Drug intelligence / Profile preview

patritumab deruxtecan + pertuzumab + trastuzumab

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

Overview

This drug is a **three-agent combination therapy** comprising patritumab deruxtecan, pertuzumab, and trastuzumab, all of which are targeted agents used in the management of HER2-positive metastatic or locally advanced breast cancer in clinical trials. - **Patritumab deruxtecan (HER3-DXd)** is an investigational antibody-drug conjugate (ADC) targeted against the HER3 receptor, composed of a monoclonal antibody linked to a cytotoxic payload via a chemical linker. After binding to HER3, it is internalized by cancer cells and releases its cytotoxic drug to induce cell death[1][2]. - **Pertuzumab** is a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2), specifically binding domain II, and inhibiting HER2/HER3 dimerization, thus blocking downstream signaling that promotes tumor cell proliferation[3]. - **Trastuzumab** is a monoclonal antibody also targeting HER2, binding a different domain than pertuzumab (domain IV), and inducing antibody-dependent cell-mediated cytotoxicity, as well as blocking HER2-mediated signaling[3][6]. This three-drug regimen is being experimentally studied in HER2-positive metastatic breast cancer, with the goal of enhancing and broadening blockade of both HER2 and HER3-driven signaling pathways. The combination is not currently approved as a marketed product and is investigational.

Brand names
None specifically assigned to the combination
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB3 (Erb-b2 receptor tyrosine kinase 3)

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