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Antibody–drug conjugates are an example of bioconjugates and immunoconjugates. ADCs combine the targeting properties of monoclonal antibodies with the cancer-killing capabilities of cytotoxic drugs, designed to discriminate between healthy and diseased tissue.
Monomethyl auristatin E is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin.The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the antimitotic mechanism.
Trastuzumab is the anti-HER2 antibody; emtansine refers to the linker-drug (SMCC-DM1). The "ado-" prefix was added at the request of the FDA to help prevent dispensing errors . [ 31 ] [ 20 ] [ 32 ] During preclinical development and clinical trials, the drug was also known as trastuzumab-DM1 or trastuzumab-MCC-DM1 (after the codename for ...
Gemtuzumab ozogamicin, sold under the brand name Mylotarg®, is an antibody-drug conjugate (a drug-linked monoclonal antibody) that is used to treat acute myeloid leukemia (AML). [ 6 ] [ 8 ] [ 9 ] The most common side effects include infection, febrile neutropenia, decreased appetite, hyperglycemia, mucositis, hypoxia, hemorrhage, increased ...
These conjugates are used in immunotherapy [citation needed] and to develop monoclonal antibody therapy as a targeted form of chemotherapy [2] when they are often known as antibody-drug conjugates. When the conjugates include a radioisotope see radioimmunotherapy. When the conjugates include a toxin see immunotoxin.
Some dimeric pyrrolobenzodiazepines are used as the cytotoxic drug payloads in antibody-drug conjugates, for example in loncastuximab tesirine. History ...