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.
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism AClostridium difficile Toxin B antibodyPeptoclostridium 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 outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
- 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 softwareAbciximab 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 risksEasily 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 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 Zinplava Injection, solution, concentrate 25 mg/ml Intravenous Merck Sharp & Dohme B.V. 2020-12-18 Not applicable EU Zinplava Injection, solution 25 mg/1mL Intravenous Merck Sharp & Dohme Llc 2016-10-21 Not applicable US
Categories
- ATC Codes
- J06BC03 — Bezlotoxumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibacterial monoclonal antibodies
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Neutralizing
- Antiinfectives for Systemic Use
- Blood Proteins
- Globulins
- Immune Sera and Immunoglobulins
- Immunoglobulins
- Immunoproteins
- Proteins
- Serum Globulins
- Specific Immunoglobulins
- 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
- 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
- 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
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets

- 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