis (potentially life-threatening or fatal) in PNH. Low titers of antibodies to eculizumab reported infrequently.