Ixekizumab

Identification

Summary

Ixekizumab is a monoclonal antibody used to treat moderate to severe plaque psoriasis.

Brand Names
Taltz
Generic Name
Ixekizumab
DrugBank Accession Number
DB11569
Background

Ixekizumab is a humanized immunoglobulin G subclass 4 (IgG4) monoclonal antibody (mAb) against interleukin-17A (IL-17A) and prevents it from interacting with the IL-17A receptor. As IL-17A is a pro-inflammatory cytokine involved in inflammation and immune responses, blocking its effect is beneficial for use in inflammatory conditions. In particular, IL-17A has been found to be implicated in a variety of autoimmune diseases including Rheumatoid Arthritis and plaque psoriasis.

Ixekizumab is produced by recombinant DNA technology in a recombinant mammalian cell line and purified using standard technology for bioprocessing. Ixekizumab is comprised of two identical light chain polypeptides of 219 amino acids each and two identical heavy chain polypeptides of 445 amino acids each, and has a molecular weight of 146,158 Daltons for the protein backbone of the molecule. It is indicated for the treatment of adults with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Chemical Formula
C6492H10012N1728O2028S46
Protein Average Weight
146158.0 Da
Sequences
>Heavy Chain Sequence
QVQLVQSGAEVKKPGSSVKVSCKASGYSFTDYHIHWVRQAPGQGLEWMGVINPMYGTTDY
NQRFKGRVTITADESTSTAYMELSSLRSEDTAVYYCARYDYFTGTGVYWGQGTLVTVSSA
STKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSVF
LFPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYR
VVSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKN
QVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGN
VFSCSVMHEALHNHYTQKSLSLSLG
>Light Chain Sequence
DIVMTQTPLSLSVTPGQPASISCRSSRSLVHSRGNTYLHWYLQKPGQSPQLLIYKVSNRF
IGVPDRFSGSGSGTDFTLKISRVEAEDVGVYYCSQSTHLPFTFGQGTKLEIKRTVAAPSV
FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL
SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
Synonyms
  • Ixekizumab
External IDs
  • LY 2439821
  • LY-2439821
  • LY2439821

Pharmacology

Indication

Ixekizumab is indicated for the treatment of patients aged six years or older with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy. It is also indicated in adult patients with active psoriatic arthritis, ankylosing spondylitis, or non-radiographic axial spondyloarthritis with objective signs of inflammation.4

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofModerate to severe plaque psoriasis••••••••••••••••••••• ••• •••••••• •••••••• •••••••••• ••• •••••••••••••••••••••
Treatment ofActive ankylosing spondylitis••••••••••••••••••••••••••
Treatment ofActive non-radiographic axial spondyloarthritis•••••••••••••••••••••••••• ••••• •• •••••••••••••••••••••
Treatment ofActive psoriatic arthritis••••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Ixekizumab is a humanized immunoglobulin G subclass 4 (IgG4) monoclonal antibody (mAb) against interleukin-17A (IL-17A) and prevents it from interacting with the IL-17A receptor. As IL-17A is a pro-inflammatory cytokine involved in inflammation and immune responses, blocking its effect is beneficial for use in inflammatory conditions. In particular, IL-17A has been found to be implicated in a variety of autoimmune diseases including Rheumatoid Arthritis and plaque psoriasis.

TargetActionsOrganism
AInterleukin-17A
antibody
Humans
Absorption

Following a single subcutaneous dose of 160 mg in subjects with plaque psoriasis, ixekizumab reached peak mean (±SD) serum concentrations (Cmax) of 16.2 ±6.6 mcg/mL by approximately 4 days post dose.

Volume of distribution

The mean (geometric CV%) volume of distribution at steady-state was 7.11 L (29%) in subjects with plaque psoriasis.

Protein binding

Not Available

Metabolism

The metabolic pathway of ixekizumab has not been characterized. As a humanized IgG4 monoclonal antibody ixekizumab is expected to be degraded into small peptides and amino acids via catabolic pathways in the same manner as endogenous IgG.

Route of elimination

Not Available

Half-life

13 days

Clearance

0.39 L/day

Adverse Effects
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Toxicity

The most common adverse reactions associated with Ixekizumab treatment are injection site reactions, upper respiratory tract infections, nausea, and tinea infections.

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 Ixekizumab.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Ixekizumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Ixekizumab.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Ixekizumab.
AducanumabThe risk or severity of adverse effects can be increased when Ixekizumab is combined with Aducanumab.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
TaltzSolution80 mg / mLSubcutaneousEli Lilly & Co. Ltd.2016-08-11Not applicableCanada flag
TaltzInjection, solution80 mgSubcutaneousEli Lilly And Company (Ireland) Limited2016-09-08Not applicableEU flag
TaltzInjection, solution80 mgSubcutaneousEli Lilly And Company (Ireland) Limited2016-09-08Not applicableEU flag
TaltzInjection, solution20 mg/0.25mLSubcutaneousEli Lilly and Company2016-03-22Not applicableUS flag
TaltzInjection, solution80 mg/1mLSubcutaneousEli Lilly and Company2016-03-22Not applicableUS flag

Categories

ATC Codes
L04AC13 — Ixekizumab
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
Affected organisms
Not Available

Chemical Identifiers

UNII
BTY153760O
CAS number
1143503-69-8

References

General References
  1. Dyring-Andersen B, Skov L, Zachariae C: Ixekizumab for treatment of psoriasis. Expert Rev Clin Immunol. 2015 Apr;11(4):435-42. doi: 10.1586/1744666X.2015.1023295. Epub 2015 Mar 8. [Article]
  2. Genovese MC, Van den Bosch F, Roberson SA, Bojin S, Biagini IM, Ryan P, Sloan-Lancaster J: LY2439821, a humanized anti-interleukin-17 monoclonal antibody, in the treatment of patients with rheumatoid arthritis: A phase I randomized, double-blind, placebo-controlled, proof-of-concept study. Arthritis Rheum. 2010 Apr;62(4):929-39. doi: 10.1002/art.27334. [Article]
  3. Bush KA, Farmer KM, Walker JS, Kirkham BW: Reduction of joint inflammation and bone erosion in rat adjuvant arthritis by treatment with interleukin-17 receptor IgG1 Fc fusion protein. Arthritis Rheum. 2002 Mar;46(3):802-5. [Article]
  4. FDA Approved Drug Products: TALTZ (ixekizumab) injection [Link]
KEGG Drug
D10071
PubChem Substance
347911203
RxNav
1745099
ChEMBL
CHEMBL1743034
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ixekizumab
FDA label
Download (6.58 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentPsoriasis / Psoriasis Vulgaris (Plaque Psoriasis)1
4CompletedTreatmentErythrodermic psoriasis / Generalized Pustular Psoriasis (GPP)1
4CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
4CompletedTreatmentPsoriatic Arthritis1
4RecruitingOtherPsoriasis Vulgaris (Plaque Psoriasis)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solution
Injection, solution80 mg/1ml
Injection, solutionParenteral; Subcutaneous80 MG
Injection, solutionSubcutaneous20 mg/0.25mL
Injection, solutionSubcutaneous40 mg/0.5mL
Injection, solutionSubcutaneous80 mg/1mL
Injection, solutionSubcutaneous80 mg
SolutionSubcutaneous80 mg
SolutionSubcutaneous80 mg / mL
SolutionSubcutaneous80.000 mg
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous80 mg/ml
Injection, solution80 mg/ml
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antibody
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

Drug created at April 06, 2016 15:41 / Updated at June 03, 2022 07:24