Radiopeptide Imaging and Therapy in the United States

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FIGURE 1.
Comparison of ¹¹¹In-octreotide image obtained at 24 h after injection with ⁶⁸Ga-DOTATOC image obtained at 1 h after injection. Subject was 35-y-old man with metastatic gastrinoma. MIP = maximum-intensity projection.

TABLE 1

Summary of Radiolabeled Peptides

Peptide	No. of amino acids	Isotope(s)	Mechanism of binding	Tumor(s)	Human studies	Approval status	Reference(s)
Pentetreotide	8	¹¹¹In	Somatostatin receptor subtype 2	Carcinoid	Yes	Approved	2–8
DOTATOC	8	⁶⁸Ga	Somatostatin receptor subtype 2	Carcinoid	Yes	Radioactive Drug Research Committee approval	20,21
DOTATATE	8	⁶⁸Ga	Somatostatin receptor subtype 2	Carcinoid	Yes	Investigational New Drug authorization
Depreotide	8	^99mTc	Somatostatin receptor subtype 2	Carcinoid	Yes	Approved but no longer available	13–16
α-MSH analog	13	¹¹¹In, ⁶⁸Ga, ⁸⁶Y, ¹⁸F	MSH receptor	Melanoma	No	Not approved	24−26
RGD	3	¹⁸F, ⁶⁴Cu, ¹²⁵I	Neoangiogenesis	Glioma, melanoma	No	Not approved	27–32
Bombesin	14	¹⁸⁸Re, ^99mTc, ⁶⁴Cu, ¹⁷⁷Lu	Gastrin-releasing peptide (GRP) receptor	Prostate, breast	Outside United States	Not approved	35–41
RGD–bombesin dimer	3 and 14	¹⁸F, ⁶⁴Cu, ⁶⁸Ga	Neoangiogenesis and GRP receptor	Breast	No	Not approved	33,34
Escherichia coli heat-stable enterotoxin	19	¹¹¹In	Guanylate cyclase C receptor	Colorectal	No	Not approved	42
Vasoactive intestinal peptide (VIP)	28	¹²³I, ⁶⁴Cu	VIP receptor	Prostate	No	Not approved	43
Pituitary adenylate cyclase–activating peptide (PACAP)	27	^99mTc, ⁶⁴Cu	PACAP receptor	Breast	No	Not approved	43