Details of the Drug

General Information of Drug (ID: DMOAD2Y)

Drug Name

Dupilumab

Synonyms

REGN-668; REGN-668); Anti-IL-4 monoclonal antibody (asthma/atopic dermatitis), sanofi-aventis; Anti-IL-4 receptor antibody (VelocImmune, allergy/immune disorder), Regeneron/sanofi-aventis

Indication

Disease Entry	ICD 11	Status	REF
Atopic dermatitis	EA80	Approved	[1]
Asthma	CA23	Phase 3	[2], [3]

Drug Type

Antibody

Sequence

>heavy chain
EVQLVESGGGLEQPGGSLRLSCAGSGFTFRDYAMTWVRQAPGKGLEWVSSISGSGGNTYY
ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCAKDRLSITIRPRYYGLDVWGQGTT
VTVSSASTKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPA
VLQSSGLYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFL
GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQ
FNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQ
EEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKS
RWQEGNVFSCSVMHEALHNHYTQKSLSLSLG
>light chain
DIVMTQSPLSLPVTPGEPASISCRSSQSLLYSIGYNYLDWYLQKSGQSPQLLIYLGSNRA
SGVPDRFSGSGSGTDFTLKISRVEAEDVGFYYCMQALQTPYTFGQGTKLEIKRTVAAPSV
FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL
SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC

ADMET Property

Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 41.8 +/- 12.4 mg/L [4]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 3-7 days [4]
Half-life: The concentration or amount of drug in body reduced by one-half in 4.8 - 7 days [5]
Metabolism: The drug is metabolized via the hepatic [5]
Vd: The volume of distribution (Vd) of drug is 4.8 +/- 1.3 L [6]

Cross-matching ID

DrugBank ID: DB12159
TTD ID: D07FUP

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Interleukin 4 receptor alpha (IL4R)	TTDWHC3	IL4RA_HUMAN	Not Available	[7]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

ICD Disease Classification

14 Disease of the skin

Disease Class

ICD-11: EA90 Psoriasis

The Studied Tissue

Skin

The Studied Disease

Atopic dermatitis [ICD-11:EA90]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Interleukin 4 receptor alpha (IL4R)	DTT	IL4R	1.48E-08	0.76	3.74

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Dupilumab (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Dupilumab and Siponimod.	Multiple sclerosis [8A40]	[13]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Dupilumab and Ozanimod.	Multiple sclerosis [8A40]	[14]
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References

1	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7574).
3	ClinicalTrials.gov (NCT01949311) Open-label Study of Dupilumab (REGN668/SAR231893) in Patients With Atopic Dermatitis. U.S. National Institutes of Health.
4	FDA Approved Drug Products: Dupixent (dupilumab) for subcutaneous injection
5	Dupixent, INN-dupilumab - European Medicines Agency - Europa EU
6	D'Ippolito D, Pisano M: Dupilumab (Dupixent): An Interleukin-4 Receptor Antagonist for Atopic Dermatitis. P T. 2018 Sep;43(9):532-535.
7	Dupilumab in persistent asthma with elevated eosinophil levels. N Engl J Med. 2013 Jun 27;368(26):2455-66.
8	Aerovance starts trial of Aerovant for uncontrolled asthma. Aerovance. March 3, 2009.
9	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1697).
10	Convection-enhanced drug delivery of interleukin-4 Pseudomonas exotoxin (PRX321): increased distribution and magnetic resonance monitoring. J Pharmacol Exp Ther. 2009 Aug;330(2):520-5.
11	The potential of biologics for the treatment of asthma. Nat Rev Drug Discov. 2012 Dec;11(12):958-72.
12	Clinical pipeline report, company report or official report of Amgen (2009).
13	Cerner Multum, Inc. "Australian Product Information.".
14	Cerner Multum, Inc. "UK Summary of Product Characteristics.".