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HTK03121
- Development stage
- Preclinical
- Lead developer
- BC Cancer
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
HTK03121 is a prostate-specific membrane antigen (PSMA)-targeting radiopharmaceutical developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It is a DOTA-conjugated lysine-ureido-glutamate-based ligand that incorporates a tranexamic acid-9-anthrylalanine affinity-modifying group and an N-(4-(p-chlorophenyl)butanoyl)-Gly albumin-binding motif. The albumin binder is designed to enhance the blood residence time, thereby increasing tumor accumulation and improving the tumor-to-kidney absorbed dose ratio. Preclinical evaluations using Lutetium-177 (177Lu) labeling have shown that HTK03121 achieves significantly higher tumor uptake compared to the standard-of-care PSMA-617, suggesting potential for improved therapeutic efficacy with lower administered doses.
- Other names
- 177Lu-HTK03121
02
Targets
PSMA (Prostate-specific membrane antigen)
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