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Identification
- Summary
Lebrikizumab is an IgG4 monoclonal antibody against IL-13 used to treat moderate-to-severe atopic dermatitis in adults and adolescents.
- Generic Name
- Lebrikizumab
- DrugBank Accession Number
- DB11914
- Background
Lebrikizumab is a monoclonal antibody that binds to IL-13 with high affinity and slow off-rate.5 It binds to a different epitope compared tralokinumab.1,2
On November 17, 2023, lebrikizumab was approved by the EMA under the brand name EBGLYSS for the treatment of moderate-to-severe atopic dermatitis in adult and adolescent patients 12 years and older with a body weight of at least 40 kg. This approval is based on the positive results obtained from the Phase 3 studies ADvocate 1 and ADvocate 2, where nearly 80% of patients taking lebrikizumab either as monotherapy or combination therapy with topical corticosteroid achieved skin clearance, itch relief and reduced disease severity by week 16.4 Lebrikizumab was also approved by the FDA on September 13, 2024.6
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>SUBUNIT_1 QVTLRESGPALVKPTQTLTLTCTVSGFSLSAYSVNWIRQPPGKALEWLAMIWGDGKIVYN SALKSRLTISKDTSKNQVVLTMTNMDPVDTATYYCAGDGYYPYAMDNWGQGSLVTVSSAS TKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSVFL FPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRV VSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQ VSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNV FSCSVMHEALHNHYTQKSLSLSLGK
>SUBUNIT_2 QVTLRESGPALVKPTQTLTLTCTVSGFSLSAYSVNWIRQPPGKALEWLAMIWGDGKIVYN SALKSRLTISKDTSKNQVVLTMTNMDPVDTATYYCAGDGYYPYAMDNWGQGSLVTVSSAS TKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTKTYTCNVDHKPSNTKVDKRVESKYGPPCPPCPAPEFLGGPSVFL FPPKPKDTLMISRTPEVTCVVVDVSQEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTYRV VSVLTVLHQDWLNGKEYKCKVSNKGLPSSIEKTISKAKGQPREPQVYTLPPSQEEMTKNQ VSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSRLTVDKSRWQEGNV FSCSVMHEALHNHYTQKSLSLSLGK
>SUBUNIT_3 DIVMTQSPDSLSVSLGERATINCRASKSVDSYGNSFMHWYQQKPGQPPKLLIYLASNLES GVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQNNEDPRTFGGGTKVEIKRTVAAPSVF IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>SUBUNIT_4 DIVMTQSPDSLSVSLGERATINCRASKSVDSYGNSFMHWYQQKPGQPPKLLIYLASNLES GVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQNNEDPRTFGGGTKVEIKRTVAAPSVF IFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLS STLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA FormatReferences:
- NIH Inxight: Lebrikizumab [Link]
- Synonyms
- Lebrikizumab
- External IDs
- TNX-650
Pharmacology
- Indication
Lebrikizumab is approved for the treatment of moderate-to-severe atopic dermatitis in adults and adolescents 12 years and older with a body weight of at least 40 kg who are candidates for systemic therapy.3,5
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 Severe atopic dermatitis •••••••••••• ••••••••••• ••••• •••• •••••• •• •• •• •• ••••• ••••••• •••••••••••• ••••••••• ••• ••• ••••••••• Treatment of Severe atopic dermatitis •••••••••••• ••••••••••• ••••• •••••••••• •••••••• •• ••••••• •••••••••• •••• •••••• •• •• •• •• •••• Treatment of Severe atopic dermatitis •••••••••••• ••••••••••• ••••• ••••••••• ••• •••••••• •••••••• •••• •••••• •• •• •• •• •••• •••••••• Treatment of Moderate atopic dermatitis •••••••••••• ••••••••••• ••••• •••• •••••• •• •• •• •• ••••• •••••••••• •••••••• •• ••••••• ••••••••• Treatment of Moderate atopic dermatitis •••••••••••• ••••••••••• ••••• •••• •••••• •• •• •• •• ••••• ••••••• •••••••••••• ••••••••• ••• ••• ••••••••• - 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
In lebrikizumab clinical studies, lebrikizumab reduced the levels of serum periostin, total immunoglobulin E (IgE), CC chemokine ligand (CCL)17 [thymus and activation-regulated chemokine (TARC)], CCL18 [pulmonary and activation-regulated chemokine (PARC)], and CCL13 [monocyte chemotactic protein-4 (MCP-4)]. The decreases in the type 2 inflammation mediators provide indirect evidence of inhibition of the IL-13 pathway by lebrikizumab.3
