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Identification
NameSecukinumab
Accession NumberDB09029
TypeBiotech
GroupsApproved
DescriptionSecukinumab (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.
Protein structureDb09029
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Protein chemical formulaC6584H10134N1754O2042S44
Protein average weight147940.0 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
SynonymsNot Available
External Identifiers
  • AIN-457
  • AIN457
  • AIN457A
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cosentyxinjection150 mg/mLsubcutaneousNovartis Pharmaceuticals Corporation2015-01-21Not applicableUs
Cosentyxsolution150 mgsubcutaneousNovartis Pharmaceuticals Canada Inc2015-04-10Not applicableCanada
Cosentyxpowder for solution150 mgsubcutaneousNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIDLG4EML025
CAS number1229022-83-6
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of moderate to severe plaque psoriasis in patients that are candidates for systemic therapy or phototherapy.
PharmacodynamicsNot Available
Mechanism of actionSecukinumab 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.
Related Articles
AbsorptionBioavailability 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 bindingNot Available
Metabolism

Mainly intracellular breakdown.

Route of eliminationNot Available
Half life22-31 days
Clearance

Serum clearance was increased with higher body weights.

ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injectionsubcutaneous150 mg/mL
Powder for solutionsubcutaneous150 mg
Solutionsubcutaneous150 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US20130202610 No2010-10-082020-10-08Us
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
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 ]
External Links
ATC CodesL04AC10
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Secukinumab.
FingolimodSecukinumab may increase the immunosuppressive activities of Fingolimod.
LeflunomideThe risk or severity of adverse effects can be increased when Secukinumab is combined with Leflunomide.
NatalizumabThe risk or severity of adverse effects can be increased when Secukinumab is combined with Natalizumab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Secukinumab.
Rabies vaccineThe risk or severity of adverse effects can be increased when Secukinumab is combined with Rabies vaccine.
RoflumilastRoflumilast may increase the immunosuppressive activities of Secukinumab.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Secukinumab.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Secukinumab.
TofacitinibSecukinumab may increase the immunosuppressive activities of Tofacitinib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Secukinumab.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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
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 ]
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Drug created on January 19, 2015 16:12 / Updated on August 17, 2016 12:24