TABLE 1

Peptide Receptors, Disease Indications, and Radiopeptide Probes in Clinical Trials in Europe

Peptide	Receptor	Disease indication	Radiopeptide probe
Somatostatin	sst2	NETs; gastroenteropancreatic NETs	¹¹¹In-DTPA-octreotide^*
			¹¹¹In-DOTA-landeotide
			¹¹¹In-/⁹⁰Y-/¹⁷⁷Lu-/⁶⁸Ga-DOTATOC
			¹⁷⁷Lu-/⁶⁸Ga-DOTATATE
			¹¹¹In-DOTA-BASS^†
			^99mTc-HYNIC-TOC/-TATE
			^99mTc-N₄-TATE
			^99mTc-depreotide
			¹⁸F-deoxyfructosyl-TATE
	sst2/sst3/sst5		⁶⁸Ga-DOTANOC
Bombesin	GRP receptor	Prostate cancer, breast cancer	^99mTc-RP527
		Gastrointestinal stromal tumor	⁶⁸Ga-BZH3
			⁶⁴Cu-CBC-AR06
			⁶⁸Ga-/¹⁷⁷Lu-AMBA
Cholecystokinin/gastrin	Cholecystokinin 2	Medullary thyroid cancer	¹¹¹In-DTPA-d-Glu-minigastrin
			^99mTc-demogastrin 2
RGD peptides	α_vβ₃ integrin	Various	¹⁸F-galacto-RGD
			¹⁸F-RGD-K5
			¹⁸F-AH111585
Substance P	Neurokinin 1	Glioblastoma	²¹³Bi-DOTA-substance P
			¹¹¹In-/⁹⁰Y-DOTAGA-substance P
GLP-1/exendin	GLP-1 receptor	Insulinomas	¹¹¹In-[Lys⁴⁰(Ahx-DTPA)NH₂]-exendin-4
			¹¹¹In-[Lys⁴⁰(Ahx-DOTA)NH₂]-exendin-4

↵* Approved.
↵† First radiolabeled somatostatin-based antagonist in clinic.
BASS = pNO₂-Phe-c(dCys-Tyr-dTrp-Lys-Thr-Cys)dTyrNH₂; CBC = cross-bridged cyclam (4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo[6.6.2]hexadecane); AMBA = DO3A-CH₂CO-Gly-(4-aminobenzoyl)-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH₂.