Ixekizumab
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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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Moderate to severe plaque psoriasis •••••••••••• ••••••••• ••• •••••••• •••••••• •••••••••• ••• •••••••••••• ••••••••• Treatment of Active ankylosing spondylitis •••••••••••• ••••• ••••••••• Treatment of Active non-radiographic axial spondyloarthritis •••••••••••• ••••• ••••••••• ••••• •• •••••••••••• ••••••••• Treatment of Active psoriatic arthritis •••••••••••• ••••• ••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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.
Target Actions Organism AInterleukin-17A antibodyHumans - 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Ixekizumab. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Ixekizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Ixekizumab. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Ixekizumab. Aducanumab The risk or severity of adverse effects can be increased when Ixekizumab is combined with Aducanumab. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Taltz Injection, solution 20 mg/0.25mL Subcutaneous Eli Lilly and Company 2016-03-22 Not applicable US Taltz Injection, solution 80 mg Subcutaneous Eli Lilly And Company (Ireland) Limited 2016-09-08 Not applicable EU Taltz Injection, solution 80 mg/1mL Subcutaneous Eli Lilly and Company 2016-03-22 Not applicable US Taltz Injection, solution 80 mg Subcutaneous Eli Lilly And Company (Ireland) Limited 2016-09-08 Not applicable EU Taltz Solution 80 mg / mL Subcutaneous Eli Lilly & Co. Ltd. 2016-08-11 Not applicable Canada
Categories
- ATC Codes
- L04AC13 — Ixekizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Dermatologicals
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunosuppressive Agents
- Interleukin Inhibitors
- Interleukin-17
- Interleukin-17A Antagonist
- Misc. Skin and Mucous Membrane Agents
- Proteins
- Serum Globulins
- 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
- 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]
- 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]
- 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]
- FDA Approved Drug Products: TALTZ (ixekizumab) injection [Link]
- External Links
- KEGG Drug
- D10071
- PubChem Substance
- 347911203
- 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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data4 Active Not Recruiting Treatment Psoriasis / Psoriasis Vulgaris (Plaque Psoriasis) 1 somestatus stop reason just information to hide 4 Completed Treatment Erythrodermic psoriasis / Generalized Pustular Psoriasis (GPP) 1 somestatus stop reason just information to hide 4 Completed Treatment Psoriasis Vulgaris (Plaque Psoriasis) 1 somestatus stop reason just information to hide 4 Completed Treatment Psoriatic Arthritis 1 somestatus stop reason just information to hide 4 Not Yet Recruiting Treatment Psoriasis Vulgaris (Plaque Psoriasis) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Injection, solution 80 mg/1ml Injection, solution Parenteral; Subcutaneous 80 MG Injection, solution Subcutaneous 20 mg/0.25mL Injection, solution Subcutaneous 40 mg/0.5mL Injection, solution Subcutaneous 80 mg/1mL Solution Subcutaneous 80 mg Solution Subcutaneous 80 mg / mL Solution Subcutaneous 80.000 mg Injection, solution Subcutaneous 80 mg Injection, solution Subcutaneous 80 mg/ml Injection, solution 80 mg/ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Effector cytokine of innate and adaptive immune system involved in antimicrobial host defense and maintenance of tissue integrity (PubMed:24120361). Signals via IL17RA-IL17RC heterodimeric receptor complex, triggering homotypic interaction of IL17RA and IL17RC chains with TRAF3IP2 adapter. This leads to downstream TRAF6-mediated activation of NF-kappa-B and MAPkinase pathways ultimately resulting in transcriptional activation of cytokines, chemokines, antimicrobial peptides and matrix metalloproteinases, with potential strong immune inflammation (PubMed:17911633, PubMed:18684971, PubMed:19825828, PubMed:21350122, PubMed:24120361, PubMed:8676080). Plays an important role in connecting T cell-mediated adaptive immunity and acute inflammatory response to destroy extracellular bacteria and fungi. As a signature effector cytokine of T-helper 17 cells (Th17), primarily induces neutrophil activation and recruitment at infection and inflammatory sites (By similarity). In airway epithelium, mediates neutrophil chemotaxis via induction of CXCL1 and CXCL5 chemokines (By similarity). In secondary lymphoid organs, contributes to germinal center formation by regulating the chemotactic response of B cells to CXCL12 and CXCL13, enhancing retention of B cells within the germinal centers, B cell somatic hypermutation rate and selection toward plasma cells (By similarity). Effector cytokine of a subset of gamma-delta T cells that functions as part of an inflammatory circuit downstream IL1B, TLR2 and IL23A-IL12B to promote neutrophil recruitment for efficient bacterial clearance (By similarity). Effector cytokine of innate immune cells including invariant natural killer cell (iNKT) and group 3 innate lymphoid cells that mediate initial neutrophilic inflammation (By similarity). Involved in the maintenance of the integrity of epithelial barriers during homeostasis and pathogen infection (PubMed:21350122). Upon acute injury, has a direct role in epithelial barrier formation by regulating OCLN localization and tight junction biogenesis (By similarity). As part of the mucosal immune response induced by commensal bacteria, enhances host's ability to resist pathogenic bacterial and fungal infections by promoting neutrophil recruitment and antimicrobial peptides release (By similarity). In synergy with IL17F, mediates the production of antimicrobial beta-defensins DEFB1, DEFB103A, and DEFB104A by mucosal epithelial cells, limiting the entry of microbes through the epithelial barriers (By similarity). Involved in antiviral host defense through various mechanisms (By similarity). Enhances immunity against West Nile virus by promoting T cell cytotoxicity (By similarity). May play a beneficial role in influenza A virus (H5N1) infection by enhancing B cell recruitment and immune response in the lung (By similarity). Contributes to influenza A virus (H1N1) clearance by driving the differentiation of B-1a B cells, providing for production of virus-specific IgM antibodies at first line of host defense (By similarity)
- Specific Function
- Cytokine activity
- 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