astatine-211-parthanatine

Astatine-211-parthanatine is an innovative **alpha-emitting radiopharmaceutical therapeutic** that targets **poly(adenosine-diphosphate-ribose) polymerase 1 (PARP1)** in cancer cells. It is specifically designed for the treatment of **high-risk neuroblastoma** and leverages a PARP inhibitor (parthanatine) radiolabeled with the alpha particle emitter **astatine-211**. This agent is part of a theranostic pair, complementing the diagnostic use of [18F]fluorthanatrace ([18F]FTT) for PET imaging of PARP1. The mechanism of action centers on selective delivery of potent alpha radiation to cancer cell nuclei via binding to PARP1, resulting in high cytotoxicity within tumor cells while minimizing off-target toxicity[1][5]. Preclinical studies have shown efficacy in patient-derived xenograft models of neuroblastoma with reversible hematologic toxicity, supporting ongoing clinical development. Astatine-211-parthanatine is structurally similar to rucaparib, differing at the radiolabel site, and demonstrates similar PARP1 binding characteristics in vitro[1][5]. The drug is being developed for other cancers expressing high levels of PARP1, including glioblastoma and ovarian cancer[3].

Brand names

[211At]PTT

Other names

astatine-211-parthanatineastatine211-parthanatineastatine 211-parthanatine211At-PTTAt211-ParthanatineAt-211-ParthanatineAt 211-Parthanatine[211At]At-PTT[211At]MM4