- Mechanism of action
Lebrikizumab is an immunoglobulin (IgG4) monoclonal antibody that binds with high affinity to interleukin (IL)-13 and selectively inhibits IL-13 signaling through the IL-4 receptor alpha (IL-4Rα)/ IL-13 receptor alpha 1 (IL-13Rα1) heterodimer, thereby inhibiting the downstream effects of IL-13. Inhibition of IL-13 signaling is expected to be of benefit in diseases in which IL-13 is a key contributor to the disease pathogenesis. Lebrikizumab does not prevent the binding of IL-13 to the IL-13 receptor alpha 2 (IL-13Rα2 or decoy receptor), which allows the internalization of IL-13 into the cell.3
Target Actions Organism AInterleukin-13 antibodyHumans - Absorption
After a subcutaneous dose of 250 mg lebrikizumab, peak serum concentrations were achieved approximately 7 to 8 days post-dose.3
Following the 500 mg loading doses at week 0 and week 2, steady-state serum concentrations were achieved with the first 250 mg Q2W dose at week 4.3
Based on a population pharmacokinetic (PK) analysis, the predicted steady-state trough concentrations (Ctrough,ss) following lebrikizumab 250 mg Q2W and Q4W subcutaneous dosing in patients with atopic dermatitis (median and 5th - 95th percentile) were 87 (46-159) µg/mL and 36 (18-68) µg/mL, respectively.3
The absolute bioavailability was estimated at 86% based on a population PK analysis. The injection site location did not significantly influence the absorption of lebrikizumab.3
- Volume of distribution
Based on a population PK analysis, the total volume of distribution at steady-state was 5.14 L.3
- Protein binding
Little information is available on the protein binding of lebrikizumab.3
- Metabolism
Specific metabolism studies were not conducted because lebrikizumab is a protein. Lebrikizumab is expected to degrade to small peptides and individual amino acids via catabolic pathways in the same manner as endogenous IgG.3
- Route of elimination
Not Available
- Half-life
The mean elimination half-life was approximately 24.5 days.3
- Clearance
In the population PK analysis, clearance was 0.154 L/day and was independent of dose.3
- Adverse Effects
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There are limited amount of data on the use of lebrikizumab in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of lebrikizumab during pregnancy.3
The mutagenic potential of lebrikizumab has not been evaluated; however monoclonal antibodies are not expected to alter DNA or chromosomes.3
Carcinogenicity studies have not been conducted with lebrikizumab. Evaluation of the available evidence related to IL-13 inhibition and animal toxicology data with lebrikizumab does not suggest carcinogenic potential for lebrikizumab.3
Single intravenous doses up to 10 mg/kg and multiple subcutaneous doses up to 500 mg have been administered to humans in clinical trials without dose-limiting toxicity. There is no specific treatment for lebrikizumab overdose. In the event of an overdose, the patient should be monitored for any signs or symptoms of adverse reactions and institute appropriate symptomatic treatment immediately.3
- 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 softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Lebrikizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Lebrikizumab. Aducanumab The risk or severity of adverse effects can be increased when Lebrikizumab is combined with Aducanumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Lebrikizumab. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Lebrikizumab. - 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 Ebglyss Injection, solution 250 mg Subcutaneous Almirall S.A. 2023-11-28 Not applicable EU 
Ebglyss Injection, solution 250 mg/2mL Subcutaneous Eli Lilly and Company 2024-09-13 Not applicable US 
