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Bezlotoxumab | CAS No: 1246264-45-8 | GMP-certified suppliers
A medication that reduces recurrence of Clostridioides difficile infection in high-risk patients receiving antibacterial therapy, indicated for use in adults and children aged one year and older.
Therapeutic categories
Amino Acids, Peptides, and ProteinsAntibacterial monoclonal antibodiesAntibodiesAntibodies, MonoclonalAntibodies, NeutralizingAntiinfectives for Systemic Use
Generic name
Bezlotoxumab
Molecule type
biotech
CAS number
1246264-45-8
DrugBank ID
DB13140
Approval status
Approved drug, Investigational drug
ATC code
J06BC03
Primary indications
- Bezlotoxumab is indicated to reduce the recurrence of _Clostridioides difficile_ infection (CDI) in patients who are receiving antibacterial drug treatment for CDI and are at high risk for CDI recurrence
- [L46976, L47191] In the US, the drug is approved for use in patients one year of age and older
- In Europe, it is approved in adults only
Product Snapshot
- Bezlotoxumab is an injectable monoclonal antibody formulated as an intravenous solution
- It is primarily used to reduce the recurrence of Clostridioides difficile infection in patients undergoing antibacterial treatment and at high risk of infection recurrence
- Bezlotoxumab is approved in both the US (for patients aged one year and older) and the EU (for adult patients)
Clinical Overview
Bezlotoxumab is a fully humanized Immunoglobulin G1 (IgG1) kappa monoclonal antibody designed to reduce the recurrence of Clostridioides difficile infection (CDI). It specifically targets and neutralizes C. difficile toxin B, a key virulence factor responsible for the pathogenesis of CDI. The antibody received FDA approval on October 21, 2016, for use in patients aged one year and older and has been authorized for adult use in the European Union since January 2017.
Clinically, bezlotoxumab is indicated as an adjunctive treatment for patients at high risk of CDI recurrence who are undergoing antibacterial therapy for CDI. The recurrence of CDI is a significant clinical challenge due to the persistent role of C. difficile toxins in mucosal injury and inflammation.
Pharmacodynamically, bezlotoxumab binds with high affinity to toxin B, neutralizing its effects by blocking the toxin’s interaction with host cell receptors. In vitro studies demonstrate that bezlotoxumab inhibits toxin B-induced expression of proinflammatory cytokines such as tumor necrosis factor-alpha (TNF-α) and interleukin-1 (IL-1) in immune and colonic cells. Clinical trials have shown a reduced rate of CDI recurrence in patients treated with bezlotoxumab compared to placebo.
Mechanistically, C. difficile infection involves the secretion of two exotoxins, toxin A and toxin B. These toxins bind to colonocyte surface receptors and are internalized, leading to cellular glucosylation of small GTPases such as Rho and Rac. This disrupts cytoskeletal integrity and cellular homeostasis, inducing epithelial damage and apoptosis. Bezlotoxumab selectively binds to two epitopes within the C-terminal CROP domain of toxin B, limiting its capacity to bind host receptors and thereby neutralizing toxin activity. The antibody does not interact with toxin A.
Key ADME characteristics include intravenous administration with a distribution consistent with large monoclonal antibodies. Bezlotoxumab is eliminated via proteolytic catabolism typical of IgG antibodies; its half-life supports dosing aligned with antibacterial therapy for CDI.
Safety and toxicity data indicate that bezlotoxumab is generally well tolerated. Adverse reaction profiles align with immune-based therapies, necessitating monitoring in patients with hypersensitivity or immunological conditions.
Notable brand names include Zinplava, marketed for adjunctive use in CDI treatment to reduce recurrence risk. Its use is primarily clinical, integrated within CDI management protocols focusing on reducing relapse rates.
For pharmaceutical sourcing, procuring bezlotoxumab as an active pharmaceutical ingredient (API) demands consideration of its biological origin, emphasizing GMP-compliant production under stringent biotechnological manufacturing conditions. Quality control must ensure antibody specificity, purity, and consistent binding affinity to maintain clinical efficacy and regulatory compliance. Storage and handling protocols should preserve monoclonal antibody stability to prevent degradation and loss of activity.
Clinically, bezlotoxumab is indicated as an adjunctive treatment for patients at high risk of CDI recurrence who are undergoing antibacterial therapy for CDI. The recurrence of CDI is a significant clinical challenge due to the persistent role of C. difficile toxins in mucosal injury and inflammation.
