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.

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
References:
  1. NIH Inxight: Bimekizumab [Link]
Download FASTA Format
Synonyms
  • Bimekizumab
External IDs
  • UCB4940

Pharmacology

Indication

Bimekizumab is indicated in the EU for the treatment of moderate-to-severe plaque psoriasis in adults who are candidates for systemic therapy.4

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Associated Conditions
Contraindications & Blackbox Warnings
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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.

TargetActionsOrganism
AInterleukin-17A
antibody
Humans
AInterleukin-17F
antibody
Humans
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
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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.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Bimekizumab.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Bimekizumab.
AbrocitinibThe metabolism of Abrocitinib can be increased when combined with Bimekizumab.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Bimekizumab.
AcebutololThe metabolism of Acebutolol can be increased when combined with Bimekizumab.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Bimekizumab.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Bimekizumab.
AcetohexamideThe metabolism of Acetohexamide can be increased when combined with Bimekizumab.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be increased when combined with Bimekizumab.
AcyclovirThe metabolism of Acyclovir can be increased when combined with Bimekizumab.
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Food Interactions
Not Available

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxSolution160 mg / mLSubcutaneousUcb Inc2022-03-30Not applicableCanada flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag
BimzelxSolution160 mg / mLSubcutaneousUcb Inc2022-03-30Not applicableCanada flag
BimzelxInjection, solution160 mgSubcutaneousUcb Pharma S.A.2021-10-06Not applicableEU flag

Categories

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
  • 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
  1. 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]
  2. 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]
  3. 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]
  4. EMA Summary of Product Characteristics: Bimzelx (bimekizumab) solution for subcutaneous injection [Link]
  5. EMA European Public Assessment Report: Bimzelx (bimekizumab) [Link]
PubChem Substance
347911408
Wikipedia
Bimekizumab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentAnkylosing Spondylitis (AS)1
3Active Not RecruitingTreatmentChronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis2
3Active Not RecruitingTreatmentHidradenitis Suppurativa (HS)2
3Active Not RecruitingTreatmentModerate to Severe Plaque Psoriasis1
3Active Not RecruitingTreatmentNon-radiographic Axial Spondyloarthritis1
3Active Not RecruitingTreatmentPsoriatic Arthritis2
3CompletedTreatmentChronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis1
3CompletedTreatmentChronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis / Psoriatic Arthritis2
3CompletedTreatmentChronic Plaque Psoriasis / Moderate to Severe Plaque Psoriasis1
3CompletedTreatmentPsoriatic Arthritis2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionSubcutaneous160 mg
SolutionSubcutaneous160 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
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
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
References
  1. 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:18684971, PubMed:21350122, PubMed:11591732, PubMed:11591768, PubMed:17911633, PubMed:11574464, 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
  1. EMA Summary of Product Characteristics: Bimzelx (bimekizumab) solution for subcutaneous injection [Link]

Drug created at October 21, 2016 01:15 / Updated at January 13, 2022 02:31