188Re-P2045 (BAY86-5284, Tozaride) is a 11-amino acid proprietary somatostatin peptide conjugate which was labeled either with 188Re or 99mTc. In June 2014, this compound was granted Orphan Drug Designation by the U.S. FDA for the treatment of pancreatic cancer.
188Re-P2045 was designed for the treatment of neuroendocrine tumors and the first trials were targeted against lung cancers. This drug could be developed for both small cell lung cancer and non-small cell lung cancer. However, it seems that the principal indication, supported now by the orphan drug status, will be oriented to the treatment of pancreas cancer.
This molecule went through one single Phase I clinical trial in small cell lung cancer and performed as early as 2004-2005. A new study is posted on the clinical trial database and was supposed to start in January 2014 but was withdrawn due to the departure of the principal investigator from the study institution.
Target/Mechanism: somatostatine receptors
Leading Emitter: beta electrons (β–)