Trastuzumab emtansine is an antibody-drug conjugate (ADC), a combination between a monoclonal antibody and a small-molecule drug. Each molecule of trastuzumab emtansine consists of a single trastuzumab molecule with several molecules of DM1, a cytotoxic maytansinoid, attached. [21]

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).

Jun 26, 2014 · 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.

Apr 23, 2023 · Kadcyla (Trastuzumab Emtansine, T-DM1), developed by Roche, is a HER2-targeted antibody-drug conjugate (ADC) which contains the humanized anti-HER2 IgG1, trastuzumab, covalently linked to the microtubule inhibitory drug DM1 (a maytansine derivative) via the stable thioether linker MCC (4-[N-maleimidomethyl] cyclohexane1-carboxylate).

Dec 16, 2019 · 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 maleimidomethyl...

Dec 10, 2024 · Currently approved ADC payloads, such as MMAE/MMAF, carchimycin, DM1/DM4, and SN38/Dxd, exhibit significantly higher toxicity—up to 1-2 orders of magnitude greater than traditional chemotherapy drugs, with some …

Antibody-drug conjugates (ADCs) represent a new class of cancer therapeutics. Their design involves a tumor-specific antibody, a linker and a cytotoxic payload. They were designed to allow specific targeting of highly potent cytotoxic agents to tumor cells whilst sparing normal cells.

Trastuzumab emtansine (T-DM1) was the first ADC approved in breast cancer in 2013 [5]. More than half a decade later, two more ADCs have received regulatory approvals in the setting of breast cancer, including trastuzumab deruxtecan (T-DXd), and sacituzumab govitecan (SG).

Dec 24, 2021 · Purpose: T-DM1 is an antibody-drug conjugate (ADC) consisting of trastuzumab and DM1 linked together. T-DM1 binds to human epidermal growth factor receptor-2 (HER2) in tumors and then triggers the endocytosis of T-DM1 and release of payload.

Oct 17, 2022 · In synthesis, the authors showed that conjugating the highly potent chemotherapy payload DM1 to trastuzumab with a stable linker allowed for an efficient delivery of the cytotoxin, with notable anticancer activity, convenient pharmacokinetic profile, and favorable toxicity profile.