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Identification
- Summary
Reslizumab is an IL-5 antagonist used as an add-on maintenance treatment of patients with severe eosinophilic asthma in adults.
- Brand Names
- Cinqair
- Generic Name
- Reslizumab
- DrugBank Accession Number
- DB06602
- Background
Reslizumab is a humanized interleukin-5 (IL-5) antagonist monoclonal antibody (IgG4 kappa) that is produced by recombinant DNA technology in murine myeloma non-secreting 0 (NS0) cells. IL-5 is a pro-inflammatory cytokine that is responsible for the growth and differentiation, recruitment, activation, and survival of eosinophils Label. Elevated levels of eosinophils increase the risk for asthma exacerbations, including both allergic forms and nonallergic forms of asthma where eosinophilia is prominent. By targeting the IL-5 and disrupting its signalling pathways, reslizumab aims to inhibit eosinophil maturation and promote programmed cell death 2.
Asthma is a chronic respiratory disease that causes inflammation in the lungs with asthma attacks that lead to severe breathing difficulties. Patients often experience persistent or exacerbating symptoms overtime despite conventional first-line therapies available. Inflammation-predominant asthma, which is chatacterized by eosinophilic infiltration of airway mucosa and elevated levels of eosinophils in the blood, sputum and BAL fluid, is associated with an increased risk for recurrent exacerbation and asthma-related hospitalizations 3. In four double-blind, randomized, placebo‑controlled trials in patients with severe asthma on currently available therapies, patients receiving reslizumab had fewer asthma attacks, and a longer time to the first attack compared to patients receiving placebo Label,3. In addition, a significant improvement in lung function was seen, as measured by the volume of air exhaled by patients in one second 4. Studies demonstrated that reslizumab was not effective in various asthma outcomes in patients without eosinophilia 1.
Reslizumab was developed by Teva Pharmaceuticals. Approved by the FDA in March 2016, reslizumab is marketed under the brand name Cinqair for intravenous injection. It is injected once every four weeks via intravenous infusion. Cinqair is indicated as an add-on maintenance therapy for adults with severe asthma with an eosinophilic phenotype. It is approved for patients who have a history of severe asthma attacks (exacerbations) despite receiving their current asthma medicines. Reslizumab is marketed as Cinqaero in Europe.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- 147000.0 Da (Approximate)
- Sequences
- Not Available
- Synonyms
- Reslizumab
- External IDs
- CEP-38072
- DCP 835
- DCP-835
- SCH-55700
- SCH55700
Pharmacology
- Indication
Indicated for the add-on maintenance treatment of patients with severe asthma aged 18 years and older with an eosinophilic phenotype.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Adjunct therapy in treatment of Severe eosinophilic asthma •••••••••••• ••••• - Contraindications & Blackbox Warnings
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A reduction in blood eosinophil counts was observed in clinical studies following an initial infusion of 3 mg/kg reslizumab and was maintained through 52 weeks of treatment with no signs of tachyphylaxis. Greater reductions of blood eosinophils were observed in subjects with higher reslizumab serum concentrations. This effect was independent of the presence of treatment-emergent anti-reslizumab antibodies Label.
- Mechanism of action
Reslizumab an interleukin-5 (IL-5) antagonist (IgG4, kappa) that binds to IL-5 with a dissociation constant of 81 pM. IL-5 is a proinflammatory cytokine responsible for the terminal maturation of eosinophils and increases chemotaxis, endothelial adhesion, activation and survival of eosinophils. Eosinophils are known to play a central role in the pathophysiology of many patients with asthma; upon activation, eosinophils release leukotrienes, platelet activation factor, major basic protein, eosinophil cationic protein, eosinophil peroxidase, eosinophil-derived neurotoxin, and other cytokines that are cytotoxic to the bronchial epithelium and lead to airway inflammation and bronchospasm 1. IL-5 production is increased by upon activation of TH2 lymphocytes after antigen exposure and IL-5 stimulates the production and maturation of eosinophil precursors in the bone marrow 1. IL-5 promotes the growth and differentiation, recruitment, activation, and survival of eosinophils via interacting with the IL-5 receptor expressed on the eosinophil surface Label. Increased production and activation of eosinophils is especially prominent in nonallergic forms of asthma 1.
Reslizumab is a humanized monoclonal antibody that occupies the region ERRR (glutamic acid, arginine, arginine, arginine) corresponding to amino acids 89–92 on IL-5, which is a region critical for its interaction with the IL-5 receptor on the eosinophil surface 1. By binding to IL-5 and disrupting its binding to the alpha chain of the IL-5 receptor complex, reslizumab inhibits the bioactivity of IL-5 and attenuates IL-5 signaling. Blocking of IL-5 signalling thereby reduces the production and survival of eosinophils and inhibits eosinophilic-driven inflammation.
Target Actions Organism AInterleukin-5 antagonistregulatorHumans - Absorption
The peak serum concentrations of reslizumab were typically observed at the end of the infusion with the serum concentrations gradually declining from the peak in a biphasic manner. Following multiple doses, serum concentrations of reslizumab accumulated approximately 1.5 to 1.9-fold. Interindividual variability in peak and overall exposure across healthy individuals, patients with asthma, and other populations in pharmacokinetic studies was around 20-30% Label. Systemic exposure to reslizumab appeared to be unaffected by the presence of treatment-emergent anti-reslizumab antibodies.
- Volume of distribution
The approximate volume of distribution of reslizumab is 5L, suggesting minimal distribution to the extravascular tissues Label.
