Identification

Summary

Bezlotoxumab is a monoclonal antibody used to reduce the recurrence of Clostridium difficile infections.

Brand Names
Zinplava
Generic Name
Bezlotoxumab
DrugBank Accession Number
DB13140
Background

Bezlotoxumab is a human monoclonal antibody that binds to Clostridium difficile toxin B and neutralizes its effects. Used to reduce the recurrence of Clostridium difficle infection in adults receiving antibiotic therapy to treat C. difficile infection and high risk of recurrence.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • Bezlotoxumab
External IDs
  • MBL-CDB1
  • MDX-1388
  • MK-6072

Pharmacology

Indication

Prevents recurrence of Clostridium difficile infection in people 18 years or older who are either currently receiving treatment for C. difficile infection or have a high risk of recurrence.

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Associated Conditions
Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug events
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Pharmacodynamics

Bezlotoxumab binds to C.difficile toxin B, a virulence factor common to practically all C.difficile, which prevents the bacteria from infecting host cells. Bezlotoxumab binds two epitopes of toxin B, via two Fab regions, which partially blocks the carbohydrate binding pockets of the toxin resulting in the prevention of toxin B from binding to host cells.

Mechanism of action

A single molecule of bezlotoxumab neutralizes Toxin B by binding its two Fab regions to two epitopes within the N-terminal half of the Toxin B CROP domain, partially blocking the carbohydrate binding pockets of the toxin and preventing toxin binding to host cells.

TargetActionsOrganism
AClostridium difficile Toxin B
antibody
Peptoclostridium difficile
Absorption

Not absorbed since give IV

Volume of distribution

7.33L

Protein binding

Binds to C.difficile virulence factor toxin B which prevents its action on host cells.

Metabolism

Catabolism

Route of elimination

Catabolism

Half-life

19 Days

Clearance

0.317 L/day

Adverse Effects
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Toxicity

No data available on overdosage.

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 Bezlotoxumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Bezlotoxumab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab is combined with Bezlotoxumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Bezlotoxumab.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Bezlotoxumab.
AmivantamabThe risk or severity of adverse effects can be increased when Bezlotoxumab is combined with Amivantamab.
AnifrolumabThe risk or severity of adverse effects can be increased when Anifrolumab is combined with Bezlotoxumab.
AnsuvimabThe risk or severity of adverse effects can be increased when Bezlotoxumab is combined with Ansuvimab.
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Anthrax immune globulin human is combined with Bezlotoxumab.
Antilymphocyte immunoglobulin (horse)The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) is combined with Bezlotoxumab.
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ZinplavaInjection, solution, concentrate25 mg/mlIntravenousMerck Sharp & Dohme B.V.2020-12-18Not applicableEU flag
ZinplavaInjection, solution25 mg/1mLIntravenousMerck Sharp & Dohme Llc2016-10-21Not applicableUS flag

Categories

ATC Codes
J06BC03 — Bezlotoxumab
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
  • Peptoclostridium difficile

Chemical Identifiers

UNII
4H5YMK1H2E
CAS number
1246264-45-8

References

General References
  1. Orth P, Xiao L, Hernandez LD, Reichert P, Sheth PR, Beaumont M, Yang X, Murgolo N, Ermakov G, DiNunzio E, Racine F, Karczewski J, Secore S, Ingram RN, Mayhood T, Strickland C, Therien AG: Mechanism of action and epitopes of Clostridium difficile toxin B-neutralizing antibody bezlotoxumab revealed by X-ray crystallography. J Biol Chem. 2014 Jun 27;289(26):18008-21. doi: 10.1074/jbc.M114.560748. Epub 2014 May 12. [Article]
  2. Zhang Z, Chen X, Hernandez LD, Lipari P, Flattery A, Chen SC, Kramer S, Polishook JD, Racine F, Cape H, Kelly CP, Therien AG: Toxin-mediated paracellular transport of antitoxin antibodies facilitates protection against Clostridium difficile infection. Infect Immun. 2015 Jan;83(1):405-16. doi: 10.1128/IAI.02550-14. Epub 2014 Nov 10. [Article]
  3. Ghetie V, Ward ES: Transcytosis and catabolism of antibody. Immunol Res. 2002;25(2):97-113. [Article]
  4. FDA Monograph for Zinplava [Link]
PubChem Substance
347911429
RxNav
1855048
Wikipedia
Bezlotoxumab

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentClostridium difficile infection recurrence1
4Not Yet RecruitingTreatmentClostridioides Difficile / Clostridium Infections / Pseudomembranous Enterocolitis1
4RecruitingPreventionC. Diff. Infections / Crohn's Disease (CD) / Inflammatory Bowel Diseases (IBD) / Ulcerative Colitis1
4RecruitingTreatmentClostridium Difficle Colitis / Clostridium; Sepsis1
4TerminatedPreventionClostridium Difficile1
4Unknown StatusPreventionClostridium difficile infection recurrence1
3CompletedPreventionClostridium Difficile Infection (CDI)1
3CompletedTreatmentClostridium Difficile Infection (CDI)2
2CompletedTreatmentClostridium Infections1
2RecruitingTreatmentClostridioides Difficile Infection / Clostridium difficile infection recurrence / Death / Organ Dysfunction Syndrome / Stool Microbiome1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous25 mg/1mL
Injection, solution, concentrateIntravenous25 mg/ml
Injection, solution, concentrateIntravenous; Parenteral25 MG/ML
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

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Kind
Protein
Organism
Peptoclostridium difficile
Pharmacological action
Yes
Actions
Antibody
General Function
Glucosyltransferase activity
Specific Function
Cytotoxin.
Gene Name
toxB
Uniprot ID
P18177
Uniprot Name
Toxin B
Molecular Weight
269709.285 Da

Drug created at November 02, 2016 18:42 / Updated at July 03, 2021 01:49