Explore a selection of our essential drug information below, or:
Identification
- Summary
Satralizumab is a subcutaneously injected anti-IL-6 receptor monoclonal antibody for the treatment of neuromyelitis optica spectrum disorder (NMOSD).
- Brand Names
- Enspryng
- Generic Name
- Satralizumab
- DrugBank Accession Number
- DB15762
- Background
Satralizumab is a recombinant humanized monoclonal antibody targeted against human interleukin-6 (IL-6) receptors, similar to tocilizumab, which is produced in Chinese hamster ovary cells and based on an IgG2 framework.4 Satralizumab is used in the treatment of neuromyelitis optica spectrum disorder (NMOSD), a rare autoimmune inflammatory disorder of the central nervous system (CNS) involving demyelinating lesions in the optic nerve, spinal cord, brainstem, and cerebrum.3 Some of the pro-inflammatory mechanisms involved in NMOSD are thought to be mediated, at least in part, by IL-6, including increased production of anti-aquaporin-4 (AQP4) autoantibodies and increased permeability of the blood-brain barrier, which allows for the passage of pro-inflammatory mediators into the CNS.2,3 Satralizumab is thought to exert its therapeutic benefits by blocking IL-6 receptors and, subsequently, these inflammatory responses.
Enspryng®, a satralizumab formulation developed by Chugai Pharmaceutical and Roche,4 is uniquely formulated with "recycling antibody technology" whereby the association of satralizumab to IL-6 receptors occurs in a pH-dependent manner3 - this allows satralizumab to bind an IL-6 receptor until it reaches an endosome, after which the drug may dissociate from the receptor and move back into the plasma to act again. This novel mechanism effectively increases the duration of action of satralizumab, as it allows for single drug molecules to interact with multiple endogenous IL-6 receptors prior to elimination.
Satralizumab was first approved for use in Canada in June 2020 for the treatment of AQP4 antibody-positive patients with NMOSD.3 It received subsequent approvals in Switzerland and Japan,3 and was approved for use by the FDA in August 2020,7 becoming the 3rd treatment to receive FDA approval for NMOSD (after eculizumab in June 2019 and inebilizumab in June 2020).
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 143000.0 Da
- Sequences
- Not Available
- Synonyms
- Humanised anti-IL-6 receptor monoclonal antibody
- Sapelizumab
- Satralizumab
- satralizumab-mwge
- External IDs
- SA-237
- SA237
Pharmacology
- Indication
Satralizumab is indicated for the treatment of neuromyelitis optica spectrum disorder (NMOSD) in adult patients who are anti-aquaporin-4 (AQP4) antibody positive.4 In Canada, it is also used in adolescent patients for the same indication.5
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Neuromyelitis optica spectrum disorder •••••••••••• ••••• •••••••••••••• • •••••••• •••••••• •••••••••• •••••••••• •••••••• - 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
Enspryng®, a satralizumab formulation developed by Chugai Pharmaceutical and Roche,4 utilizes a novel "recycling antibody technology" whereby the association of satralizumab to IL-6 receptors occurs in a pH-dependent manner.3 Satralizumab-bound IL-6 receptors are taken up into cells and transported into endosomes, a relatively acidic environment in comparison to plasma (pH 5.5-6.0 vs. pH 7.4) - this decrease in pH allows satralizumab to dissociate from the IL-6 receptor and be recycled back into the plasma, where it can bind to another IL-6 receptor and repeat the process.3
Satralizumab has been associated with an increased risk of infection, including serious and potentially fatal infections. It should not be administered to patients with active infections, including localized infections, until the infection resolves, and is contraindicated for use in patients with active hepatitis B or tuberculosis.4
- Mechanism of action
Interleukin-6 (IL-6) is a pro-inflammatory cytokine2 which has been implicated in the pathogenesis of NMOSD.3 The inflammatory cascade triggered by IL-6 signaling is thought to result in the differentiation of T-cells into pro-inflammatory TH17 cells3 and the differentiation of B-cells into plasmablasts producing AQP4 autoantibodies.3,2 IL-6 may also play a role in increasing the permeability of the blood-brain barrier, thereby allowing penetration of autoantibodies and pro-inflammatory mediators into the central nervous system.3,2
Satralizumab is a humanized monoclonal antibody targeted against human IL-6 receptors.4 It binds to soluble and membrane-bound IL-6 receptors and prevents the signaling cascade, and subsequent pro-inflammatory effects, associated with its binding to endogenous IL-6.
Target Actions Organism AInterleukin-6 receptor subunit alpha binderantibodyHumans - Absorption
The Cmax and AUC at steady-state, achieved after an 8-week loading period, were approximately 31.5 mcg/mL and 737 mcg.mL/day, respectively.4 Average Ctrough concentrations were approximately 19 mcg/mL.5 The bioavailability of satralizumab following subcutaneous injection has been reported to be between 78.5% and 85%.4,5
- Volume of distribution
Satralizumab is subject to biphasic distribution - the estimated volume of distribution for the central and peripheral compartments are 3.46 L and 2.07 L, respectively.5
- Protein binding
Not Available
- Metabolism
While the metabolism of satralizumab has not been studied directly,4 monoclonal antibodies as a class are principally cleared by catabolism.4,1
- Route of elimination
Monoclonal antibodies are typically eliminated via uptake into cells and subsequent catabolism via lysosomal degradation. Due to their large size, they are only eliminated renally under pathologic conditions.1
- Half-life
The terminal half-life of satralizumab is approximately 30 days (range 22-37 days).4
- Clearance
The total clearance of satralizumab is concentration-dependent and is estimated to be 0.0601-0.0679 L/day.4,5 The inter-compartmental clearance was 0.336 L/day.4
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
There is no data regarding overdose of satralizumab. No serious adverse effects were noted in healthy adults receiving a single dose of 240mg subcutaneously in clinical trials.5 Patients experiencing a suspected overdose should be treated with symptomatic and supportive measures as clinically indicated.
