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225Ac-DOTA-LM3
- Development stage
- Preclinical
- Lead developer
- Curanosticum Wiesbaden-Frankfurt
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
225Ac-DOTA-LM3 is an investigational targeted alpha-emitting radiopharmaceutical (radioligand therapy) designed for the treatment of somatostatin receptor subtype 2 (SSTR2)-positive neuroendocrine neoplasms (NENs), particularly well-differentiated grade 3 neuroendocrine tumors (NET G3). It consists of the somatostatin receptor antagonist DOTA-LM3 labeled with the alpha-emitting radionuclide actinium-225 (225Ac). Unlike traditional SSTR2 agonists (such as DOTATATE or DOTATOC), DOTA-LM3 is an antagonist that binds to a larger number of receptor sites on the cell membrane without being internalized, leading to higher tumor accumulation and longer retention. The actinium-225 payload delivers high-energy, short-range alpha particles that induce lethal double-strand DNA breaks in cancer cells while sparing surrounding healthy tissues. It is being evaluated in investigator-initiated clinical studies as monotherapy or in tandem with the beta-emitter lutetium-177 (177Lu).
- Other names
- 225Ac-LM3225Ac-labeled SSTR antagonist DOTA-LM3Actinium-225-DOTA-LM3Actinium225-DOTA-LM3Actinium 225-DOTA-LM3[225Ac]Ac-DOTA-LM3[225Ac]-DOTA-LM3
02
Targets
SSTR2 (Somatostatin receptor type 2)
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