trastuzumab-PNU

trastuzumab-PNU is a preclinical-stage antibody-drug conjugate (ADC) developed by NBE-Therapeutics (now Boehringer Ingelheim). It consists of the anti-HER2 monoclonal antibody trastuzumab site-specifically conjugated to a derivative of the highly potent anthracycline toxin PNU-159682 (such as PNU-EDA-Gly5) via a non-cleavable peptide linker using sortase-mediated antibody conjugation (SMAC) technology. Trastuzumab-PNU targets HER2-expressing tumor cells, where it is internalized and releases the PNU-159682 payload. PNU-159682 acts as an extremely potent DNA-damaging agent by intercalating into DNA, forming covalent adducts, and inhibiting topoisomerase II, leading to cell cycle arrest and apoptosis. In addition to direct cytotoxicity, trastuzumab-PNU has been shown to induce immunogenic cell death and stimulate anti-tumor immune responses, including CD8+ T-cell activation. It has been utilized primarily as a benchmark and proof-of-concept molecule for the SMAC technology platform and as an isotype control in preclinical oncology studies.

Other names

Tras-G5-PNUTras-G-5-PNUTras-G 5-PNUTras-PNUtrastuzumab-G5-PNUtrastuzumab-G-5-PNUtrastuzumab-G 5-PNUtrastuzumab-PNU-159682trastuzumab-PNU159682trastuzumab-PNU 159682trastuzumab-PNU-159682 antibody-drug conjugatetrastuzumab-PNU159682 antibody-drug conjugatetrastuzumab-PNU 159682 antibody-drug conjugatetrastuzumab-PNU-EDA-Gly5trastuzumab-PNU-EDA-Gly-5trastuzumab-PNU-EDA-Gly 5trastuzumab-PNU-EDA-Glys