- 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 software1,2-Benzodiazepine The serum concentration of 1,2-Benzodiazepine can be decreased when it is combined with Satralizumab. Abatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Satralizumab. Abemaciclib The serum concentration of Abemaciclib can be decreased when it is combined with Satralizumab. Abiraterone The serum concentration of Abiraterone can be decreased when it is combined with Satralizumab. Abrocitinib The serum concentration of Abrocitinib can be decreased when it is combined with Satralizumab. - 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.- International/Other Brands
- Enspryng (Genentech)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Enspryng Solution 120 mg / mL Subcutaneous Hoffmann La Roche 2020-08-26 Not applicable Canada 
Enspryng Injection, solution 120 mg/ml Subcutaneous Roche Registration Gmb H 2021-10-08 Not applicable EU 
Enspryng Injection, solution 120 mg/1mL Subcutaneous Genentech Inc. 2020-08-14 Not applicable US 
Enspryng Injection, solution 120 mg/ml Subcutaneous Roche Registration Gmb H 2021-10-08 Not applicable EU
Categories
- ATC Codes
- L04AC19 — Satralizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunosuppressive Agents
- Interleukin Inhibitors
- Interleukin-6 Receptor Antagonist
- Proteins
- 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
- YB18NF020M
- CAS number
- 1535963-91-7
References
- General References
- Temrikar ZH, Suryawanshi S, Meibohm B: Pharmacokinetics and Clinical Pharmacology of Monoclonal Antibodies in Pediatric Patients. Paediatr Drugs. 2020 Apr;22(2):199-216. doi: 10.1007/s40272-020-00382-7. [Article]
- Duchow A, Paul F, Bellmann-Strobl J: Current and emerging biologics for the treatment of neuromyelitis optica spectrum disorders. Expert Opin Biol Ther. 2020 Sep;20(9):1061-1072. doi: 10.1080/14712598.2020.1749259. Epub 2020 Apr 13. [Article]
- Heo YA: Satralizumab: First Approval. Drugs. 2020 Aug 14. pii: 10.1007/s40265-020-01380-2. doi: 10.1007/s40265-020-01380-2. [Article]
- FDA Approved Drug Products: Enspryng (satralizumab-mwge) for subcutaneous injection [Link]
- Health Canada Product Monograph: Enspryng (satralizumab) for subcutaneous injection [Link]
- Creative BioLabs: Satralizumab Data Sheet [Link]
- FDA News Release: FDA Approves Treatment for Rare Disease Affecting Optic Nerves, Spinal Cord [Link]
- External Links
- 2391551
- Wikipedia
- Satralizumab
- FDA label
- Download (991 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 data4 Terminated Treatment Neuromyelitis Optica Spectrum Disorders 1 somestatus stop reason just information to hide 3 Active Not Recruiting Treatment Generalized Myasthenia Gravis 1 somestatus stop reason just information to hide 3 Completed Treatment Neuromyelitis Optica (NMO) / Neuromyelitis Optica Spectrum Disorders 2 somestatus stop reason just information to hide 3 Completed Treatment Neuromyelitis Optica Spectrum Disorders 1 somestatus stop reason just information to hide 3 Recruiting Treatment LGI1 Autoimmune Encephalitis / NMDAR Autoimmune Encephalitis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Subcutaneous 120 mg/ml Injection, solution Subcutaneous 120 MG Injection, solution Subcutaneous 120 mg/1mL Solution Subcutaneous 120 mg / mL Solution Subcutaneous 120 mg/1ml Injection, solution Subcutaneous 120 mg/ml Solution Subcutaneous 120 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- BinderAntibody
- General Function
- Part of the receptor for interleukin 6. Binds to IL6 with low affinity, but does not transduce a signal (PubMed:28265003). Signal activation necessitate an association with IL6ST. Activation leads to the regulation of the immune response, acute-phase reactions and hematopoiesis (PubMed:30995492, PubMed:31235509). The interaction with membrane-bound IL6R and IL6ST stimulates 'classic signaling', the restricted expression of the IL6R limits classic IL6 signaling to only a few tissues such as the liver and some cells of the immune system. Whereas the binding of IL6 and soluble IL6R to IL6ST stimulates 'trans-signaling'. Alternatively, 'cluster signaling' occurs when membrane-bound IL6:IL6R complexes on transmitter cells activate IL6ST receptors on neighboring receiver cells (Probable)
- Specific Function
- ciliary neurotrophic factor binding
- Gene Name
- IL6R
- Uniprot ID
- P08887
- Uniprot Name
- Interleukin-6 receptor subunit alpha
- Molecular Weight
- 51547.015 Da
References
- FDA Approved Drug Products: Enspryng (satralizumab-mwge) for subcutaneous injection [Link]
Drug created at August 18, 2020 19:52 / Updated at June 03, 2022 07:24