TABLE 1.

Excerpts of Human Studies of Pretargeted Nuclear Medicine Using Streptavidin–Biotin System

Antibody radioligand pair and pretargeting timeline	Radioligand dose	Target antigen and study population	Main findings	Reference
Hour 0: Biotinylated antitenascin mAb BC4 Hour 36: (strept)avidin CA Hour 54–60: 90Y-DOTA-biotin	2.22–2.96 GBq/m2	Tenascin and high-grade glioma patients	Reduction in tumor in 25% patients, all patients developed immune response.	(8)
Hour 0: SA-conjugated C2B8 mAb Hour 34: biotin CA Hour 52: 111In/90Y-DOTA-biotin	3–5 mCi (111In), 30–50 mCi/m2 (90Y)	CD20 and non-Hodgkin lymphoma patients	Good tumor–to–whole-body ratios (38:1), mild hematologic toxicity, 28% of patients with CR.	(12)
Hour 0: SA-conjugated NR-LU-10 mAb Hour 24–72: Biotin-galactose-HSA CA Hour 28–96: 111In/90Y-DOTA-biotin	185 MBq (111In), 370 MBq/m2 (90Y)	Ep-CAM and adenocarcinoma patients (majority colorectal and lung)	Good tumor-to-marrow absorbed dose ratio (63:1), all tested patients developed immune response.	(16)
Hour 0: Biotinylated antitenascin mAb BC4 Hour 24: avidin CA Hour 42: 90Y-DOTA-biotin (procedure repeated again 8–10 wk apart)	0.555–1.110 GBq	Tenascin and recurrent high-grade glioma, anaplastic astrocytoma patients	25% overall response to PRIT, no hematologic toxicity observed.	(14)
Hour 0: Biotinylated antitenascin mAb BC4 Hour 24–36: avidin CA Hour 40–54: 90Y-DOTA-biotin	2.2 GBq/m2	Tenascin and high-grade glioma patients	Significantly higher OS in treated cohort than in control.	(15)
Hour 0: SA-conjugated CC49-(scFv)4 Hour 48/72: biotin CA Hour 72/96: 111In/90Y-DOTA-biotin	185 MBq (111In), 370 MBq/m2 (90Y)	TAG-72 and metastatic colorectal cancer	Tumor–to–normal-tissue dose ratio 54.5, immune response or toxicity not reported.	(11)

CR = complete response; SA = streptavidin; OS = overall survival.