Bimekizumab
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Identification
- Summary
Bimekizumab is an anti-IL-17A, IL-17F, and IL-17AF monoclonal antibody used in the treatment plaque psoriasis.
- Generic Name
- Bimekizumab
- DrugBank Accession Number
- DB12917
- Background
Bimekizumab is a humanized monoclonal antibody directed towards IL-17, which was approved for use in the EU on August 20, 2021, for the treatment of plaque psoriasis.4,5 It is the first IL-17 inhibitor to target both IL-17A and IL-17F.3 It has demonstrated superior efficacy as compared to another IL-17 inhibitor, secukinumab, as well as ustekinumab (an IL-12/23 inhibitor) and adalimumab (a TNF inhibitor) in the treatment of moderate-to-severe psoriasis,2,3 likely owing to its dual inhibition of both IL-17A and IL-17F. Bimekizumab was also granted FDA approval on October 18, 2023.7
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- C6552H10132N1750O2029S42
- Protein Average Weight
- Not Available
- Sequences
>SUBUNIT_1 EVQLVESGGGLVQPGGSLRLSCAASGFTFSDYNMAWVRQAPGKGLEWVATITYEGRNTYY RDSVKGRFTISRDNAKNSLYLQMNSLRAEDTAVYYCASPPQYYEGSIYRLWFAHWGQGTL VTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPA VLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAP ELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPR EEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLP PSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTV DKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
>SUBUNIT_2 EVQLVESGGGLVQPGGSLRLSCAASGFTFSDYNMAWVRQAPGKGLEWVATITYEGRNTYY RDSVKGRFTISRDNAKNSLYLQMNSLRAEDTAVYYCASPPQYYEGSIYRLWFAHWGQGTL VTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPA VLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAP ELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPR EEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLP PSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTV DKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
>SUBUNIT_3 AIQLTQSPSSLSASVGDRVTITCRADESVRTLMHWYQQKPGKAPKLLIYLVSNSEIGVPD RFSGSGSGTDFRLTISSLQPEDFATYYCQQTWSDPWTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>SUBUNIT_4 AIQLTQSPSSLSASVGDRVTITCRADESVRTLMHWYQQKPGKAPKLLIYLVSNSEIGVPD RFSGSGSGTDFRLTISSLQPEDFATYYCQQTWSDPWTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA FormatReferences:
- NIH Inxight: Bimekizumab [Link]
- Synonyms
- Bimekizumab
- External IDs
- UCB4940
Pharmacology
- Indication
Bimekizumab is indicated for the treatment of moderate-to-severe plaque psoriasis in adults who are candidates for systemic therapy 4 or phototherapy.6,8
In Canada, it is also approved for the treatment of active psoriatic arthritis in adults alone or in combination with a conventional non-biologic disease-modifying antirheumatic drug (cDMARD).8 It is also used to treat adults with active ankylosing spondylitis who have responded inadequately or are intolerant to conventional therapy.8 Bimekizumab is also used for the treatment of adult patients with active non-radiographic axial spondyloarthritis with objective signs of inflammation as indicated by elevated C-reactive protein (CRP) and/or magnetic resonance imaging (MRI) who have responded inadequately or are intolerant to nonsteroidal anti-inflammatory drugs (NSAIDs).8
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 Non-radiographic axial spondyloarthritis •••••••••••• ••••• ••••••••• ••••• •• •••••••••••• •••••••••• •••••••• Treatment of Severe plaque psoriasis •••••••••••• ••••• •••••••••• ••• •••••••••••• •••••••••• •••••••• Treatment of Severe plaque psoriasis •••••••••••• ••••• ••••••••• ••• •••••••• ••••••• •••••••••• •••••••• Treatment of Active ankylosing spondylitis •••••••••••• ••••• •••••••••• •••••••• Treatment of Active ankylosing spondylitis •••••••••••• ••••• ••••••••••• •••• •••••••••••• ••••••• - 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
Bimekizumab exerts its pharmacologic effects by binding to and inhibiting one of the pro-inflammatory cytokines involved in psoriasis pathogenesis.4 It is administered once-monthly as a subcutaneous injection.
