copper Cu 64 ucasareotide dasaroxetan

A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional chelator 5-(8-methyl-3,6,10,13,16,19-hexaaza-bicyclo[6.6.6]icosan-1-ylamino)-5-oxopentanoic acid (MeCOSar) and labeled with the positron emission tomography (PET) tracer copper Cu 64, which may be used to image somatostatin receptor (SSTR)-expressing neuroendocrine tumors (NETs) upon PET. Upon administration of copper Cu 64 ucasareotide dasaroxetan, the TATE moiety targets and binds to SSTRs, with high affinity for type 2 SSTR, present on the cell membranes of many types of NETs. This allows for visualization of SSTR-positive tumor cells upon PET. TATE is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine. SSTRs have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTRs.