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Updated: Sep 26, 2026

Analyzing Tumor and Tissue Distribution of Target Antigen Specific Therapeutic Antibody
Published on: May 16, 2020
Monoclonal antibody drug immunoconjugates for targeted treatment of cancer
Pamela A Trail1, H Dalton King, Gene M Dubowchik
1pamela.trail.b@bayer.com
Abstract:
Monoclonal antibodies (mAb) directed to tumor-associated antigens (TAA) or antigens differentially expressed on the tumor vasculature have been covalently linked to drugs that have different mechanisms of action and various levels of potency. The use of these mAb immunoconjugates to selectively deliver drugs to tumors has the potential to both improve antitumor efficacy and reduce the systemic toxicity of therapy. Several immunoconjugates, particularly those that incorporate internalizing antibodies and tumor-selective linkers, have demonstrated impressive activity in preclinical models. Immunoconjugates that deliver doxorubicin, maytansine and calicheamicin are currently being evaluated in clinical trials. The feasibility of using immunoconjugates as cancer therapeutics has been clearly demonstrated. Gemtuzumab ozogamicin, a calicheamicin conjugate that targets CD33, has recently been approved by the Food and Drug Administration (FDA) for treatment of acute myelogenous leukemia (AML). This review concentrates on the properties of the tumor and the characteristics of the mAb, linker, and drugs that influence the efficacy, potency, and selectivity of immunconjugates selected for cancer treatment.
Insights
Monoclonal antibody immunoconjugates selectively deliver potent drugs to tumors, enhancing efficacy and reducing toxicity. This approach shows promise for cancer treatment, with some conjugates already in clinical trials and one approved for leukemia.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- Monoclonal antibodies (mAbs) targeting tumor-associated antigens (TAAs) or tumor vasculature can be linked to potent drugs.
- These mAb immunoconjugates aim to selectively deliver therapeutics to tumors, potentially improving antitumor efficacy and reducing systemic toxicity.
Purpose of the Study:
- To review the properties of tumors, mAbs, linkers, and drugs that influence the efficacy, potency, and selectivity of immunoconjugates for cancer treatment.
- To highlight the demonstrated feasibility and ongoing evaluation of immunoconjugates in clinical settings.
Main Methods:
- Review of preclinical and clinical data on monoclonal antibody immunoconjugates.
- Analysis of factors influencing immunoconjugate performance, including antibody internalization, linker stability, drug potency, and tumor-specific antigen expression.
Main Results:
- Several immunoconjugates, especially those with internalizing antibodies and tumor-selective linkers, show significant activity in preclinical models.
- Immunoconjugates delivering doxorubicin, maytansine, and calicheamicin are in clinical trials, with Gemtuzumab ozogamicin approved for AML.
Conclusions:
- The use of immunoconjugates as cancer therapeutics is feasible and supported by clinical evidence.
- Optimizing tumor characteristics, mAb properties, linker technology, and drug selection is crucial for developing effective immunoconjugate therapies.
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