Drug intelligence / Profile preview

RO7881583

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

Overview

RO7881583 is an investigational antibody-drug conjugate (ADC) developed by Roche (Genentech) that targets the Human Epidermal Growth Factor Receptor 2 (HER2). It is designed to treat various HER2-expressing malignancies, including HER2-positive and HER2-low metastatic breast cancer, as well as other advanced solid tumors. The molecule consists of a HER2-targeted monoclonal antibody conjugated to a potent cytotoxic payload, specifically a topoisomerase I inhibitor, via a protease-cleavable linker. This mechanism allows for the targeted delivery of the chemotherapy agent directly into cancer cells upon binding and internalization, where the payload is released to induce DNA damage and apoptosis. RO7881583 is part of a next-generation ADC platform intended to provide enhanced efficacy and a favorable safety profile compared to earlier HER2-targeted therapies. It is currently being evaluated in early-phase clinical trials to determine its safety, pharmacokinetics, and preliminary anti-tumor activity.

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP1 (DNA Topoisomerase I)

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