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trastuzumab-PHPMA conjugate

Development stage: Preclinical
Lead developer: University of Maryland, Baltimore
Modality: Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration: Intravenous

Overview

Trastuzumab-PHPMA conjugate is a preclinical polymer-protein conjugate consisting of the humanized anti-HER2 monoclonal antibody trastuzumab covalently linked to a water-soluble poly[N-(2-hydroxypropyl)methacrylamide] (PHPMA) copolymer backbone. Developed at the University of Maryland, Baltimore, this conjugate is designed to actively target HER2-overexpressing cancer cells while prolonging the therapeutic activity of the antibody. In vitro studies in HER2-positive breast cancer cell lines (such as BT-474 and SK-BR-3) have demonstrated that the conjugate retains the bioactivity of free trastuzumab, downregulates downstream MAPK and Akt signaling pathways with a prolonged effect, and exhibits synergistic growth inhibition when combined with the tyrosine kinase inhibitor PKI-166.

Other names: PHPMA-trastuzumab conjugatepoly[N-(2-hydroxypropyl)methacrylamide]-trastuzumab conjugatetrastuzumab-HPMA copolymer conjugatetrastuzumab-HPMA conjugateTRZ-HPMA copolymer conjugateTRZ-HPMA conjugateTRZ-PHPMA 1:1 conjugateTRZ-PHPMA conjugate

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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