Drug intelligence / Profile preview

trastuzumab deruxtecan + pertuzumab

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

**Trastuzumab deruxtecan + pertuzumab** is a combination regimen consisting of the antibody-drug conjugate trastuzumab deruxtecan (T-DXd) and the monoclonal antibody pertuzumab, designed for the treatment of HER2-positive, locally advanced or metastatic breast cancer. Trastuzumab deruxtecan is an antibody-drug conjugate that targets HER2 receptors and delivers the cytotoxic payload deruxtecan to HER2-expressing cells, inducing cell death. Pertuzumab is a recombinant humanized monoclonal antibody that inhibits HER2 dimerization, further blocking HER2-mediated signaling. This combination provides a dual blockade of HER2 and leverages both targeted cytotoxicity and inhibition of downstream growth signals. The DESTINY-Breast09 phase III trial has demonstrated that this combination nearly doubles progression-free survival compared to the previous standard regimen (taxane, trastuzumab, pertuzumab) and is likely to change first-line treatment practice for metastatic HER2-positive breast cancer[3][5].

Brand names
Enhertu + Perjeta
Other names
fam-trastuzumab deruxtecan-nxki + pertuzumabT-DXd + pertuzumab
02

Targets

TOP1 (DNA Topoisomerase I)HER2 ECD subdomain II (Human epidermal growth factor receptor 2 dimerization interface)

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