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.
Ref: Breeman, W. et al. Int. J. Cancer 104, 376 (2003); Chinol, M. et al. Semin. Nucl. Med. 32, 141 (2002); De Jong, M. et al. Semin. Nucl. Med. 32, 133 (2002).
Sequence (One-Letter Code)
DOTA-fCYwKTCT-ol (Disulfide bridge: 2-7)
Sequence (Three-Letter Code)
DOTA - D - Phe - Cys - Tyr - D - Trp - Lys - Thr - Cys - Thr - ol (Disulfide bridge: 2 - 7)