In the field of Antibody-Directed Enzyme Prodrug Therapy (ADEPT), Creative Biolabs is committed to fostering innovation and advancement, providing fresh solutions for cancer treatment worldwide. Our pre-enzyme drug synthesis services prioritize effective and accurate chemical synthesis techniques to enhance drug development, thereby laying a strong groundwork for the expanded use of ADEPT technology.

Introduction

The chemical synthesis of prodrug substances is particularly crucial in ADEPT development. By creating prodrugs, researchers can design and refine the precursors of the drugs, thereby enhancing their selectivity and efficacy while also minimizing side effects. Furthermore, the chemical synthesis of prodrugs contributes to a deeper understanding of enzyme catalytic mechanisms. By synthesizing specific precursor compounds, scientists can observe the reactive characteristics of enzymes during the catalytic process. Additionally, by designing prodrugs that activate under certain conditions, targeted drug release can be achieved, improving treatment efficiency while reducing the impact on healthy cells.

Fig.1 Biocatalyzed Synthesis of Drugs Chemicals.¹

Services

In the rapidly evolving landscape of ADEPT studies, Creative Biolabs is actively advancing cutting-edge research in this domain, particularly in the area of pre-enzyme drug chemical synthesis services. Our pre-enzyme drug synthesis services enable the provision of more accurate active ingredients for antibody drugs, enhancing therapeutic efficacy while minimizing side effects.

Synthesis of Pharmaceutical Precursors: Tailoring the synthesis of specific pharmaceutical precursors according to client specifications to lay the groundwork for subsequent drug development.

Structural Optimization and Modification: Offering structural optimization services for existing drug molecules by synthesizing various derivatives to enhance their efficacy and properties.

Design of Multi-step Synthesis Pathways: Creating and executing intricate multi-step synthesis pathways to ensure high yield and purity of target molecules.

Enzyme-Catalyzed Synthesis: Utilizing enzyme-catalysis techniques for the synthesis of specific compounds, providing environmentally friendly and sustainable synthesis options.

Safety and Efficacy Assessment: Conduct preliminary safety and efficacy evaluations during the chemical synthesis process, aiding clients in assessing the potential applications of the synthesized compounds.

Fig.2 A Modified RNA Oligonucleotide Synthesis Analysis.²

Process

1. Designing and Selecting Suitable Prodrugs: We will create appropriate prodrugs based on specific targets and disease types. Our prodrugs are characterized by low toxicity and can be converted into active drugs through specific enzyme catalysis, enabling selective targeting of cancer cells.

2. Synthesis of Prodrugs: Once the structure of the prodrug is finalized, our laboratory initiates the process of organic synthesis. This typically involves multiple reaction steps, including the introduction of functional groups, cyclization reactions, and purification, ultimately yielding high-purity prodrugs.

3. Enzyme Screening and Optimization: To achieve effective conversion of prodrugs, our team selects compatible enzymes. By screening various enzymes and conducting activity tests, we identify the most suitable ones. Additionally, we can enhance enzyme efficiency and selectivity through genetic engineering techniques.

4. Development of Targeted Antibodies: While optimizing the prodrugs and enzymes, our researchers will design and synthesize antibodies that specifically bind to tumor antigens.

5. Construction of Antibody-Enzyme Complexes: We couple the selected antibodies with enzymes using chemical cross-linking and other methods to form antibody-enzyme complexes. During this step, we prioritize the stability of the complexes and their appropriate release in vivo.

6. In Vitro and In Vivo Testing: After constructing the antibody-enzyme complexes, we first conduct in vitro experiments to validate their effectiveness against target cells, followed by animal studies to assess their therapeutic efficacy and safety.

Case Study

Recently, Creative Biolabs has successfully synthesized a series of high-purity proenzyme drugs, laying the groundwork for the ADEPT discovery.

a. Design of Target Molecules

Before synthesis, we begin by establishing the chemical structure of the target proenzymes. Based on the target antigens and the mechanism of action, we designed a range of candidate molecules and used computational chemistry software for structural optimization, ensuring that they exhibit favorable biocompatibility and specificity.

b. Synthesis Route Planning

Once the structures of the candidate molecules were determined, our scientists engaged in thorough planning of the synthesis routes. This phase included literature reviews, confirmation of functional groups, and optimization of reaction conditions. Additionally, small-scale experiments were conducted to identify the best reaction conditions and reagents.

c. Large-Scale Synthesis

Following the optimization of small-scale synthesis, our team moved on to the large-scale synthesis process. We selected appropriate reactors and solvents in our laboratory to enhance yield and purity. Key factors in this stage included controlling reaction conditions such as temperature, duration, and pH to prevent the formation of side products.

d. Purification and Characterization

After synthesis, Creative Biolabs employed HPLC and mass spectrometry (MS) for the purification and characterization of the synthesized proenzyme drugs, ensuring that the final products met the required structural and purity standards.

e. Biological Activity Assessment

Once we obtained purified proenzyme drugs, we conducted in vitro biological activity assessments to confirm their targeting efficacy and catalytic properties in cellular models.

Features

• Comprehensive Toxicity Assessment: Creative Biolabs offers an extensive range of toxicity testing protocols, including evaluations for acute, subacute, and chronic toxicity. Our systematic approach allows for a thorough examination of potential toxic reactions induced by various dosages over different periods.
• Diverse Animal Models: To more accurately replicate human physiological responses, Creative Biolabs uses a variety of animal models such as mice, rats, and dogs. We select the most appropriate subjects based on the specific characteristics of the drug, ensuring the reliability and translatability of the results.
• Tailored Services: In alignment with the unique attributes of different ADEPT candidate drugs and their development needs, we provide customized experimental designs and testing plans. This ensures compliance with specific regulatory requirements and facilitates the achievement of scientific goals.
• Comprehensive Data Analysis: Beyond standard toxicity assays, Creative Biolabs offers data analysis, statistical support, and report generation services. This enables research teams to thoroughly interpret experimental results, providing a solid scientific foundation for subsequent decision-making.
• Rapid Turnaround: Creative Biolabs is typically equipped with efficient experimental processes and ample resource allocation, allowing them to quickly address client needs, reduce research timelines, and assist in the swift transition of products into the clinical stage.

Whether you are in the early stages of new ADEPT development or conducting preclinical research, Creative Biolabs can provide you with tailored, efficient, and precise pre-enzyme drug chemical synthesis solutions. Our laboratory employs cutting-edge synthetic techniques to guarantee high yields and purity of compounds. If you're interested in learning more about our services, please feel free to contact us at any time!

References

1. Hoyos, Pilar, Vittorio Pace, and Andrés R. Alcántara. "Biocatalyzed synthesis of statins: A sustainable strategy for the preparation of valuable drugs." Catalysts 9.3 (2019): 260. Distributed under Open Access license CC BY, without modification.
2. Wiegand, Daniel J., et al. "Template-independent enzymatic synthesis of RNA oligonucleotides." Nature Biotechnology (2024): 1-11. Distributed under Open Access license CC BY 4.0, without modification.

For Research Use Only | Not For Clinical Use