Somatostatin Analog Affinities
| Affinity | |||||||
| Somatostatin analog | Chemical structure | sstr1 | sstr2 | sstr3 | sstr4 | sstr5 | Status |
| Agonist | |||||||
| In-DTPA-octreotide* | 111In-DTPA-d-Phe-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)Thr(ol) | >10,000 | 22 ± 3.6 | 182 ± 13 | >1,000 | 237 ± 52 | FDA approved |
| Ga-DOTATOC* | 68Ga-DOTA-d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr(ol) | >10,000 | 2.5 ± 0.5 | 613 ± 140 | >1,000 | 73 ± 21 | Phase 2 studies |
| Y-DOTATOC* | 90Y-DOTA-d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr(ol) | >10,000 | 11 ± 1.7 | 389 ± 135 | >10,000 | 114 ± 29 | Phase 2 studies |
| Ga-DOTATATE* | 68Ga-DOTA-d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr | >10,000 | 0.20 ± 0.04 | >1,000 | 300 ± 140 | 377 ± 18 | FDA approved |
| Y-DOTATATE* | 90Y-DOTA-d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr | >10,000 | 1.6 ± 0.4 | >1,000 | 523 ± 239 | 187 ± 50 | Unknown |
| Lu-DOTATATE† | 177Lu-DOTA-d-Phe-cyclo(Cys-Tyr-d-Trp-Lys-Thr-Cys)Thr | >1,000 | 2.0 ± 0.8 | 162 ± 16 | >1,000 | >1,000 | Phase 3 study |
| Ga-DOTANOC‡ | 68Ga-DOTA-d-Phe-cyclo(Cys-1-Nal-d-Trp-Lys-Thr-Cys)Thr(ol) | >10,000 | 1.9 ± 0.4 | 40.0 ± 5.8 | 260 ± 74 | 7.2 ± 1.6 | Phase 2 studies |
| Antagonist | |||||||
| In-DOTA-BASS§ | 111In-DOTA-p-NO2-Phe-cyclo(d-Cys-Tyr-d-Trp-Lys-Thr-Cys)d-Tyr-NH2 | >1,000 | 9.4 ± 0.4 | >1,000 | 380 ± 57 | >1,000 | Pilot study |
| In-DOTA-JR11|| | 111In-DOTA-Cpa-cyclo[d-Cys-Aph(Hor)-d-Aph(Cbm)-Lys-Thr-Cys]-d-Tyr-NH2 | >1,000 | 3.8 ± 0.7 | >1,000 | >1,000 | >1,000 | Pilot study |
| Ga-DOTA-JR11|| (Ga-OPS201) | 68Ga-DOTA-Cpa-cyclo[d-Cys-Aph(Hor)-d-Aph(Cbm)-Lys-Thr-Cys]-d-Tyr-NH2 | >1,000 | 29 ± 2.7 | >1,000 | >1,000 | >1,000 | Pilot study |
| Ga-NODAGA-JR11|| (Ga-OPS202) | 68Ga-NODAGA-Cpa-cyclo[d-Cys-Aph(Hor)-d-Aph(Cbm)-Lys-Thr-Cys]-d-Tyr-NH2 | >1,000 | 1.2 ± 0.2 | >1,000 | >1,000 | >1,000 | Phase 1/2 study |
| Lu-DOTA-JR11|| (Lu-OPS201) | 177Lu-DOTA-Cpa-cyclo[d-Cys-Aph(Hor)-d-Aph(Cbm)-Lys-Thr-Cys]-d-Tyr-NH2 | >1,000 | 0.73 ± 0.15 | >1,000 | >1,000 | >1,000 | Pilot study |
↵* Data are from Reubi et al. (12).
↵† Data are from Schottelius et al. (23) (different laboratory).
↵‡ Data are from Antunes et al. (24).
↵§ Data are from Ginj et al. (6).
↵|| Data are from Fani et al. (15).
FDA = Food and Drug Administration; 1-Nal = 1-naphthylalanine; Cpa = 4-Cl-phenylalanine; Aph(Hor) = 4-amino-l-hydroorotylphenylalanine; d-Aph(Cbm) = d-4-aminocarbamoylphenylalanine.
All data are mean ± SD, excepting Lu-DOTATATE data, which are mean ± SD (laboratory that generated Lu-DOTATATE data was different from laboratory that generated rest of data).