Antibody-Antibiotic Conjugation

BOC Sciences has accumulated over a decade of expertise in antibody engineering, linker design, and pharmacological evaluation. Our scientific team is pioneering the development of antibody-antibiotic conjugates, leveraging their extensive knowledge to address the unique needs of your project.

What is an Antibody-Antibiotic Conjugate?

The antibody-antibiotic conjugate (AAC) is a cutting-edge approach to resolving the significant threat to global public health caused by antibiotic resistance. This approach will enhance the efficacy of conventional antibiotics and decrease the complexity of treating bacterial infections. The emergence of multidrug-resistant pathogens, such as Methicillin-resistant Staphylococcus aureus (MRSA) and Carbapenem-resistant Enterobacteriaceae (CRE), underscores the urgent need for innovative therapeutic strategies. The antibody-antibiotic conjugate can meet the need.

Antibodies are specialized proteins produced by the immune system to recognize and bind to specific antigens on pathogens, which means antibody-antibiotic conjugates also hold this capability to precise targets. That means conjugating antibodies with potent antibiotics can enable the selective delivery of antimicrobial agents directly to bacterial targets. That will reduce the risk of systemic toxicity and preserve the efficacy of antibiotics. This targeted delivery not only enhances the concentration of antibiotics at infection sites but also minimizes systemic exposure.

The synergistic combination of antibodies and antibiotics in conjugates offers several advantages over traditional antibiotic therapies. Antibodies can recognize bacterial surface antigens or virulence factors with high specificity, facilitating the precise localization of antibiotics to infected tissues or cells. This targeted approach is particularly advantageous in combating infections caused by antibiotic-resistant bacteria, where conventional treatments often fail due to resistance mechanisms such as efflux pumps or enzymatic degradation of antibiotics.

Moreover, antibody-antibiotic conjugates hold promise for addressing diverse clinical challenges, including infections associated with medical devices, biofilm-forming bacteria, and intracellular pathogens. They offer a multifaceted approach to overcoming barriers that limit the effectiveness of antibiotics, such as poor penetration into biofilms or bacterial cells. By enhancing the antimicrobial potency of antibiotics and mitigating resistance mechanisms, antibody-antibiotic conjugates represent a pivotal advancement in infectious disease management.

Continued research and development efforts are focused on optimizing the design, stability, and therapeutic efficacy of antibody-antibiotic conjugates. Advances in bioconjugation technologies, antibody engineering, and antibiotic formulation are driving innovation in this field, paving the way for the clinical translation of novel conjugates. These efforts aim to expand the applicability of antibody-antibiotic conjugates across various infectious diseases, improve patient outcomes, and contribute to the global fight against antibiotic resistance.

The Characteristics of Antibody-Antibiotic Conjugates (Mariathasan S., et al., 2017)

Antibody-Antibiotic Conjugates Mechanism of Action

The mechanism of action of antibody-antibiotic conjugates comprises the internalization of extracellular S. aureus and the killing of intracellular S. aureus bacteria by intracellular release of the active antibiotic.

1. Intracellular antibiotic activation: While in circulation, the AAC is a prodrug because the covalently linked dmDNA31 is inactive. The high affinity of the b-GlcNAc-WTA antibody to the highly abundant antigen on the surface of S. aureus ensures that S. aureus circulating in the bloodstream, or released from lysed infected host cells, are rapidly opsonized or tagged with TACs; a single bacterium can be coated with as many as 50,000 AAC molecules.

2. Cellular internalization: The S. aureus–AAC complexes are then internalized by both phagocytic and non-phagocytic cells. For phagocytic cells, such as neutrophils and macrophages, opsonized (AAC-tagged) bacteria are internalized through opsonophagocytosis. For non-phagocytic epithelial and endothelial cells, entry of AAC-tagged bacteria occurs through the endogenous host invasion mechanism of S. aureus, such as that mediated by fibronectin-binding protein. When AAC-tagged bacteria are sequestered within acidic endo-or phagolysosomes, cathepsins released within these subcellular vesicles can cleave the ValCit linker and release active antibiotics.

3. Efficient bacterial eradication: Entry of AAC-tagged bacteria into cells containing resident S. aureus and subsequent intracellular release of active antibiotics in these cells can then result in the elimination of tagged and bystander killing of untagged resident bacteria. By this mechanism, AAC molecules are able to concentrate active dmDNA31 specifically in a location where S. aureus is poorly treated by conventional antibiotics. Indeed, in vitro, AAC-tagged S. aureus have been shown to be efficiently killed inside every cell type tested, including human macrophages as well as human endothelial and epithelial cell lines.

Mechanisms of Action of Antibody–Antibiotic Conjugates. (Mariathasan S., et al., 2017)

Advantages of Antibody-Antibiotic Conjugates

Penetration Capabilities: The key advantage of antibody-antibiotic conjugates lies in their ability to penetrate bacterial biofilms and eliminate intracellular pathogens, areas where conventional antibiotics often fail. Bacterial biofilms, which are complex communities of bacteria encased in a protective matrix, pose a significant challenge for traditional antibiotics due to their limited penetration capabilities. Antibody-antibiotic conjugates, however, are designed to target these biofilms effectively, breaking down the protective barrier and delivering antibiotics directly to the bacterial cells within. This targeted approach is crucial for treating persistent infections associated with biofilms, such as those found in chronic wounds, medical device infections, and cystic fibrosis.