Pharmacodynamically, bezlotoxumab binds with high affinity to toxin B, neutralizing its effects by blocking the toxin’s interaction with host cell receptors. In vitro studies demonstrate that bezlotoxumab inhibits toxin B-induced expression of proinflammatory cytokines such as tumor necrosis factor-alpha (TNF-α) and interleukin-1 (IL-1) in immune and colonic cells. Clinical trials have shown a reduced rate of CDI recurrence in patients treated with bezlotoxumab compared to placebo.
Mechanistically, C. difficile infection involves the secretion of two exotoxins, toxin A and toxin B. These toxins bind to colonocyte surface receptors and are internalized, leading to cellular glucosylation of small GTPases such as Rho and Rac. This disrupts cytoskeletal integrity and cellular homeostasis, inducing epithelial damage and apoptosis. Bezlotoxumab selectively binds to two epitopes within the C-terminal CROP domain of toxin B, limiting its capacity to bind host receptors and thereby neutralizing toxin activity. The antibody does not interact with toxin A.
Key ADME characteristics include intravenous administration with a distribution consistent with large monoclonal antibodies. Bezlotoxumab is eliminated via proteolytic catabolism typical of IgG antibodies; its half-life supports dosing aligned with antibacterial therapy for CDI.
Safety and toxicity data indicate that bezlotoxumab is generally well tolerated. Adverse reaction profiles align with immune-based therapies, necessitating monitoring in patients with hypersensitivity or immunological conditions.
Notable brand names include Zinplava, marketed for adjunctive use in CDI treatment to reduce recurrence risk. Its use is primarily clinical, integrated within CDI management protocols focusing on reducing relapse rates.
For pharmaceutical sourcing, procuring bezlotoxumab as an active pharmaceutical ingredient (API) demands consideration of its biological origin, emphasizing GMP-compliant production under stringent biotechnological manufacturing conditions. Quality control must ensure antibody specificity, purity, and consistent binding affinity to maintain clinical efficacy and regulatory compliance. Storage and handling protocols should preserve monoclonal antibody stability to prevent degradation and loss of activity.
Identification & chemistry
| Generic name | Bezlotoxumab |
|---|---|
| Molecule type | Biotech |
| CAS | 1246264-45-8 |
| UNII | 4H5YMK1H2E |
| DrugBank ID | DB13140 |
Pharmacology
| Summary | Bezlotoxumab is a monoclonal antibody targeting Clostridium difficile toxin B, neutralizing its pathological activity by binding to epitopes in the toxin’s C-terminal domain and preventing receptor interaction. By inhibiting toxin B, bezlotoxumab mitigates toxin-induced disruption of host cell signaling, inflammation, and epithelial damage associated with C. difficile infection. This mechanism supports its therapeutic use aimed at reducing recurrence risk in patients undergoing antibacterial treatment for C. difficile infection. |
|---|---|
| Mechanism of action | _C. difficile_ infections are caused by two exotoxins, toxin A and toxin B. Exotoxins are believed to bind to cell surface receptors expressed on colonocytes and are internalized via endocytosis. This process is followed by the acidification of the endosome, leading to a conformation change of the toxin, allowing for the transport of the endosome, autocleavage of the toxin via a cysteine protease domain, and the release of glucosyltransferase domain (GTD) from the endosome to the host cell cytoplasm. GTD glucosylates and inactivates small GTPases, such as Rac and Rho, critical for maintaining the actin cytoskeleton, cell adhesion, epithelial permeability, and other cellular function and homeostasis processes. Exotoxins eventually induce apoptosis and cell loss.[A18722, A260101] Endotoxins also promote the release of proinflammatory mediators that recruit neutrophils and macrophages to the injury site, further aggravating the gut injury and damage. _C. difficile_ infections are associated with a high risk of recurrence.[A260101, A260106] Bezlotoxumab binds to _C. difficile_ toxin B and neutralizes it. According to the findings of surface plasmon resonance analysis, bezlotoxumab binds to the toxin via two epitopes in the C-terminal CROP domain of the toxin, partially blocking the putative receptor binding pockets and preventing it from binding to host cell receptors. Bezlotoxumab does not bind to _C. difficile_ toxin A. |
| Pharmacodynamics | Bezlotoxumab directly neutralizes the toxic effects of _C. difficile_ by binding to the toxin with high affinity.[A260106, A260096, L46976] _In vitro_, bezlotoxumab inhibited _C. difficile_ toxin B-mediated expression of tumour necrosis factor-alpha (TNF-α) and interleukin-1 (IL-1) in human peripheral blood monocyte cells and human colonic and explants. In clinical trials, the rate of recurrent _C. difficile_ infection was lower in patients at risk for recurrent _C. difficile_ infection receiving bezlotoxumab compared to placebo. The administration of bezlotoxumab plus [actoxumab], another antibody directed against the _C. difficile_ toxin resulted in dose-dependent protection against _C. difficile_ toxin-induced damage and inflammation, as well as a reduced recurrence of _C. difficile_ infection in mice. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Clostridium difficile Toxin B | Peptoclostridium difficile | antibody, neutralizer |
