Drug intelligence / Profile preview

trastuzumab emtansine + paclitaxel + pertuzumab

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

Overview

This is a **combination regimen** consisting of **trastuzumab emtansine** (an antibody-drug conjugate, also known as T-DM1), **paclitaxel** (a microtubule-stabilizing chemotherapy agent), and **pertuzumab** (a monoclonal antibody) used in the treatment of **HER2-positive breast cancer**. - **Trastuzumab emtansine** is an antibody-drug conjugate that combines trastuzumab, a humanized monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2), with emtansine (DM1), a cytotoxic agent inhibiting microtubule assembly. Trastuzumab directs the cytotoxic payload to HER2-overexpressing cells, resulting in cell death while sparing normal tissues[1][2][3][4][5][6]. - **Paclitaxel** is a classic antineoplastic chemotherapeutic that binds to and stabilizes tubulin, inhibiting cell division. - **Pertuzumab** is a monoclonal antibody that blocks HER2 dimerization, complementing trastuzumab’s blockade of the HER2 pathway and enhancing anti-tumor effects[3][4]. This multimodal combination is designed for **synergistic anti-tumor activity** in patients with advanced/metastatic or high-risk HER2-positive breast cancer, especially those previously treated with other HER2-directed therapies.

02

Targets

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

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