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225Ac-Macropa-trastuzumab-PEG6-DM1

Development stage: Preclinical
Lead developer: CHU de Québec-Université Laval
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration: Intravenous

Overview

**225Ac-Macropa-trastuzumab-PEG6-DM1** is an investigational preclinical anti-HER2 antibody-drug radioconjugate developed for targeted alpha radiotherapy of HER2-positive breast cancer, including trastuzumab-resistant and T-DM1-resistant disease. It combines the HER2-directed monoclonal antibody trastuzumab, a PEG6-linked DM1 maytansinoid cytotoxic payload, the p-SCN-macropa actinium chelator, and the alpha-emitting radionuclide actinium-225. HER2-mediated tumor localization and internalization support intracellular DM1-mediated microtubule disruption while actinium-225 delivers high-linear-energy-transfer alpha radiation that causes localized DNA damage. In HER2-positive breast-cancer xenograft models, the construct showed greater antitumor activity than trastuzumab-PEG6-DM1, including activity in trastuzumab-resistant JIMT-1 tumors. ([jnm.snmjournals.org](https://jnm.snmjournals.org/content/65/supplement_2/242451))

Other names: 225Ac-Macropa-trastuzumab-PEG6-DM1[225Ac]Ac-Macropa-trastuzumab-PEG6-DM1

Targets

TUBB (Tubulin (alpha and beta subunits))DNAERBB2 (Erb-b2 receptor tyrosine kinase 2)

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