ADME / PK
| Absorption | After a single intravenous dose of 10 mg/kg bezlotoxumab, geometric mean AUC<sub>0-∞</sub> and C<sub>max</sub> were 53000 mcg x h/mL and 185 mcg/mL, respectively, in patients with CDI. |
|---|---|
| Half-life | Based on a population pharmacokinetic analysis, the geometric mean (%CV) elimination half-life is approximately 19 days (28%). |
| Protein binding | No information is available. |
| Metabolism | Bezlotoxumab undergoes protein catabolism.[A260106, L360] |
| Route of elimination | Bezlotoxumab is mainly eliminated by catabolism. |
| Volume of distribution | Based on a population pharmacokinetic analysis, the geometric mean (%CV) volume of distribution was 7.33 L (16%). |
| Clearance | Based on a population pharmacokinetic analysis, the geometric mean (%CV) clearance of bezlotoxumab was 0.317 L/day (41%). The clearance of bezlotoxumab increased with increasing body weight: the resulting exposure differences are adequately addressed by the administration of a weight-based dose. |
Formulation & handling
- Bezlotoxumab is a biotech-derived injectable solution intended for intravenous administration only.
- As a peptide-based biologic, it requires careful handling to maintain stability and prevent denaturation.
- The liquid concentrate formulation should be stored and handled under recommended cold chain conditions to preserve efficacy.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's primary patent protection has expired in both the EU and US, allowing for generic market entry and increased competition. The product is now in a mature phase of its lifecycle across these regions. |
|---|
| Markets | EU, US |
|---|
Supply Chain
| Supply chain summary | Bezlotoxumab is marketed under the brand name Zinplava in both the US and EU markets, indicating a presence in major regulatory regions. The supply landscape involves originator companies responsible for its production and distribution. Given the absence of generic alternatives listed, patent protection likely remains in place, suggesting limited or no generic competition currently. |
|---|
Safety
| Toxicity | The intravenous LD<sub>50</sub> was >125 mg/kg in mice. There is no clinical experience with the overdosage of bezlotoxumab. In clinical trials, healthy subjects received up to 20 mg/kg, which was generally well tolerated. In case of overdose, patients should be closely monitored for signs or symptoms of adverse reactions, and appropriate symptomatic treatment should be instituted. |
|---|
High Level Warnings:
- Intravenous LD50 in mice exceeds 125 mg/kg, indicating low acute toxicity
- Clinical administration up to 20 mg/kg was generally well tolerated in healthy subjects
- Overdose management requires monitoring for adverse reactions and implementation of symptomatic treatment
Bezlotoxumab is a type of Antibacterials
Antibacterials, a category of pharmaceutical active pharmaceutical ingredients (APIs), play a crucial role in combating bacterial infections. These APIs are chemical compounds that target and inhibit the growth or kill bacteria, helping to eliminate harmful bacterial pathogens from the body.
Antibacterials are essential for the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and more. They are commonly prescribed by healthcare professionals to combat both mild and severe bacterial infections.
Within the category of antibacterials, there are different classes and subclasses of APIs, each with distinct mechanisms of action and target bacteria. Some commonly used antibacterials include penicillins, cephalosporins, tetracyclines, macrolides, and fluoroquinolones. These APIs work by interfering with various aspects of bacterial cellular processes, such as cell wall synthesis, protein synthesis, DNA replication, or enzyme activity.
The development and production of antibacterial APIs require stringent quality control measures to ensure their safety, efficacy, and purity. Pharmaceutical manufacturers must adhere to Good Manufacturing Practices (GMP) and follow rigorous testing protocols to guarantee the quality and consistency of these APIs.
As bacterial resistance to antibiotics continues to be a significant concern, ongoing research and development efforts aim to discover and develop new antibacterial APIs. The evolution of antibacterials plays a crucial role in combating emerging bacterial strains and ensuring effective treatment options for infectious diseases.
In summary, antibacterials are a vital category of pharmaceutical APIs used to treat bacterial infections. They are designed to inhibit or kill bacteria, and their development requires strict adherence to quality control standards. By continually advancing research in this field, scientists and pharmaceutical companies can contribute to the ongoing battle against bacterial infections.
