[225Ac]Ac-DOTA-2Rs15d

[225Ac]Ac-DOTA-2Rs15d is a preclinical radiopharmaceutical consisting of the alpha-emitting radioisotope actinium-225 conjugated to the anti-HER2 single-domain antibody (sdAb) fragment 2Rs15d via a DOTA chelator. The 2Rs15d sdAb, also known as a nanobody, specifically targets the Human Epidermal Growth Factor Receptor 2 (HER2), which is overexpressed in various malignancies including breast, gastric, and ovarian cancers. By utilizing the high linear energy transfer (LET) of alpha particles, the drug induces potent DNA double-strand breaks in targeted tumor cells while minimizing damage to surrounding healthy tissue due to the short range of alpha radiation. Preclinical studies have demonstrated significant therapeutic efficacy in HER2-positive intraperitoneal ovarian cancer models, although some renal toxicity was observed due to kidney accumulation.

Other names

225Ac-labeled anti-HER2 sdAb225Ac-labeled 2Rs15d