Antibody-Drug Conjugates Targeting Delivery Development Services

Antibody-drug conjugates (ADCs) are targeted drug delivery systems in which specific antibodies are used to target specific cells and cytotoxic substances are coupled to them via linker molecules. Antibody-drug coupling technology uses monoclonal antibodies or other biological agents to deliver a highly active drug component to a target cell. In coupled form, highly active drug components can exhibit increased selective therapeutic activity, shielding non-target cells from many toxic effects and improving safety. CD Formulation is committed to the development of drug delivery technologies and their use to develop more targeted and safe products for the treatment of disease. Novel biocoupled drugs are also available in various payload and antibody forms to serve a variety of applications and indications.

ADCs for Drug Delivery

ADCs, as novel targeted drug delivery systems using monoclonal antibodies as carriers, consist of monoclonal monoclonal antibodies, cytotoxic small molecule drugs, and antibody-drug linkers. The main function of monoclonal antibodies is to act as drug carriers, controlling ADC drug targeting, delivering and enriching drugs to tumor sites, and the anti-tumor effect of ADC drugs depends mainly on the killing effect of selected cytotoxic small molecule drugs. The linker mainly plays a bridging role, carrying the functions of ADC stabilization, water solubility and intra-tumor cell release.

Optimal Design of ADCs

The development of ADCs depends mainly on the optimization of each parameter of ADCs, among which the selection of suitable antigen targets and coupling methods as well as the selection of the three components of ADCs (antibodies, coupling chains and cytotoxic drugs) are the focus of optimal design.

• Antibody and target selection

The selection of targets and antibodies is the first step in the design of ADC drugs. The role of antibodies is to act as carriers to load cytotoxic drugs to specifically bind to target cell surface antigens. These antigens will usually be involved in normal cell growth or proliferation processes and are typically cell surface proteins, glycoproteins or peptides.

• Choice of coupling chain and coupling method

The coupling chain is the bridge between the antibody and the cytotoxic drug. The ideal coupling chain must be stable in vitro or in circulation to prevent systemic toxicity due to early release of cytotoxic drugs, and at the same time be able to release effective cytotoxic drugs rapidly to kill cancer cells upon entry into cancer cells.

• Selection of cytotoxic drugs

Cytotoxic drugs are the key part of ADCs that exert anti-tumor effects. Currently, the most used cytotoxic drugs can be divided into two categories according to their mechanism of action: 1) DNA-acting calicheamicin (CLM); 2) microtubule protein inhibitors.

ADCs should have the Following Conditions

• High stability

ADCs must be structurally and chemically stable in the circulation to prevent premature release of cytotoxic drugs and to reduce their toxic accumulation in non-target tissues, and they need to have a long half-life. Therefore, the stability of the coupling chain of ADCs is strictly required to reduce systemic toxicity.

• Have a non-specific immune response

ADCs must maintain high immunoaffinity and must not disrupt the specific binding ability of the monoclonal antibody itself during the binding of cytotoxic drugs to the monoclonal antibody.

• High drug release capacity

ADCs enter cancer cells through internalization after specific binding to antigen, and release cytotoxic drugs through endosomal or lysosomal action, which can only work when the cytotoxic drugs reach effective concentration.

• Strong drug action

The released cytotoxic drug needs to be able to kill cancer cells even at very low concentrations.

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