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actinium (225Ac) zadavotide guraxetan
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules, Peptides
- Administration
- Intravenous
01
Overview
Actinium (225Ac) zadavotide guraxetan (AZD2265) is a PSMA-targeted alpha radioconjugate (TAT) being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). The molecule consists of the alpha-emitting radioisotope actinium-225 conjugated to zadavotide guraxetan, a small-molecule ligand derived from the PSMA-I&T scaffold that binds with high affinity to prostate-specific membrane antigen (PSMA). PSMA is highly overexpressed on the surface of prostate cancer cells, allowing for the targeted delivery of high-energy alpha particles. These alpha particles induce complex double-strand DNA breaks within a short range (50-100 μm), leading to potent cell death while sparing distant healthy tissues. AstraZeneca acquired the asset through its acquisition of Fusion Pharmaceuticals and is currently evaluating it in the pivotal Phase III VECTRA-01 trial.
- Other names
- actinium (225Ac) zadavotide guraxetanActinium-225 PSMA-I&T[225Ac]-PSMA-I&T225Ac-zadavotide guraxetan
02
Targets
PSMA (Prostate-specific membrane antigen)DNA
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