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HTK03123
- Development stage
- Preclinical
- Lead developer
- BC Cancer
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
HTK03123 is a small-molecule radiopharmaceutical conjugate designed for the imaging and treatment of prostate cancer. It consists of a lysine-ureido-glutamate targeting moiety that binds with high affinity to prostate-specific membrane antigen (PSMA), a DOTA chelator for radiolabeling with isotopes such as Lutetium-177 or Gallium-68, and a specific albumin-binding motif (N-(4-(p-methoxyphenyl)butanoyl)-Gly) combined with a tranexamic acid-9-anthrylalanine affinity-modifying group. The albumin binder is engineered to prolong the drug's blood half-life, thereby increasing tumor accumulation and improving the therapeutic index by maximizing the tumor-to-kidney absorbed dose ratio. It was developed by researchers at BC Cancer and the University of British Columbia for the management of metastatic castration-resistant prostate cancer (mCRPC).
- Other names
- 177Lu-HTK0312368Ga-HTK03123
02
Targets
PSMA (Prostate-specific membrane antigen)
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