Bimekizumab

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:

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.

Target	Actions	Organism
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.

Drug	Interaction
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Abatacept	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.
Acebutolol	The metabolism of Acebutolol can be increased when combined with Bimekizumab.
Acenocoumarol	The metabolism of Acenocoumarol can be increased when combined with Bimekizumab.
Acetaminophen	The metabolism of Acetaminophen can be increased when combined with Bimekizumab.
Acetohexamide	The metabolism of Acetohexamide can be increased when combined with Bimekizumab.
Acetylsalicylic acid	The metabolism of Acetylsalicylic acid can be increased when combined with Bimekizumab.

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Food Interactions

Not Available

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Solution	160 mg / mL	Subcutaneous	Ucb Inc	2022-03-30	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Injection, solution	160 mg	Subcutaneous	Ucb Pharma S.A.	2021-10-06	Not applicable
Bimzelx	Solution	160 mg / mL	Subcutaneous	Ucb Inc	2022-03-30	Not applicable

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]

External Links

PubChem Substance: 347911408
Wikipedia: Bimekizumab

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Not Yet Recruiting	Treatment	Active Psoriatic arthritis / Psoriasis Vulgaris (Plaque Psoriasis)	1
4	Recruiting	Treatment	Psoriasis (PsO) / Psoriasis Vulgaris (Plaque Psoriasis)	1
3	Active Not Recruiting	Treatment	Ankylosing Spondylitis (AS) / Axial Spondyloarthritis (AxSpA) / Nr-axSpA / R-axSpa	1
3	Active Not Recruiting	Treatment	Chronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis	2
3	Active Not Recruiting	Treatment	Hidradenitis Suppurativa (HS)	2
3	Active Not Recruiting	Treatment	Non-radiographic Axial Spondyloarthritis	1
3	Active Not Recruiting	Treatment	Psoriatic Arthritis	1
3	Completed	Treatment	Ankylosing Spondylitis (AS)	1
3	Completed	Treatment	Chronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis	1
3	Completed	Treatment	Chronic Plaque Psoriasis / Moderate to Severe Chronic Plaque Psoriasis / Psoriatic Arthritis	2

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Subcutaneous	160 mg
Solution	Subcutaneous	160 mg / mL

Prices

Not Available

Patents

Not Available

Properties

State: Solid
Experimental Properties: Not Available

Targets

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Details1. Interleukin-17A

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

EMA Summary of Product Characteristics: Bimzelx (bimekizumab) solution for subcutaneous injection [Link]

Details2. Interleukin-17F

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

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

Bimekizumab

Identification

References:

Pharmacology

Interactions

Products

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Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References