Mertansine, also called DM1 (and in some of its forms emtansine), is a thiol-containing maytansinoid that for therapeutic purposes is attached to a monoclonal antibody through reaction of the thiol group with a linker structure to create an antibody-drug conjugate (ADC).

2014年6月26日 · Ado-trastuzumab emtansine (T-DM1) is an antibody–drug conjugate that combines the antitumor properties of the humanized anti-human epidermal growth factor receptor 2 (HER2) antibody, trastuzumab, with the maytansinoid, DM1, a potent microtubule-disrupting agent, joined by a stable linker.

2014年3月5日 · Trastuzumab emtansine (T-DM1) is an antibody-drug conjugate that is effective and generally well tolerated when administered as a single agent to treat advanced breast cancer. Efficacy has now been demonstrated in randomized trials as first line, second line, and later than the second line treatment …

2019年12月16日 · Trastuzumab emtansine (T-DM1, Kadcyla®) is an antibody–drug conjugate (ADC) comprised of the humanised, monoclonal, anti-HER2 antibody trastuzumab conjugated via a non-cleavable...

2024年2月1日 · In this study, a Fab-nondestructive ADC loaded with maytansine (DM1) (T-NPLG-DM135) was prepared with drug-to-antibody ratio (DAR) of up to 35 by utilizing the carboxyl groups on the side-chain of poly (L-glutamic acid) (PLG) as the payload binding sites.

2023年3月1日 · Twenty candidate drugs are in current preclinical and clinical phases in DM1. Three new interventional first-in-human clinical trials got underway during 2021–2022. New clinical trials involve two nucleic acid-based therapies, and one repurposed molecule. Tideglusib metformin mexiletine are already in phase III clinical evaluation.

Trastuzumab emtansine (T-DM1) is an antibody–drug conjugate comprising trastuzumab and DM1, a microtubule polymerization inhibitor, covalently bound via a stable thioether linker.

2010年4月26日 · Trastuzumab-DM1 (T-DM1) is an antibody-drug conjugate that uses trastuzumab to specifically deliver the maytansinoid antimicrotubule agent DM1 to HER2-positive cells. This first-in-human study of T-DM1 evaluated safety, pharmacokinetics, and preliminary activity of T-DM1 in patients with advanced HER2-positive breast cancer.

2011年8月28日 · Synthetic derivatives of the microtubule-targeted agent maytansine, commonly known as drug maytansinoids or DMs, are emerging as potential cancer therapeutics. DM1 is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumo …

2013年2月22日 · The new drug carries a boxed warning alerting patients and health care professionals that ado-trastuzumab emtansine can cause reductions in left ventricular ejection fraction, liver toxicity, and death. The drug can also cause severe birth defects, so a patient's pregnancy status should be determined prior to treatment.