Peptides  >  GPCR Peptide Ligands  >  Somatostatin  >>  DOTA-[Tyr3]-Octreotide; DOTA-TOC

DOTA-Octreotides are a group of compounds comprising DOTA, a metal chelator that carries a radionuclide and octreotide (an octapeptide that is a potent somatostatin (SST)) analog (where DOTA is tetra-aza-cyclododecane-N N’N’’N-’’’-tetra-acetate). Replacement of Phe by Tyr has been shown to increase affinity of DOTA-Octreotide radioconjugates to SST2-positive tumors both in-vitro and in-vivo. This form also has moderately high affinity for SST5 and intermediate affinity for SST3. Studies have shown therapeutic benefits including antimitotic effects and symptomatic cure of malignant insulinomas and gastrinomas.