Drug intelligence / Profile preview

trastuzumab deruxtecan + durvalumab

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 **combination therapy** consisting of **trastuzumab deruxtecan**, an antibody-drug conjugate (ADC), and **durvalumab**, an immune checkpoint inhibitor. - **Trastuzumab deruxtecan** targets and binds to HER2-expressing tumor cells using a humanized anti-HER2 monoclonal antibody. Once bound, the ADC is internalized, and its cytotoxic payload (a topoisomerase I inhibitor—deruxtecan) is released inside the tumor cell through cleavage of a linker by lysosomal cathepsins, causing inhibition of DNA replication and apoptosis. - **Durvalumab** is a monoclonal antibody that blocks PD-L1, preventing its interaction with PD-1 and CD80 and restoring antitumor immune responses by T cells. This combination aims to both **target and kill HER2-expressing cancer cells directly** and **enhance immune-mediated tumor cell destruction**. It is being investigated primarily for **stage III HER2-expressing inflammatory breast cancer** in neoadjuvant settings[1][5][7].

Brand names
ImfinziEnhertu
Other names
fam-trastuzumab deruxtecan-nxkitrastuzumab deruxtecandurvalumab
02

Targets

TOP1 (DNA Topoisomerase I)CD274 (Programmed cell death protein 1 ligand 1)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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