Bezlotoxumab

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.

Reduce drug development failure rates

Build, train, & validate machine-learning models
with evidence-based and structured datasets.

See how

Build, train, & validate predictive machine-learning models with structured datasets.

See how

Associated Conditions

Clostridium difficile infection recurrence

Contraindications & Blackbox Warnings

Avoid life-threatening adverse drug events

Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.

Learn more

Avoid life-threatening adverse drug events & improve clinical decision support.

Learn more

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.

Target	Actions	Organism
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

Improve decision support & research outcomes

With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.

Learn more

Improve decision support & research outcomes with our structured adverse effects data.

Learn more

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.

Drug	Interaction
Integrate drug-drug interactions in your software
Abciximab	The risk or severity of adverse effects can be increased when Abciximab is combined with Bezlotoxumab.
Adalimumab	The risk or severity of adverse effects can be increased when Adalimumab is combined with Bezlotoxumab.
Aducanumab	The risk or severity of adverse effects can be increased when Aducanumab is combined with Bezlotoxumab.
Alemtuzumab	The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Bezlotoxumab.
Alirocumab	The risk or severity of adverse effects can be increased when Alirocumab is combined with Bezlotoxumab.
Amivantamab	The risk or severity of adverse effects can be increased when Bezlotoxumab is combined with Amivantamab.
Anifrolumab	The risk or severity of adverse effects can be increased when Anifrolumab is combined with Bezlotoxumab.
Ansuvimab	The risk or severity of adverse effects can be increased when Bezlotoxumab is combined with Ansuvimab.
Anthrax immune globulin human	The 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.

Identify potential medication risks

Easily compare up to 40 drugs with our drug interaction checker.

Get severity rating, description, and management advice.

Learn more

Food Interactions

No interactions found.

Products

Drug product information from 10+ global regions

Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.

Access now

Access drug product information from over 10 global regions.

Access now

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Zinplava	Injection, solution, concentrate	25 mg/ml	Intravenous	Merck Sharp & Dohme B.V.	2020-12-18	Not applicable
Zinplava	Injection, solution	25 mg/1mL	Intravenous	Merck Sharp & Dohme Llc	2016-10-21	Not applicable

Chemical Identifiers

UNII: 4H5YMK1H2E
CAS number: 1246264-45-8

References

General References

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]
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]
Ghetie V, Ward ES: Transcytosis and catabolism of antibody. Immunol Res. 2002;25(2):97-113. [Article]
FDA Monograph for Zinplava [Link]

External Links

PubChem Substance: 347911429
RxNav: 1855048
Wikipedia: Bezlotoxumab

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Clostridium difficile infection recurrence	1
4	Not Yet Recruiting	Treatment	Clostridioides Difficile / Clostridium Infections / Pseudomembranous Enterocolitis	1
4	Recruiting	Prevention	C. Diff. Infections / Crohn's Disease (CD) / Inflammatory Bowel Diseases (IBD) / Ulcerative Colitis	1
4	Recruiting	Treatment	Clostridium Difficle Colitis / Clostridium; Sepsis	1
4	Terminated	Prevention	Clostridium Difficile	1
4	Unknown Status	Prevention	Clostridium difficile infection recurrence	1
3	Completed	Prevention	Clostridium Difficile Infection (CDI)	1
3	Completed	Treatment	Clostridium Difficile Infection (CDI)	2
2	Completed	Treatment	Clostridium Infections	1
2	Recruiting	Treatment	Clostridioides Difficile Infection / Clostridium difficile infection recurrence / Death / Organ Dysfunction Syndrome / Stool Microbiome	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Intravenous	25 mg/1mL
Injection, solution, concentrate	Intravenous	25 mg/ml
Injection, solution, concentrate	Intravenous; Parenteral	25 MG/ML

Prices