Dupilumab

Identification

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Name
Dupilumab
Accession Number
DB12159
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

Dupilumab injection to treat adults with moderate-to-severe eczema (atopic dermatitis). Dupilumab is intended for patients whose eczema is not controlled adequately by topical therapies, or those for whom topical therapies are not advisable. Dupilumab can be used with or without topical corticosteroids. FDA approval on March 28, 2017.

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
Not Available
Synonyms
  • Dupilumab
External IDs
REGN 668 / REGN-668 / REGN668 / SAR 231893 / SAR-231893 / SAR231893
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DupixentInjection, solution200 mg/1.14mLSubcutaneoussanofi-aventis U.S. LLC2018-10-19Not applicableUs
DupixentInjection, solution300 mg/2mLSubcutaneoussanofi-aventis U.S. LLC2017-03-28Not applicableUs
DupixentInjection, solution300 mg/2mLSubcutaneoussanofi-aventis U.S. LLC2017-03-28Not applicableUs
DupixentSolution150 mgSubcutaneousSanofi Aventis2018-02-06Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
420K487FSG
CAS number
1190264-60-8

Pharmacology

Indication

Dupilumab is a monoclonal antibody designed for the treatment of atopic diseases such as eczema.

Associated Conditions
Pharmacodynamics

Consistent with receptor blockade, serum levels of IL-4 and IL-13 were increased following dupilumab treatment. The relationship between the pharmacodynamic activity and the mechanism(s) by which dupilumab exerts its clinical effects is unknown.

Mechanism of action

It binds to the alpha subunit of the interleukin-4 receptor (IL-4Rα). By binding IL-4Rα the agent is subsequently capable of modulating signals associated with both the interleukin 4 and interleukin 13 process routes.

TargetActionsOrganism
AInterleukin-4 receptor subunit alpha
antagonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Following an initial subcutaneous (SC) dose of 600 mg, dupilumab reached peak mean ±SD concentrations (Cmax) of 70.1±24.1 mcg/mL by approximately 1 week post dose. Steady-state concentrations were achieved by Week 16 following the administration of 600 mg starting dose and 300 mg dose either weekly (twice the recommended dosing frequency) or every other week. Across clinical trials, the mean ±SD steady-state trough concentrations ranged from 73.3±40.0 mcg/mL to 79.9±41.4 mcg/mL for 300 mg administered every 2 weeks and from173±75.9 mcg/mL to 193±77.0 mcg/mL for 300 mg administered weekly. The bioavailability of dupilumab following a SC dose is estimated to be 64%.

Volume of distribution

4.8±1.3 L

Protein binding
Not Available
Metabolism
Not Available
Route of elimination

The metabolic pathway of dupilumab has not been characterized. As a human monoclonal IgG4 antibody, dupilumab is expected to be degraded into small peptides and amino acids viacatabolic pathways in the same manner as endogenous IgG. After the last steady-state dose of300 mg Q2W or 300 mg QW dupilumab, the median times to non-detectable concentration (<78 ng/mL) are 10 and 13 weeks, respectively.

Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Dupilumab.
AbituzumabThe risk or severity of adverse effects can be increased when Dupilumab is combined with Abituzumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Dupilumab.
AdecatumumabThe risk or severity of adverse effects can be increased when Adecatumumab is combined with Dupilumab.
AducanumabThe risk or severity of adverse effects can be increased when Dupilumab is combined with Aducanumab.
AfelimomabThe risk or severity of adverse effects can be increased when Afelimomab is combined with Dupilumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Dupilumab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Dupilumab.
AmatuximabThe risk or severity of adverse effects can be increased when Dupilumab is combined with Amatuximab.
AMG 108The risk or severity of adverse effects can be increased when AMG 108 is combined with Dupilumab.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Evidence Level