Bimekizumab may increased the risk of infection, including upper respiratory tract infections and oral candidiasis.4 Any clinically important active infections should be resolved prior to therapy. In addition, the use of live vaccines during bimekizumab therapy is not recommended - ensure patients beginning therapy have completed all age appropriate immunizations prior to initiation.4
- Mechanism of action
The pathophysiology of psoriasis involves a dysregulation of the immune system and is facilitated by a variety of cytokines released by dendritic cells and T-helper cells.1 Plaque psoriasis, the most common subtype of psoriasis, is driven primarily by tumor necrosis factor-alpha (TNF-α) and interleukins 17 and 23 (IL-17 and IL-23), with the axis between these three cytokines integral to the maintenance phase of psoriasis. IL-17 acts through two separate mechanisms: the first, dependent on the cytoplasmic adaptor protein ACT1, involves the activation of NF-κB and the transcription of inflammatory genes. The second, independent of ACT1, involves the activation of the JAK/STAT signaling cascade, which leads to further transcription of pro-inflammatory proteins and continued psoriasis pathogenicity.1
Bimekizumab is a monoclonal antibody targeted against IL-17A, IL-17F, and a heterodimer of the two called IL-17AF.4 It blocks the interaction of these interleukins with their respective receptors, thus reducing psoriatic inflammation.
Target Actions Organism AInterleukin-17A antibodyHumans AInterleukin-17F antibodyHumans - Absorption
In healthy volunteers, the absolute bioavailability of bimekizumab following subcutaneous injection was 70.1%.4
- Volume of distribution
In patients with plaque psoriasis, the median volume of distribution at steady-state was 11.2 L.4
- Protein binding
Not Available
- Metabolism
As a monoclonal antibody, bimekizumab is likely degraded into smaller peptides and amino acids via catabolic processes.4
- Route of elimination
Not Available
- Half-life
The mean terminal elimination half-life of bimekizumab in patients with plaque psoriasis was 23 days.4
- Clearance
The median apparent clearance of bimekuzmab in patients with plaque psoriasis was 0.337 L/day.4
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Single doses of up to 640mg given both intravenously and subcutaneously have been administered in clinical studies without evidence of dose-limiting toxicities.4 If overdosage of bimekizumab is suspected, monitor the patient for adverse reactions and institute symptomatic treatment as clinically indicated.
- 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 Bimekizumab. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Bimekizumab. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Bimekizumab. Abrocitinib The metabolism of Abrocitinib can be increased when combined with Bimekizumab. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Bimekizumab. - Food Interactions
- Not Available
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 Bimzelx Injection, solution 320 mg Subcutaneous Ucb Pharma S.A. 2024-08-14 Not applicable EU Bimzelx Injection, solution 160 mg Subcutaneous Ucb Pharma S.A. 2021-10-06 Not applicable EU Bimzelx Injection, solution 160 mg Subcutaneous Ucb Pharma S.A. 2021-10-06 Not applicable EU Bimzelx Injection, solution 160 mg Subcutaneous Ucb Pharma S.A. 2021-10-06 Not applicable EU Bimzelx Solution 160 mg / mL Subcutaneous Ucb Inc 2022-03-30 Not applicable Canada
Categories
- ATC Codes
- L04AC21 — Bimekizumab
- Drug Categories
- Agents reducing cytokine levels
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunosuppressive Agents
- Interleukin Inhibitors
- 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
- Humans and other mammals
Chemical Identifiers
- UNII
- 09495UIM6V
- CAS number
- 1418205-77-2
References
- Synthesis Reference
Adams R, Maroof A, Baker T, Lawson ADG, Oliver R, Paveley R, Rapecki S, Shaw S, Vajjah P, West S, Griffiths M: Bimekizumab, a Novel Humanized IgG1 Antibody That Neutralizes Both IL-17A and IL-17F. Front Immunol. 2020 Aug 21;11:1894. doi: 10.3389/fimmu.2020.01894. eCollection 2020.
