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ePSMA-DM1
- Development stage
- Preclinical
- Modality
- Alpha Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta Emitters → Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
01
Overview
ePSMA-DM1 is an experimental **theranostic small-molecule drug conjugate** being investigated for **prostate cancer**. It consists of a **glutamate-urea-lysine prostate-specific membrane antigen targeting vector** linked to the **maytansinoid cytotoxic payload DM1** and a **DOTA chelator**, enabling both targeted drug delivery and radiolabeling with diagnostic or therapeutic radionuclides such as indium-111 and lutetium-177. Mechanistically, the molecule binds **prostate-specific membrane antigen** on PSMA-expressing tumor cells, undergoes PSMA-specific uptake, and is designed to release DM1 in a reducing intracellular environment, where the payload disrupts microtubule function and kills cancer cells. Published preclinical work showed PSMA-specific cellular uptake, marked cytotoxicity in PSMA-positive cells, and successful radiolabeling for SPECT/CT imaging and potential radiotheranostic applications; development appears to remain at the preclinical stage.
- Other names
- ePSMA-DM1ePSMA-DM-1ePSMA-DM 1theranostic small-molecule drug conjugateT-SMDC
02
Targets
PSMA (Prostate-specific membrane antigen)TUBB (Tubulin (alpha and beta subunits))
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