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Drug intelligence / Profile preview
[225Ac]Ac-HTK03149
- Development stage
- Preclinical
- Lead developer
- BC Cancer
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
[225Ac]Ac-HTK03149 is a preclinical-stage, prostate-specific membrane antigen (PSMA)-targeted radioligand therapy developed by BC Cancer and the University of British Columbia. It consists of the novel PSMA-targeting ligand HTK03149, which incorporates a lysine-urea-2-aminoadipic acid (Lys-urea-Aad) pharmacophore instead of the traditional lysine-urea-glutamic acid (Lys-urea-Glu) motif, labeled with the alpha-emitting radioisotope actinium-225 ([225Ac]). This structural modification is designed to maintain high binding affinity and tumor uptake while significantly reducing off-target accumulation in the kidneys and salivary glands, thereby minimizing potential renal and salivary toxicities. The therapeutic effect is mediated by the localized delivery of high-energy alpha radiation from actinium-225, which induces lethal double-strand DNA breaks in PSMA-expressing prostate cancer cells.
- Other names
- actinium (225Ac) HTK03149actinium-225 HTK03149actinium225 HTK03149actinium 225 HTK03149
02
Targets
PSMA (Prostate-specific membrane antigen)
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