Drug intelligence / Profile preview

trastuzumab emtansine + docetaxel

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Trastuzumab emtansine + docetaxel is a **combination therapy** consisting of the antibody-drug conjugate **trastuzumab emtansine** (T-DM1, also known as ado-trastuzumab emtansine) and **docetaxel**, a chemotherapeutic agent. Trastuzumab emtansine is composed of the monoclonal antibody trastuzumab linked via a stable thioether linker to the cytotoxic agent DM1, a microtubule inhibitor. Trastuzumab emtansine specifically targets HER2 (ErbB2)-overexpressing cancer cells, delivering DM1 directly to these cells, resulting in cell-cycle arrest and apoptosis through inhibition of microtubule polymerization. In addition to direct cytotoxicity, trastuzumab mediates inhibition of HER2 signaling and antibody-dependent cell-mediated cytotoxicity. Docetaxel is a microtubule-stabilizing chemotherapeutic agent that also induces mitotic arrest, but through a distinct mechanism. The combination shows enhanced antitumor activity in preclinical and clinical studies, most notably in HER2-positive metastatic and locally advanced breast cancer patients[1][3][4].

Other names
T-DM1 + docetaxelado-trastuzumab emtansine + docetaxel
02

Targets

TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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