Secukinumab

Identification

Name
Secukinumab
Accession Number
DB09029
Description

Secukinumab (Cosentyx) is a human monoclonal antibody designed for the treatment of uveitis, rheumatoid arthritis, ankylosing spondylitis, and psoriasis. Secukinumab is an interleukin-17A (IL-17A) inhibitor marketed by Novartis. IL-17 is a group of proinflammatory cytokines released by cells of the immune system and and exist in higher levels in many immune conditions associated with chronic inflammation. By targeting IL-17A, secukinumab has shown excellent efficacy in psoriasis by normalizing skin histology and was approved by the United States Food and Drug Administration on January 21, 2015 to treat adults with moderate-to-severe plaque psoriasis.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Db09029
Protein Chemical Formula
C6584H10134N1754O2042S44
Protein Average Weight
147940.0 Da
Sequences
> Secukinumab Heavy Chain (CAS 875356-43-7)
EVQLVESGGGLVQPGGSLRLSCAASGFTFSNYWMNWVRQAPGKGLEWVAAINQDGSEKYY
VGSVKGRFTISRDNAKNSLYLQMNSLRVEDTAVYYCVRDYYDILTDYYIHYWYFDLWGRG
TLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTF
PAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCP
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYT
LPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKL
TVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
> Secukinumab Light Chain (CAS 875356-44-8)
EIVLTQSPGTLSLSPGERATLSCRASQSVSSSYLAWYQQKPGQAPRLLIYGASSRATGIP
DRFSGSGSGTDFTLTISRLEPEDFAVYYCQQYGSSPCTFGQGTRLEIKRTVAAPSVFIFP
PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL
TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
Synonyms
Not Available
External IDs
  • AIN-457
  • AIN457
  • AIN457A

Pharmacology

Indication

For the treatment of moderate to severe plaque psoriasis in patients that are candidates for systemic therapy or phototherapy.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics
Not Available
Mechanism of action

Secukinumab is a human monoclonal antibody that targets IL-17A cytokine to downregulate inflammation in psoriasis, an autoimmune dermatological disease. The pathophysiology of psoriasis has not been fully established, however it is known that dysregulation of innate and adaptive immune responses plays part in the chronic inflammation associated with the disease. IL-17 represents is a six-membered family (IL-17A to F) of pleiotropic pro-inflammatory cytokines, expression of which is found to be elevated in psoriatic skin. These cytokines act on many different cell types and provide defense against different extracellular pathogens causing fungal or bacterial infections. IL-17 cytokines are produced by many cells involved in immune system defense, such as Th17, mast cells, neutrophils, and dendritic cells - all implicated in promoting inflammation. There is evidence linking IL-17 to pathogenesis of multiple autoimmune diseases including rheumatoid arthritis, spondyloarthritis, psoriasis, Crohn's disease, multiple sclerosis, and even atherosclerosis.

TargetActionsOrganism
AInterleukin-17A
antagonist
Humans
Absorption

Bioavailability after subcutaneous administration was 55-77%.

Volume of distribution

Volume of distribution (Vd) in interstitial fluid of skin (+/- psoriasis) was 27-40% of that in serum after single subcutaneous dose of 300 mg. Vd increased at higher body weights.

Protein binding
Not Available
Metabolism

Mainly intracellular breakdown.

Route of elimination
Not Available
Half-life

22-31 days

Clearance

Serum clearance was increased with higher body weights.

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity
Not Available
Affected organisms
  • Humans and other mammals
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.
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Secukinumab.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Secukinumab.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Secukinumab.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Secukinumab.
AcebutololThe metabolism of Acebutolol can be increased when combined with Secukinumab.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Secukinumab.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Secukinumab.
AcetohexamideThe metabolism of Acetohexamide can be increased when combined with Secukinumab.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be increased when combined with Secukinumab.
AcyclovirThe metabolism of Acyclovir can be increased when combined with Secukinumab.
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
    Action

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

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Food Interactions
No interactions found.

