Drug intelligence / Profile preview

trastuzumab deruxtecan + paclitaxel + trastuzumab + pertuzumab

Development stage
Unknown
Lead developer
Daiichi Sankyo
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** composed of four agents: **trastuzumab deruxtecan**, **paclitaxel**, **trastuzumab**, and **pertuzumab**. - **Trastuzumab deruxtecan** is an antibody-drug conjugate targeting HER2 (human epidermal growth factor receptor 2), delivering a cytotoxic topoisomerase I inhibitor payload specifically to HER2-expressing cells. - **Paclitaxel** is a taxane-class microtubule inhibitor used as chemotherapy. - **Trastuzumab** and **pertuzumab** are both monoclonal antibodies directed against different domains of HER2, together providing dual blockade and enhancing antitumor activity through inhibition of proliferation, induction of ADCC (antibody-dependent cellular cytotoxicity), and complement-mediated cytotoxic effects[4]. This combination represents an investigational or off-label use (distinct from standard-of-care combinations) and may be studied in clinical trials as an experimental regimen for **HER2-positive metastatic breast cancer**.

02

Targets

TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))

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