Thus, the strategy of combining powerful cell killing ability of potent cytotoxic agents with target specificity symbolizes a potentially new model in treatment of cancer

Antibody drug conjugates are monoclonal antibody chemically coupled to a linker and cytotoxic drug. At present the therapeutic use of ADCs is focused almost completely on the treatment of cancer. The targets for ADCs do not need to be causal in tumor progression in contrast to small molecule cancer agents or function blocking monoclonal antibodies. The monoclonal antibodies used in first generation ADCs identified cell surface antigens with varying levels of tumor selectivity. It also included monoclonal antibodies that internalized following antigen binding and those that did not.

Non internalizing ADCs needed to remain entire in the circulation to be effective, and however selectively release active drug at the tumor site. Characteristically these ADCs make use of peptidyl linkers designed to be cleaved by enzymes such as cathepsins and matrix metalloproteinases articulated in the linker, or tumor that would liberate drug by hydrolysis at the slightly acidic pH observed in many solid tumors.

These non-internalizing ADCs did not show significant antigen specific activity for the most part, and did not improve the therapeutic index relative to that of the free drug. The use of MAbs that internalize following antigen binding has resulted in the design of linkers that are stable in circulation and efficiently release active drug following internalization, antigen specific binding, and trafficking to endosomes or lysosomes. Impressive preclinical and clinical activity has been demonstrated by internalizing ADCs.

Major advances in the efficacy and safety of ADCs have resulted from incorporating highly potent drugs and using stable linkers to better make use of the half life of the MAb component of the ADC. There are continuing efforts to increase the selectivity of ADC and efficacy by optimizing linkers, MAb attachment sites and cytotoxic payloads further.

For the design of ADC, the selection of suitable ADC targets remains a critical challenge. Characteristics of the ADC target can be used to guide the selection of linker that may be cleavable or non cleavable and the potency and characteristics of the released drug.

Though, further insight into the optimal design characteristics of effective ADCs will be best gained as additional clinical data become available. The emerging technologies that seek to further advance this exciting area of research are also increasing.

Our company has more than a decade of experience in Antibody Drug Conjugate (ADC) technology, which makes powerful monoclonal antibodies to treat the targeted diseased area more successfully.

The type of components of GAP antibody drug conjugate technology is the stable linkers and the synthetic cytotoxic agents. At various phases of clinical trials our ADCs have been shown to be approximately 5 times more efficient and roughly 10 times safer than the conventional chemotherapeutic agents.

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