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Search results for maytansine in Standardized Name (approximate match)
Status:
Investigational
Source:
USAN:SORAVTANSINE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Soravtansine (DM4-SULFO-TBA), a maytansinoid derivative, is an antineoplastic agent. Antibody–maytansinoid conjugates (like Mirvetuximab soravtansine) are in clinical trials for the treatment of various cancers. Thus, Mirvetuximab soravtansine (IMGN853) is an antibody-drug conjugate (ADC) that targets FRα (folate receptor alpha) for tumor-directed delivery of the maytansinoid DM4, a potent agent that induces mitotic arrest by suppressing microtubule dynamics.
Status:
Investigational
Source:
Sci Rep. Sep 2019;9(1):12760.: Phase 3 Human clinical trial Completed Breast Neoplasms/metabolism/mortality
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Maytansine is an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata. Maytansine inhibits the assembly of microtubules by binding to tubulin at or near the vinblastine-binding site, decreases microtubule dynamic instability and cause mitotic arrest in cells. It exerts cytotoxicity against a number of tumor cell lines and inhibits tumor growth in vivo. However, in human clinical trials, maytansine showed a small therapeutic window due to its neurotoxicity and harmful effects on the gastrointestinal tract. 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.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Mertansine (Maytansine) is a 19–member ansa macrolide structure attached to a chlorinated benzenering. It was originally isolated from the shrub Maytenus ovatus. Mertansine (DM1) is a tubulin inhibitor, it inhibits the assembly of microtubules by binding to tubulin, with a linker structure can create an antibody-drug conjugate (ADC). Mertansine is a potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at sub-nanomolar concentrations. The antimitotic effect of maytansine has been attributed to its ability to inhibit microtubule assembly by binding to tubulin with a KD of ~ 1 umol/L, at or near the vinblastine-binding site. Experimental ADCs with the SPP-DM1 design include lorvotuzumab mertansine. DM1 can also be linked to an antibody using the SMCC (4-(3-mercapto-2,5-dioxo-1-pyrrolidinylmethyl)-cylohexanecarboxylic acid) linker, in which case the International Nonproprietary Name of the conjugate formed contains the word emtansine. DM1 and its attachment via these linkers result from ImmunoGen Inc research. Trastuzumab emtansine (T-DM1) is an anti-HER2/neu antibody-drug conjugate.