Intracellular Pathogen Eradication: Furthermore, antibody-antibiotic conjugates excel in addressing intracellular pathogens—bacteria that can invade and survive within host cells, evading the immune system and conventional antibiotic treatments. These conjugates utilize antibodies that specifically bind to bacterial antigens, facilitating the entry of the antibiotic into infected cells and ensuring the bacteria are eradicated from their intracellular hideouts. This capability is particularly important for treating infections caused by pathogens like Staphylococcus aureus and Mycobacterium tuberculosis, which can persist inside host cells and cause recurrent infections.

Targeted resistance prevention: By delivering potent antimicrobial action precisely where it's needed most, antibody-antibiotic conjugates significantly reduce the likelihood of resistance development. Traditional antibiotics often expose both harmful and beneficial bacteria to their effects, creating selective pressure that can lead to the emergence of resistant strains. In contrast, the targeted delivery system of antibody-antibiotic conjugates minimizes this selective pressure by focusing the antibiotic's activity exclusively on the pathogenic bacteria, thereby preserving the microbiome and reducing the chance of resistance.

Revolutionizing bacterial treatment: Our innovative conjugates at BOC Sciences are meticulously engineered to combine the strengths of both antibodies and antibiotics, offering a powerful solution to the limitations of conventional treatments. Through precision targeting and enhanced delivery mechanisms, our antibody-antibiotic conjugates promise to revolutionize the treatment of stubborn and resistant bacterial infections, providing new hope in the fight against antibiotic resistance.

Applications of Antibody-antibiotic conjugates

Infectious Diseases: In the realm of infectious diseases, antibody-antibiotic conjugates offer a promising solution for complex infections, including those caused by resistant bacterial strains. These conjugates are particularly effective against infections that conventional antibiotics struggle to treat, such as those involving multidrug-resistant bacteria and biofilms. By delivering antibiotics directly to the infection site, antibody-antibiotic conjugates can significantly improve treatment outcomes for chronic and severe infections.

Targeted Therapies: Additionally, these conjugates draw upon technologies pioneered by leaders in the development of antibody-drug conjugates (ADCs), highlighting their versatility in targeted therapies. This technology can be adapted for various medical applications, including the treatment of infections in immunocompromised patients and preventing post-surgical infections. By leveraging targeted delivery, our antibody-antibiotic conjugates at BOC Sciences provide a powerful and adaptable tool for addressing a wide range of medical challenges, enhancing the effectiveness and precision of antimicrobial treatments.

Solving Critical Challenges with Antibody-Antibiotic Conjugates

At BOC Sciences, we specialize in producing AACs to address some of the most pressing challenges in modern medicine. Our AACs are designed to combat the growing threat of antibiotic-resistant infections, which have rendered many conventional antibiotics ineffective. By harnessing the precision targeting capabilities of antibodies, our AACs can specifically target and neutralize multidrug-resistant bacterial pathogens such as Methicillin-resistant Staphylococcus aureus (MRSA) and Carbapenem-resistant Enterobacteriaceae (CRE).

This targeted approach not only enhances the therapeutic efficacy of antibiotics but also significantly reduces the collateral damage to healthy tissues, minimizing side effects and improving patient outcomes. Furthermore, our AACs are effective against biofilm-forming bacteria, which are notorious for their resistance to standard antibiotics and their role in chronic infections associated with medical devices. By delivering antibiotics directly to the infection site, our AACs can penetrate and disrupt biofilms, ensuring a more effective treatment.

Additionally, our technology addresses the challenge of intracellular pathogens by facilitating the delivery of antibiotics into host cells where these pathogens reside, thereby overcoming a major limitation of traditional antibiotic therapies. Through continuous innovation and rigorous quality control, BOC Sciences is committed to providing cutting-edge AAC solutions that not only enhance the potency of existing antibiotics but also pave the way for novel treatments, ultimately contributing to the global fight against antibiotic resistance.

Our Antibody-Antibiotic Conjugates Services

BOC Sciences offers comprehensive Antibody-Antibiotic Conjugates (AAC) services designed to meet the diverse needs of pharmaceutical and biotechnology research. Our AAC services combine cutting-edge antibody technology with potent antibiotics, enabling precise targeting and therapeutic efficacy against various diseases.

Wide Selection of Antibiotics: Access to a broad range of antibiotics, including both traditional and novel compounds.

Quality Assurance: Rigorous quality control measures to guarantee batch-to-batch consistency and reproducibility.

Application Support: Comprehensive technical support and consultation throughout the AAC development process.

Advantages of Choosing BOC Sciences

When you partner with BOC Sciences for your Antibody-Antibiotic Conjugates needs, you benefit from:

Expertise and Experience: Decades of experience in chemical and biochemical research, ensuring reliable and innovative solutions.

Customization Capability: Flexibility to tailor AAC services to specific research goals and project requirements.

Timely Delivery: Efficient project management to meet deadlines and milestones effectively.

Cost-Effectiveness: Competitive pricing without compromising on the quality and integrity of our services.

Choosing BOC Sciences means partnering with a trusted provider dedicated to advancing scientific research through innovative AAC solutions.