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
  1. Wenzel S, Ford L, Pearlman D, Spector S, Sher L, Skobieranda F, Wang L, Kirkesseli S, Rocklin R, Bock B, Hamilton J, Ming JE, Radin A, Stahl N, Yancopoulos GD, Graham N, Pirozzi G: Dupilumab in persistent asthma with elevated eosinophil levels. N Engl J Med. 2013 Jun 27;368(26):2455-66. doi: 10.1056/NEJMoa1304048. Epub 2013 May 21. [PubMed:23688323]
  2. FDA Approval [Link]
External Links
PubChem Substance
347911292
Wikipedia
Dupilumab
ATC Codes
D11AH05 — Dupilumab
AHFS Codes
  • 84:92.00 — Misc. Skin and Mucous Membrane Agents
FDA label
Download (2.38 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentRhinosinusitis Chronic / Sleep Apnea Syndrome1
1CompletedBasic ScienceAtopic Dermatitis (AD)1
1CompletedTreatmentAtopic Dermatitis (AD) / Atopic disorders1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentSkin Inflammation1
1RecruitingTreatmentAsthma, Allergic1
1, 2CompletedTreatmentAtopic Dermatitis (AD)1
2Active Not RecruitingTreatmentAsthma Bronchial1
2CompletedTreatmentAsthma Bronchial2
2CompletedTreatmentAtopic Dermatitis (AD)6
2CompletedTreatmentOesophagitis, Eosinophilic1
2CompletedTreatmentPolyps, Nasal1
2Not Yet RecruitingTreatmentChronic Hand Eczema1
2Not Yet RecruitingTreatmentEosinophilic Gastritis / Eosinophilic Gastroenteritis1
2Not Yet RecruitingTreatmentFood Allergy / Hypersensitivity / Hypersensitivity, Food / Peanut Allergies / Peanut Hypersensitivity1
2Not Yet RecruitingTreatmentProstate Cancer1
2RecruitingTreatmentAllergic Rhinitis (AR)1
2RecruitingTreatmentAlopecia Areata (AA)1
2RecruitingTreatmentAspirin-exacerbated Respiratory Disease1
2RecruitingTreatmentAtopic Dermatitis (AD)1
2RecruitingTreatmentCholinergic Urticaria1
2RecruitingTreatmentChronic Spontaneous Urticaria / Recurrent Angioedema1
2RecruitingTreatmentPeanut Allergies2
2, 3Active Not RecruitingTreatmentAsthma Bronchial1
2, 3RecruitingTreatmentAtopic Dermatitis (AD)1
3Active Not RecruitingTreatmentAtopic Dermatitis (AD)1
3Active Not RecruitingTreatmentPolyps, Nasal1
3CompletedTreatmentAsthma Bronchial2
3CompletedTreatmentAtopic Dermatitis (AD)5
3CompletedTreatmentAtopic Dermatitis (AD) / Dermatitis, Dermatitis Atopic / Disease, Eczematous Skin / Diseases Genetic, Genetic / Diseases Inborn, Skin / Eczema, Skin Diseases, Skin / Hypersensitivity, Immediate / Hypersensitivity, Immune System Diseases / Moderate-to-Severe Atopic Dermatiti / Moderate-to-severe Atopic Dermatitis1
3CompletedTreatmentPolyps, Nasal1
3Enrolling by InvitationTreatmentAtopic Dermatitis (AD)2
3Not Yet RecruitingTreatmentAsthma Bronchial1
3RecruitingTreatmentAsthma Bronchial3
3RecruitingTreatmentAtopic Dermatitis (AD)2
3RecruitingTreatmentAtopic Dermatitis (AD) / Dermatitis, Eczematous / Genetic Diseases, Inborn / Hypersensitivity / Hypersensitivity, Immediate / Immune System Diseases / Skin Diseases / Skin Diseases, Eczematous / Skin Diseases, Genetic / Skin Inflammation1
3RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)1
3RecruitingTreatmentOesophagitis, Eosinophilic1
4Not Yet RecruitingTreatmentAsthma Bronchial1
4Not Yet RecruitingTreatmentDermatitis, Allergic Contact1
4RecruitingTreatmentAtopic Dermatitis (AD)1
4RecruitingTreatmentAtopic Dermatitis (AD) / Atopic Dermatitis Eczema1
4RecruitingTreatmentAtopic Dermatitis (AD) / Atopic Dermatitis and Related Conditions / Atopic Dermatitis Eczema / Dermatitis, Eczematous1
Not AvailableApproved for MarketingNot AvailableAsthma Bronchial1
Not AvailableEnrolling by InvitationNot AvailableAtopic Dermatitis (AD)1
Not AvailableNot Yet RecruitingNot AvailableAdverse Pregnancy Outcomes / Atopic Dermatitis (AD)1
Not AvailableRecruitingNot AvailableAtopic Dermatitis (AD)1
Not AvailableRecruitingNot AvailableAtopic Dermatitis (AD) / Psoriasis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous200 mg/1.14mL
Injection, solutionSubcutaneous300 mg/2mL
SolutionSubcutaneous150 mg
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available

Taxonomy

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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor signaling protein activity
Specific Function
Receptor for both interleukin 4 and interleukin 13. Couples to the JAK1/2/3-STAT6 pathway. The IL4 response is involved in promoting Th2 differentiation. The IL4/IL13 responses are involved in regu...
Gene Name
IL4R
Uniprot ID
P24394
Uniprot Name
Interleukin-4 receptor subunit alpha
Molecular Weight
89657.42 Da
References
  1. Wenzel S, Ford L, Pearlman D, Spector S, Sher L, Skobieranda F, Wang L, Kirkesseli S, Rocklin R, Bock B, Hamilton J, Ming JE, Radin A, Stahl N, Yancopoulos GD, Graham N, Pirozzi G: Dupilumab in persistent asthma with elevated eosinophil levels. N Engl J Med. 2013 Jun 27;368(26):2455-66. doi: 10.1056/NEJMoa1304048. Epub 2013 May 21. [PubMed:23688323]

Drug created on October 20, 2016 15:30 / Updated on May 20, 2019 14:46