• Trastuzumab emtansine (T-DM1), an antibody-drug conjugate of trastuzumab and the cytotoxic agent emtansine (DM1), a maytansine derivative and microtubule inhibitor, provides benefit in patients with metastatic breast cancer that was previously treated with chemotherapy plus HER2-targeted therapy. (nih.gov)
  • T-DM1 is an antibody drug conjugate (ADC) which contains a chemotherapy (maytansine) stably linked to Herceptin. (pharmatimes.com)
  • T-DM1 retains the antibody functionalities of trastuzumab and adds the potency of a cytotoxic maytansine payload. (biorxiv.org)
  • Site-specific conjugation of a maytansine payload. (adcreview.com)
  • We have developed a trastuzumab-based ADC site-specifically conjugated to maytansine through a noncleavable linker. (biorxiv.org)
  • That's a HER2 antibody with a Herceptin-like backbone, but it is linked by a cleavable linker to a type of chemotherapy called maytansine that gets into those cancer cells. (onclive.com)
  • The eponymous natural cytotoxic agent maytansine is a 19-member lactam (ansa macrolide) structure originally isolated from the Ethiopian shrub Maytenus ovatus. (creativebiolabs.net)
  • Maytansine, a cancer drug was later isolated from the same plants in the United States. (or.ke)
  • SAR3419(huB4-DM4) is a new type of ADC that is composed of a humanized monoclonal IgG1 anti-CD19 antibody (huB4) attached to the potent cytotoxic drug, a maytansine derivative (N2′-deacetyl-N2′-[4-mercapto-4-methyl-1-oxopentyl] [DM4]), through a cleavable disulfide cross-linking agent, N-Succinimidyl-4-2-pyridyldithio butanoic acid (SPDB). (musechem.com)
  • This protein has been shown to be an effective transporter of the cytotoxic drug maytansine, which is used in antibody-based targeting of cancer cells. (nih.gov)
  • Mechanisms by which payload molecules can kill tumor cells include DNA cleavage and cross-linking (calicheamicin, pyrrolobenzodiazepine dimer), microtubule inhibition (auristatin, maleimidocaproyl monomethyl F, maytansine, maytansinoid DM4), topoisomerase inhibition (Deruxtecan, SN-38) and induction of apoptosis (Pseudomonas exotoxin A). Table 1 lists malignancies targeted by ADCs currently in the clinic. (pharmafocusamerica.com)
  • The most commonly used cytotoxins for ADCs under clinical development include auristatin, calicheamicin, maytansine and duocarmycin, though auristatin " dominates the market and accounts for over 50% of ADCs in clinical development ​," the report says. (biopharma-reporter.com)
  • The antibody-drug conjugate trastuzumab-DM1 (T-DM1) was designed to combine the biological activity of trastuzumab with the targeted delivery of a highly potent antimicrotubule agent, DM1 (N-methyl-N-[3-mercapto-1-oxopropyl]-l-alanine ester of maytansinol), a maytansine derivative, to HER2-positive breast cancer cells. (ccij-online.org)
  • CPGJ701 is a recombinant humanized anti-human epidermal growth factor receptor-2 (HER2) monoclonal antibody-derivative of the cytotoxic agent maytansine (DM1) conjugate for the treatment of HER2-positive metastatic breast cancer. (zhihuiya.com)
  • AVE9633 is an antibody-drug conjugate comprising the cytotoxic maytansinoid drug DM4 (N2′-deacetyl-N2′-(4-methyl-4(oxobutyldithio)-1-oxopentyl)-maytansine) linked via disulfide bonds to the anti-CD33 monoclonal antibody huMy9-6. (scienza-under-18.org)
  • Maytansine, a benzoansamacrolide, is a highly potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at subnanomolar concentrations. (adcreview.com)
  • Maytansine and its analogs (maytansinoids DM1 and DM4) are potent microtubule-targeted compounds that inhibit proliferation of cells at mitosis. (adcreview.com)
  • The potent cell killing ability of maytansine can be used in a targeted delivery approach, such as an antibody-drug conjugate, for the selective delivery of the drug and destruction of cancer cells. (adcreview.com)
  • DM4, a structural analogue of maytansine, is usually a new thiol-containing and potent maytansinoid. (scienza-under-18.org)
  • ADCs based on the natural product maytansine have been successfully employed clinically. (bvsalud.org)
  • Maytansine exhibits cytotoxicity against many tumor cell lines and may inhibit tumor growth in vivo. (adcreview.com)
  • The authors in this report further explore the maytansine scaffold to develop tubulin inhibitors capable of cell permeation. (bvsalud.org)