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trastuzumab-Gly5-PNU
- Development stage
- Unknown
- Lead developer
- Boehringer Ingelheim
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Trastuzumab-Gly5-PNU (also known as T-PNU) is a site-specific antibody-drug conjugate (ADC) developed by NBE-Therapeutics (now part of Boehringer Ingelheim) using its proprietary sortase-mediated antibody conjugation (SMAC) technology. It consists of the HER2-targeting monoclonal antibody trastuzumab conjugated to PNU-159682, an extremely potent anthracycline derivative, via a noncleavable pentaglycine (Gly5-EDA) linker. The payload, PNU-159682, acts as a DNA topoisomerase II inhibitor that induces potent cytotoxicity and immunogenic cell death, stimulating adaptive anti-tumor immunity. Trastuzumab-Gly5-PNU is designed to treat HER2-positive malignancies, including breast cancer, and has demonstrated efficacy in models resistant to trastuzumab and ado-trastuzumab emtansine (T-DM1), as well as in tumors with moderate HER2 expression levels.
- Other names
- Trastuzumab-Gly5-PNUTrastuzumab-Gly-5-PNUTrastuzumab-Gly 5-PNU
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TOP2A (DNA topoisomerase II)
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