- General References
- Singh R, Koppu S, Perche PO, Feldman SR: The Cytokine Mediated Molecular Pathophysiology of Psoriasis and Its Clinical Implications. Int J Mol Sci. 2021 Nov 26;22(23). pii: ijms222312793. doi: 10.3390/ijms222312793. [Article]
- Freitas E, Torres T: Bimekizumab: the new drug in the biologics armamentarium for psoriasis. Drugs Context. 2021 Jun 8;10. pii: dic-2021-4-1. doi: 10.7573/dic.2021-4-1. eCollection 2021. [Article]
- Oliveira DG, Faria R, Torres T: An Overview of Bimekizumab for the Treatment of Psoriatic Arthritis: The Evidence so Far. Drug Des Devel Ther. 2021 Mar 9;15:1045-1053. doi: 10.2147/DDDT.S267405. eCollection 2021. [Article]
- EMA Summary of Product Characteristics: Bimzelx (bimekizumab) solution for subcutaneous injection [Link]
- EMA European Public Assessment Report: Bimzelx (bimekizumab) [Link]
- FDA Approved Drug Products: BIMZELX (bimekizumab-bkzx) injection, for subcutaneous use [Link]
- PR Newswire: BIMZELX Approved by the U.S. FDA for the Treatment of Adults with Moderate-to-Severe Plaque Psoriasis [Link]
- Health Canada Approved Drug Products: BIMZELX (bimekizumab) Subcutaneous Injection [Link]
- FDA Approved Drug Products: Bimzelx (bimekizumab-bkzx) solution for subcutaneous injection (September 2024) [Link]
- External Links
- PubChem Substance
- 347911408
- 2668041
- Wikipedia
- Bimekizumab
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 Recruiting Treatment Psoriasis Vulgaris (Plaque Psoriasis) 1 somestatus stop reason just information to hide 4 Withdrawn Treatment Active Psoriatic arthritis / Psoriasis Vulgaris (Plaque Psoriasis) 1 somestatus stop reason just information to hide 3 Active Not Recruiting Treatment Ankylosing Spondylitis (AS) / Axial Spondyloarthritis (AxSpA) / Nr-axSpA / R-axSpa 1 somestatus stop reason just information to hide 3 Active Not Recruiting Treatment Chronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous 160 mg/1mL Injection, solution Subcutaneous 160 mg Injection, solution Subcutaneous 320 mg Solution Subcutaneous 160 mg / mL Solution Subcutaneous 160.00 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- Curator comments
- Bimekizumab is a humanized IgG1/κ monoclonal antibody that selectively binds with high affinity to IL-17A, IL-17F and IL-17AF cytokines, blocking their interaction with the IL-17RA/IL-17RC receptor complex.
- 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
References
- EMA Summary of Product Characteristics: Bimzelx (bimekizumab) solution for subcutaneous injection [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- Curator comments
- Bimekizumab is a humanized IgG1/κ monoclonal antibody that selectively binds with high affinity to IL-17A, IL-17F and IL-17AF cytokines, blocking their interaction with the IL-17RA/IL-17RC receptor complex.
- General Function
- Effector cytokine of innate and adaptive immune system involved in antimicrobial host defense and maintenance of tissue integrity (PubMed:21350122). IL17A-IL17F signals via IL17RA-IL17RC heterodimeric receptor complex, triggering homotypic interaction of IL17RA and IL17RC chains with TRAF3IP2 adapter through SEFIR domains. 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:11574464, PubMed:11591732, PubMed:11591768, PubMed:17911633, PubMed:18684971, PubMed:21350122, PubMed:28827714). IL17A-IL17F is primarily involved in host defense against extracellular bacteria and fungi by inducing neutrophilic inflammation (By similarity). As signature effector cytokine of T-helper 17 cells (Th17), primarily induces neutrophil activation and recruitment at infection and inflammatory sites (By similarity). Stimulates 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). IL17F homodimer can signal via IL17RC homodimeric receptor complex, triggering downstream activation of TRAF6 and NF-kappa-B signaling pathway (PubMed:32187518). Via IL17RC induces transcriptional activation of IL33, a potent cytokine that stimulates group 2 innate lymphoid cells and adaptive T-helper 2 cells involved in pulmonary allergic response to fungi. Likely via IL17RC, promotes sympathetic innervation of peripheral organs by coordinating the communication between gamma-delta T cells and parenchymal cells. Stimulates sympathetic innervation of thermogenic adipose tissue by driving TGFB1 expression (By similarity). Regulates the composition of intestinal microbiota and immune tolerance by inducing antimicrobial proteins that specifically control the growth of commensal Firmicutes and Bacteroidetes (By similarity)
- Specific Function
- cytokine activity
- Gene Name
- IL17F
- Uniprot ID
- Q96PD4
- Uniprot Name
- Interleukin-17F
- Molecular Weight
- 18044.88 Da
References
- EMA Summary of Product Characteristics: Bimzelx (bimekizumab) solution for subcutaneous injection [Link]
Drug created at October 21, 2016 01:15 / Updated at September 27, 2024 10:03