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    Anti-tumor Antibody Prodrug Products

    Introduction Mechanism Advantages Technology Choose Us

    Introduction

    Antitumor antibody prodrugs (mAb-prodrugs) represent a revolutionary class of biologics designed to overcome the core challenge of modern oncology: the limited therapeutic window. By enhancing tumor specificity, mAb-prodrugs can widen or even create a therapeutic window for potent anticancer agents that are otherwise difficult or impossible to use due to poor tolerability. This sophisticated strategy involves administering an inactive drug form that is only converted into a fully active antibody or conjugate upon entering the diseased tissue. The mAb-prodrug concept has demonstrated proof-of-concept in numerous preclinical and early clinical trials, with published data supporting potent antitumor activity alongside improved safety profiles.

    The Action Mechanism of Antibody Prodrugs

    The core of the mAb-prodrug strategy relies on strategically leveraging a fundamental difference between healthy tissue and cancer. The tumor microenvironment (TME) is rich in overexpressed enzymes, particularly proteases. This universal feature provides the ideal, tumor-exclusive trigger. The underlying technology for mAb-prodrugs is protease-mediated activation, a finely tuned process that exploits the distinct biochemical landscape of cancer.

    • Protection Mechanism (Inactive form)

    Normal tissues maintain an elaborate and redundant control system over proteases, ensuring they remain inactive until needed. This robust control means the prodrug remains predominantly intact and inactive in circulation.

    • Activation Mechanism (Active form)

    The central component is the cleavable linker-substrate engineered to be recognized by the TME's high concentration of proteases. Examples of relevant proteases include Matrix Metalloproteinases (MMP) and Serine Proteases like matriptase.

    • The Molecular Switch

    Upon entering the TME, these upregulated proteases cleave the linker, the masking peptide is released, and the antibody becomes fully competent to bind its target. This mechanism is distinct from and superior to attempts using viral vectors for localized delivery, which have issues with inconsistent expression and systemic activity assessment.

    The Structure and Mechanism of Antibody Prodrug. (OA Literature)Fig.1 The Structure and Action Mechanism of Antibody Prodrug.1

    Advantages of Antibody Prodrugs

    The mAb-prodrugs offer distinct advantages over traditional monoclonal antibody (mAb) therapies, fundamentally changing the risk-benefit profile for patients.

    Mitigated On-Target, Off-Tumor Toxicity

    By preventing the prodrug from binding to antigens in healthy, non-malignant tissues, mAb-prodrugs dramatically reduce mechanism-dependent toxicities. This is critical for antigens that are merely overexpressed on tumor cells but still present in vital organs.

    Wider Therapeutic
    Index

    The platform allows the administration of the therapeutic agent at higher, more effective doses without incurring the severe systemic side effects associated with the unmasked parent antibody, thus truly expanding the therapeutic window.

    Unlocking Undruggable Targets

    mAb-prodrugs enable the targeting of antigens (CD71, high CTLA-4, EGFR) previously considered inaccessible to conventional ADCs and immunotherapies due to ubiquitous normal tissue expression or dose-limiting toxicity.

    Reduced Antigen-Dependent Clearance

    In the masked form, mAb-prodrugs exhibit reduced binding to peripheral targets, which prevents rapid sequestration and metabolism of the drug, resulting in a prolonged elimination half-life and potentially higher drug exposure in the tumor.

    Our Antibody Prodrug Technology

    While other mAb-prodrug strategies employ steric hindrance (using bulky domains to block antigen binding), Creative biolabs' platform is founded on affinity masking, a modular and quantifiable design strategy that delivers superior precision compared to generalized approaches.


    Specific Mask Identification

    A peptide is specifically identified and engineered to bind directly to the antibody's Complementarity-Determining Regions (CDR).


    Tunable Masking

    The masking efficiency is quantified and can be tuned by selecting peptides with varying degrees of affinity for the CDR. This precise control is vital for achieving the optimal therapeutic index.


    Model-Informed Design (QSP)

    We apply Quantitative Systems Pharmacology (QSP) modeling to rationally design antibody prodrug constructs. This predictive modeling suggests the need for an optimal mask strength (Kmask), which balances maximal protection and efficient activation.

    Choose Us

    Creative biolabs is your trusted partner in developing safer, more potent antibody therapeutics. By focusing on exquisite control over activation within the TME, we minimize serious toxicities, enable higher dosing, and expand the landscape of druggable targets. Our antitumor antibody prodrugs platform leverages proprietary affinity masking and QSP modeling to expand your target landscape and de-risk your lead candidates for the clinic.

    Contact Us for More Information and Discuss Your Project.

    Reference

    1. Long, Rou, et al. "Antibody-drug conjugates in cancer therapy: applications and future advances." Frontiers in Immunology 16 (2025): 1516419. Distributed under Open Access license CC BY 4.0, without modification. https://doi.org/10.3389/fimmu.2025.1516419
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