TABLE 12

Ligand-binding affinities of SRIF-based radiochemicals

	SST₁	SST₂	SST₃	SST₄	SST₅	Regulatory Status
Agonists with Predominant SST₂ Affinity
DTPA-octreotide^{^a}	>10,000	12 ± 2	376 ± 84	>1000	299 ± 50
DOTA-lanreotide^{^a}	>10,000	26 ± 3.4	771 ± 229	>10,000	73 ± 12
In-DTPA-OC^{^a}	>10,000	22 ± 3.6	182 ± 13	>1000	237 ± 52	FDA approved
DOTA-TOC^{^a}	>10,000	14 ± 2.6	880 ± 324	>1000	393 ± 84
Y-DOTA-TOC^{^a}	>10,000	11 ± 1.7	389 ± 135	>10,000	114 ± 29	Phase II studies
DOTA-OC^{^a}	>10,000	14 ± 3	27 ± 9	>1000	103 ± 39
Y-DOTA-OC^{^a}	>10,000	20 ± 2	27 ± 8	>10,000	57 ± 22
Ga-DOTA-TOC^{^a}	>10,000	2.5 ± 0.5	613 ± 140	>1000	73 ± 21	EMA approved
Ga-DOTA-OC^{^a}	>10,000	7.3 ± 1.9	120 ± 45	>1000	60 ± 14
DTPA-TATE^{^a}	>10,000	3.9 ± 1	>10,000	>1000	>1000
In-DTPA-TATE^{^a}	>10,000	1.3 ± 0.2	>10,000	433 ± 16	>1000
DOTA-TATE^{^a}	>10,000	1.5 ± 0.4	>1000	453 ± 176	547 ± 160
Y-DOTA-TATE^{^a}	>10,000	1.6 ± 0.4	>1000	523 ± 239	187 ± 50
In-DOTA-TOC^{^b}	>10,000	4.6 ± 0.2	120 ± 26	230 ± 82	130 ± 17
Ga-DOTA-TATE^{^a}	>10,000	0.2 ± 0.04	>1000	300 ± 140	377 ± 18	FDA approved
Lu-DOTATATE^{^c}	>1000	2.0 ± 0.8	162 ± 16	>1000	>1000	Phase III completed
I-Gluc-TOC^{^d}	—	2.2 ± 0.7	357 ± 22	—	64 ± 24
I-Gluc-TTE^{^d}	—	2.0 ± 0.5	>1000	—	521 ± 269
I-Gluc-S-TATE^{^d}	—	2.0 ± 0.7	398 ± 19	—	310 ± 156
I-Gal-S-TATE^{^d}	—	2.0 ± 0.8	491 ± 63	—	413 ± 167
Gluc-Lys(FP)-TATE^{^e}	>10,000	2.8 ± 0.4	>1000	437 ± 84	123 ± 8.8
Agonists with Pansomatostatin-Like Binding Profile
Ga-DOTA-NOC^{^f}	>10,000	1.9 ± 0.4	40.0 ± 5.8	260 ± 74	7.2 ± 1.6	Phase II studies
In-DOTA-NOC^{^g}	>1000	3.3 ± 0.3	26 ± 1.9	>1000	10.4 ± 1.6
In-DOTA-BOC^{^g}	>10,000	3.1 ± 0.3	12 ± 1.0	455 ± 65	6 ± 1.8
NOC-ATE^{^b}	>1000	3.6 ± 1.6	302 ± 137	260 ± 95	16.7 ± 9.9
BOC-ATE^{^b}	>1000	0.8 ± 0.4	33 ± 5.5	80 ± 20	3.6 ± 1.5
In-DOTA-NOC-ATE^{^b}	>10,000	2 ± 0.35	13 ± 4	160 ± 3.8	4.3 ± 0.5
Lu-DOTA-NOC-ATE^{^d}	—	3.6 ± 0.3	31 ± 2	—	15 ± 1
In-DOTA-BOC-ATE^{^b}	>1000	1.4 ± 0.37	5.5 ± 0.8	135 ± 32	3.9 ± 0.2
Lu-DOTA-BOC-ATE^{^d}	—	2.4 ± 0.3	11 ± 1	—	8.3 ± 0.4
KE108^{^h}	0.96 ± 0.15	0.4 ± 0.04	0.44 ± 0.06	0.6 ± 0.03	0.26 ± 0.04
KE121^{^h}	1.6 ± 0.7	0.5 ± 0.2	0.3 ± 0.1	0.4 ± 0.2	0.2 ± 0.1
Y-DOTA-K121^{^h} (Y-KE88)	2 ± 0.8	4.3 ± 0.8	0.7 ± 0.2	0.5 ± 0.2	0.7 ± 0.2
Ga-DOTA-K121^{^h} (Ga-KE88)	3.5 ± 1.6	1.8 ± 1.6	0.8 ± 0.3	1.8 ± 0.5	0.9 ± 0.2
Y-DOTAGA-KE121^{^h} (Y-KE87)	6.7 ± 2.1	2.7 ± 2.4	0.6 ± 0.1	1.6 ± 0.6	1.3 ± 0.4
Antagonists
In-DOTA-BASS^ⁱ	>1000	9.4 ± 0.4	>1000	380 ± 57	>1000	Pilot study
In-DOTA-JR11^{^j}	>1000	3.8 ± 0.7	>1000	>1000	>1000	Pilot study
Ga-DOTA-JR11^{^j} (Ga-OPS201)	>1000	29 ± 2.7	>1000	>1000	>1000	Pilot study
Ga-NODAGA-JR11^{^j} (Ga-OPS202)	>1000	1.2 ± 0.2	>1000	>1000	>1000	Phase I/II study
Lu-DOTA-JR11^{^j} (Lu-OPS201)	>1000	0.73 ± 0.15	>1000	>1000	>1000
sst₃-ODN-8^{^d}	—	>1000	6.7 ± 2.6		>1000
DOTA-sst₃-ODN-8^{^g}	>1000	>1000	5.2 ± 1.3	>1000	>1000
In-DOTA-sst₃-ODN-8^{^g}	>1000	>1000	15 ± 5.2	>1000	>1000

EMA, European Medicines Agency.
↵^a Data from Reubi et al. (2000a).
↵^b Data from Ginj et al. (2005).
↵^c Data from Schottelius et al. (2015).
↵^d Data from Cescato et al. (2006).
↵^e Data from Wester et al. (2003).
↵^f Data from Antunes et al. (2007).
↵^g Data from Ginj et al. (2006a).
↵^h Data from Ginj et al. (2008).
↵ⁱ Data from Ginj et al. (2006b).
↵^j Data from Fani et al. (2012).