Drug intelligence / Profile preview

[225Ac]Ac-macropa-nimotuzumab-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
Administration
Intravenous
01

Overview

[225Ac]Ac-macropa-nimotuzumab-PEG6-DM1 is a preclinical **anti-EGFR antibody-drug radioconjugate** for EGFR-positive colorectal cancer, including KRAS-mutant and BRAF V600E-mutant metastatic disease. It consists of the humanized anti-EGFR monoclonal antibody nimotuzumab, a PEG6-linked DM1 maytansinoid payload, and the alpha-emitting radionuclide actinium-225 chelated by macropa. EGFR-directed tumor localization enables delivery of both DM1-mediated microtubule disruption and localized high-linear-energy-transfer alpha radiation, producing enhanced cytotoxicity and durable antitumor responses in colorectal cancer xenograft models. ([citedrive.com](https://www.citedrive.com/en/discovery/an-anti-egfr-antibody-drug-radioconjugate-labeled-with-actinium-225-elicits-durable-anti-tumor-responses-in-kras-and-braf-mutant-colorectal-cancer/))

Other names
[225Ac]Ac-macropa-nimotuzumab-PEG6-DM1
02

Targets

TUBB (Tubulin (alpha and beta subunits))DNA

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