Mylotarg-linker is a drug-linker conjugate for ADC by using N-Acetyl-Calicheamicin and Osu-AcBut-acetyl hydrozide derivative.
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Mylotarg-linker is a specialized drug-linker conjugate used in the synthesis of certain antibody-drug conjugates (ADCs), with N-Acetyl-Calicheamicin serving as the cytotoxic payload. N-Acetyl-Calicheamicin is a potent antitumor antibiotic known for its ability to induce double-stranded DNA breaks, thereby triggering apoptosis in target cells. This mechanism of action makes it a powerful agent in chemotherapy, particularly when delivered directly to cancer cells through the ADC approach. The Mylotarg-linker system facilitates the precise delivery of N-Acetyl-Calicheamicin to malignant cells, enhancing the therapeutic efficacy while minimizing systemic toxicity and off-target effects.
The key to the Mylotarg-linker's functionality is its integration with Osu-AcBut-acetyl hydrazide derivative, which acts as the connection between the antibody and the cytotoxic drug. This derivative provides a cleavable moiety that is specifically designed to remain stable in the bloodstream, preventing premature release of the drug. Upon reaching the target cancer cell, endosomal and lysosomal enzymes facilitate the cleavage of the linker, resulting in the localized release of N-Acetyl-Calicheamicin within the cancerous cells. This controlled release mechanism allows for a high concentration of the cytotoxic agent precisely where it is needed, thereby maximizing cell-killing efficacy while reducing collateral damage to normal tissues.
The application of the Mylotarg-linker system is particularly significant in the treatment of acute myeloid leukemia (AML), where it has been utilized to create therapies that target specific antigens expressed on the surface of leukemia cells. By conjugating N-Acetyl-Calicheamicin to antibodies that bind to CD33, a transmembrane receptor expressed on AML cells, this ADC approach affords a targeted therapeutic strategy that can induce remission in patients with limited treatment options. This specificity not only improves patient outcomes but also represents a step forward in the development of personalized oncology treatments that are tailored to the genetic and molecular profiles of individual cancers.
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