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CosentyxSolution150 mgSubcutaneousNovartis2015-04-10Not applicableCanada flag
CosentyxInjection150 mg/1mLSubcutaneousNovartis Pharmaceuticals Corporation2015-01-21Not applicableUS flag
CosentyxPowder, for solution150 mgSubcutaneousNovartisNot applicableNot applicableCanada flag
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

ATC Codes
L04AC10 — Secukinumab
Drug Categories
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

Chemical Identifiers

UNII
DLG4EML025
CAS number
1229022-83-6

References

General References
  1. McInnes IB, Sieper J, Braun J, Emery P, van der Heijde D, Isaacs JD, Dahmen G, Wollenhaupt J, Schulze-Koops H, Kogan J, Ma S, Schumacher MM, Bertolino AP, Hueber W, Tak PP: Efficacy and safety of secukinumab, a fully human anti-interleukin-17A monoclonal antibody, in patients with moderate-to-severe psoriatic arthritis: a 24-week, randomised, double-blind, placebo-controlled, phase II proof-of-concept trial. Ann Rheum Dis. 2014 Feb;73(2):349-56. doi: 10.1136/annrheumdis-2012-202646. Epub 2013 Jan 29. [PubMed:23361084]
  2. Jaleel T, Elmets C, Weinkle A, Kassira S, Elewski B: Secukinumab (AIN-457) for the treatment of Psoriasis. Expert Rev Clin Pharmacol. 2016 Feb;9(2):187-202. doi: 10.1586/17512433.2016.1129894. [PubMed:26647300]
  3. Wong IT, Shojania K, Dutz J, Tsao NW: Clinical and economic review of secukinumab for moderate-to-severe plaque psoriasis. Expert Rev Pharmacoecon Outcomes Res. 2016 Apr;16(2):153-66. doi: 10.1586/14737167.2016.1133301. Epub 2016 Feb 2. [PubMed:26681527]
  4. Roman M, Madkan VK, Chiu MW: Profile of secukinumab in the treatment of psoriasis: current perspectives. Ther Clin Risk Manag. 2015 Dec 2;11:1767-77. doi: 10.2147/TCRM.S79053. eCollection 2015. [PubMed:26664127]
KEGG Drug
D09967
PubChem Substance
347910391
RxNav
1599788
ChEMBL
CHEMBL1743068
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Secukinumab
AHFS Codes
  • 84:92.00 — Misc. Skin and Mucous Membrane Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAnkylosing Spondylitis (AS)1
4Active Not RecruitingTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
4CompletedBasic SciencePsoriasis1
4CompletedOtherPsoriasis Vulgaris (Plaque Psoriasis)1
4CompletedTreatmentAnkylosing Spondylitis (AS)1
4CompletedTreatmentChronic Plaque Psoriasis1
4CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)2
4CompletedTreatmentPsoriatic Arthritis1
4Enrolling by InvitationTreatmentPsoriasis1
4Not Yet RecruitingOtherPsoriasis Vulgaris (Plaque Psoriasis)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionSubcutaneous150 mg/1mL
Injection, powder, for solutionCutaneous150 MG
Injection, solution150 mg/1mL
Injection, solutionCutaneous; Parenteral150 MG
Powder, for solutionSubcutaneous150 mg
SolutionSubcutaneous150 mg
Solution
Injection, powder, for solution
Powder
Injection, powder, for solution150 mg
Injection, powder, lyophilized, for solutionSubcutaneous150 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US20130202610No2010-10-082020-10-08US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Cytokine receptor binding
Specific Function
Induces stromal cells to produce proinflammatory and hematopoietic cytokines. Enhances the surface expression of ICAM1/intracellular adhesion molecule 1 in fibroblasts.
Gene Name
IL17A
Uniprot ID
Q16552
Uniprot Name
Interleukin-17A
Molecular Weight
17503.92 Da
References
  1. Ohtsuki M, Morita A, Abe M, Takahashi H, Seko N, Karpov A, Shima T, Papavassilis C, Nakagawa H: Secukinumab efficacy and safety in Japanese patients with moderate-to-severe plaque psoriasis: subanalysis from ERASURE, a randomized, placebo-controlled, phase 3 study. J Dermatol. 2014 Dec;41(12):1039-46. doi: 10.1111/1346-8138.12668. Epub 2014 Oct 30. [PubMed:25354738]

Drug created on January 19, 2015 16:12 / Updated on October 21, 2020 01:55

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