Radiopeptides for Targeted Radiotherapy
| Peptide receptor | Radioligands used in humans for therapy | Radioligands in development |
|---|---|---|
| Somatostatin | Carbohydrated derivatives and other biodistribution modifiers | |
| sst2 | 111In-DTPAOC | |
| 90Y-DOTATOC | ||
| 177Lu-DOTATATE | ||
| sst2, sst5 | 90Y-DOTA-lanreotide | |
| sst2, sst3, sst5 | DOTANOC | |
| DOTABOC | ||
| DOTANOCate | ||
| DOTABOCate | ||
| TETA-octreotide | ||
| Bombesin | ||
| GRP-R | 177Lu-BNN8 analog | Bombesin analogs, including BBN8 analog, DOTA-[Lys3]bombesin, and DOTA-PEG-BN(7–14) |
| Cholecystokinin | ||
| CCK2 | Minigastrin; CCK analog | |
| Oxytocin | DOTALVT |
DOTA = 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; DTPA = diethylenepentaacetic acid; 111In-DTPAOC = [111In-DTPA0,d-Phe1]octreotide; 90Y-DOTATOC = [90Y-DOTA,Tyr3]octreotide; 90Y-DOTA-lanreotide = [90Y-DOTA,Tyr3]lanreotide; 177Lu-DOTATATE = [177Lu-DOTA0,Tyr3,Thr8]octreotide; DOTANOC = [DOTA,1-Nal3]octreotide; DOTABOC = [DOTA,BzThi3]octreotide; DOTANOCate = [DOTA,1-Nal3,Thr8]octreotide; DOTABOCate = [DOTA,BzThi3,Thr8]octreotide; TETA-octreotide = 1,4,8,11-tetraazacyclotetradecane-N,N′,N″,N‴-tetraacetic acid-octreotide; 177Lu-BBN8 analog = 177Lu-DO3A-CH2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2; DOTA-[Lys3]bombesin = [DOTA-Lys3]bombesin; DOTA-PEG-BN(7–14) = [DOTA-PEG]bombesin; CCK2 = cholecystokinin dipeptide; DOTALVT = [DOTA,Lys8]vasotocin. Modified from Reubi et al. (7).