Mertansine

Mertansine, also known as DM1, is a microtubule inhibitor and is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC). ADC (antibody drug conjugates) are a promising therapeutic strategy. ADCs are composed of an antibody that can bind to a target in the cells, such as HER2 (human epidermal growth factor receptor 2) in breast cancer cells, a linker and a payload (cytotoxic drug). Mertansine is a microtubule inhibitor drug that can be easily used to prepare ADCs. One example is SHR-A1201. SHR-A1201 is an ADC composed of the anti-HER2 antibody trastuzumab, a SMCC linker and the microtubule inhibitor mertansine. It is under investigation for the treatment of HER2-positive breast cancer patients.