Ebglyss Injection, solution 250 mg Subcutaneous Almirall S.A. 2023-11-28 Not applicable EU Ebglyss Injection, solution 250 mg Subcutaneous Almirall S.A. 2023-11-28 Not applicable EU Ebglyss Injection, solution 250 mg Subcutaneous Almirall S.A. 2023-11-28 Not applicable EU
Categories
- ATC Codes
- D11AH10 — Lebrikizumab
- 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
- U9JLP7V031
- CAS number
- 953400-68-5
References
- General References
- Simpson EL, Flohr C, Eichenfield LF, Bieber T, Sofen H, Taieb A, Owen R, Putnam W, Castro M, DeBusk K, Lin CY, Voulgari A, Yen K, Omachi TA: Efficacy and safety of lebrikizumab (an anti-IL-13 monoclonal antibody) in adults with moderate-to-severe atopic dermatitis inadequately controlled by topical corticosteroids: A randomized, placebo-controlled phase II trial (TREBLE). J Am Acad Dermatol. 2018 May;78(5):863-871.e11. doi: 10.1016/j.jaad.2018.01.017. Epub 2018 Jan 17. [Article]
- Prajapati S, Fardos M, Desai AD, Feldman SR: The role of lebrikizumab in the treatment of atopic dermatitis in the adult population. Immunotherapy. 2023 Sep;15(13):981-991. doi: 10.2217/imt-2023-0066. Epub 2023 Jul 4. [Article]
- EMA Approved Drug Products: Ebglyss (Lebrikizumab) solution for subcutaneous injection [Link]
- Almirall Receives European Commission Approval of EBGLYSS® (lebrikizumab) for Moderate-to-Severe Atopic Dermatitis [Link]
- FDA Approved Drug Products: EBGLYSS (lebrikizumab-lbkz), injection, for subcutaneous use [Link]
- Eli Lilly and Company News Release: FDA Approves Lilly's EBGLYSS™ (lebrikizumab-lbkz) for Adults and Children 12 Years and Older with Moderate-to-Severe Atopic Dermatitis [Link]
- External Links
- PubChem Substance
- 347911256
- Wikipedia
- Lebrikizumab
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 data3 Active Not Recruiting Treatment Atopic Dermatitis 4 somestatus stop reason just information to hide 3 Completed Other Atopic Dermatitis 1 somestatus stop reason just information to hide 3 Completed Treatment Asthma 4 somestatus stop reason just information to hide 3 Completed Treatment Atopic Dermatitis 6 somestatus stop reason just information to hide 3 Completed Treatment Atopic Dermatitis / Dermatitis / Skin Diseases / Skin Diseases, Genetic 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous 250 mg/2mL Injection, solution Subcutaneous 250 mg Solution Subcutaneous 250 mg / 2 mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Cytokine that plays important roles in allergic inflammation and immune response to parasite infection (PubMed:8096327, PubMed:8097324). Synergizes with IL2 in regulating interferon-gamma synthesis (PubMed:8096327). Stimulates B-cell proliferation, and activation of eosinophils, basophils, and mast cells (PubMed:7903680, PubMed:8759755). Plays an important role in controlling IL33 activity by modulating the production of transmembrane and soluble forms of interleukin-1 receptor-like 1/IL1RL1 (By similarity). Displays the capacity to antagonize Th1-driven proinflammatory immune response and downregulates synthesis of many proinflammatory cytokines including IL1, IL6, IL10, IL12 and TNF-alpha through a mechanism that partially involves suppression of NF-kappa-B (By similarity). Functions also on nonhematopoietic cells, including endothelial cells where it induces vascular cell adhesion protein 1/VCAM1, which is important in the recruitment of eosinophils (PubMed:8639787). Exerts its biological effects through its receptors which comprises the IL4R chain and the IL13RA1 chain, to activate JAK1 and TYK2, leading to the activation of STAT6 (PubMed:9013879). Aside from IL13RA1, another receptor IL13RA2 acts as a high affinity decoy for IL13 and mediates internalization and depletion of extracellular IL13 (PubMed:21622864)
- Specific Function
- cytokine activity
- Gene Name
- IL13
- Uniprot ID
- P35225
- Uniprot Name
- Interleukin-13
- Molecular Weight
- 15787.535 Da
References
- EMA Approved Drug Products: Ebglyss (Lebrikizumab) solution for subcutaneous injection [Link]
Drug created at October 20, 2016 21:00 / Updated at September 22, 2024 11:16