- Protein binding
Not Available
- Metabolism
Like other monoclonal antibodies, reslizumab is assumed to undergo enzymatic proteolysis into smaller peptides and amino acids. As reslizumab bind to the target, it is not expected to undergo a target-mediated clearance Label.
- Route of elimination
Not Available
- Half-life
The half-life is approximately 24 days Label.
- Clearance
Reslizumab clearance was approximately 7 mL/hour Label.
- Adverse Effects
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Single doses of up to 732 mg have been administered intravenously to subjects in clinical trials without evidence of dose-related toxicities. There is no specific treatment for an overdose with reslizumab. If the event of an overdose, the patient should be treated supportively with appropriate monitoring as necessary Label.
Based on the findings of a 6-month bioassay, reslizumab showed no evidence of carcinogenicity. In a fertility study, administration of reslizumab to parental mice at doses up to 50 mg/kg (approximately 6 times the MRHD on an AUC basis) had no effects on male or female mating or fertility. The malignancy risk of reslizumab in humans with effects on tumor growth is not yet established Label.
- 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 risk or severity of adverse effects can be increased when Abciximab is combined with Reslizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Reslizumab. Aducanumab The risk or severity of adverse effects can be increased when Reslizumab is combined with Aducanumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Reslizumab. Alirocumab The risk or severity of adverse effects can be increased when Reslizumab is combined with Alirocumab. - 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 Cinqaero Injection, solution, concentrate 10 mg/mL Intravenous Teva B.V. 2020-12-16 Not applicable EU 
Cinqaero Injection, solution, concentrate 10 mg/mL Intravenous Teva B.V. 2016-09-08 Not applicable EU Cinqaero Injection, solution, concentrate 10 mg/mL Intravenous Teva B.V. 2020-12-16 Not applicable EU Cinqaero Injection, solution, concentrate 10 mg/mL Intravenous Teva B.V. 2020-12-16 Not applicable EU Cinqair Solution 10 mg / mL Intravenous TEVA Canada Limited 2016-12-19 Not applicable Canada 
Categories
- ATC Codes
- R03DX08 — Reslizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Anti-Asthmatic Agents
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Blood Proteins
- Drugs for Obstructive Airway Diseases
- Globulins
- Immunoglobulins
- Immunoproteins
- Interleukin Antagonists
- Interleukin-5 Antagonist
- Proteins
- Respiratory System Agents
- 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
- Not Available
Chemical Identifiers
- UNII
- 35A26E427H
- CAS number
- 241473-69-8
References
- General References
- Maselli DJ, Velez MI, Rogers L: Reslizumab in the management of poorly controlled asthma: the data so far. J Asthma Allergy. 2016 Aug 31;9:155-62. doi: 10.2147/JAA.S94164. eCollection 2016. [Article]
- Castro M, Zangrilli J, Wechsler ME, Bateman ED, Brusselle GG, Bardin P, Murphy K, Maspero JF, O'Brien C, Korn S: Reslizumab for inadequately controlled asthma with elevated blood eosinophil counts: results from two multicentre, parallel, double-blind, randomised, placebo-controlled, phase 3 trials. Lancet Respir Med. 2015 May;3(5):355-66. doi: 10.1016/S2213-2600(15)00042-9. Epub 2015 Feb 23. [Article]
- Bjermer L, Lemiere C, Maspero J, Weiss S, Zangrilli J, Germinaro M: Reslizumab for Inadequately Controlled Asthma With Elevated Blood Eosinophil Levels: A Randomized Phase 3 Study. Chest. 2016 Oct;150(4):789-798. doi: 10.1016/j.chest.2016.03.032. Epub 2016 Apr 4. [Article]
- FDA approves Cinqair to treat severe asthma [Link]
- External Links
- PubChem Substance
- 347910352
- 1746889
- Wikipedia
- Reslizumab
- FDA label
- Download (416 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 Asthma 1 somestatus stop reason just information to hide Not Available Unknown Status Not Available Asthma 1 somestatus stop reason just information to hide Not Available Withdrawn Not Available Asthma / Chronic Sinusitis / Nasal Polyps 1 somestatus stop reason just information to hide 4 Completed Treatment Eosinophilic Asthma 1 somestatus stop reason just information to hide 4 Terminated Treatment Asthma 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution, concentrate Intravenous 10 MG/ML Injection, solution, concentrate Intravenous 10 mg/1mL Solution Intravenous 10 mg / mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AntagonistRegulator
- General Function
- Homodimeric cytokine expressed predominantly by T-lymphocytes and NK cells that plays an important role in the survival, differentiation, and chemotaxis of eosinophils (PubMed:2653458, PubMed:9010276). Acts also on activated and resting B-cells to induce immunoglobulin production, growth, and differentiation (By similarity). Mechanistically, exerts its biological effects through a receptor composed of IL5RA subunit and the cytokine receptor common subunit beta/CSF2RB (PubMed:1495999, PubMed:22528658). Binding to the receptor leads to activation of various kinases including LYN, SYK and JAK2 and thereby propagates signals through the RAS-MAPK and JAK-STAT5 pathways respectively (PubMed:7613138)
- Specific Function
- cytokine activity
- Gene Name
- IL5
- Uniprot ID
- P05113
- Uniprot Name
- Interleukin-5
- Molecular Weight
- 15237.695 Da
References
- Agarwal A, Spath D, Sherris DA, Kita H, Ponikau JU: Therapeutic Antibodies for Nasal Polyposis Treatment: Where Are We Headed? Clin Rev Allergy Immunol. 2020 Oct;59(2):141-149. doi: 10.1007/s12016-019-08734-z. [Article]
Drug created at March 19, 2008 16:40 / Updated at June 03, 2022 07:24