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Table 1 Examples of pretargeting methods and applications

From: Pretargeting for imaging and therapy in oncological nuclear medicine

Pretargeting agent Target antigen Chase Radioactivity vector Pretargeted radionuclides Results References
Murine antibody or ScFv-streptavidin conjugate Ep-CAM biotinylated galactosyl-human serum albumin DOTA-biotin Yttrium-90 Clinical radioimmunotherapy of lung cancer and lymphoma (Hnatowich et al. 1987; Houghton et al. 2017)
Pros: targeting efficacy, high tumour/non-tumour ratio
Cons: complexity (3 compounds), presence of endogenous biotin, toxicity (lung cancer), immunogenicity of streptavidin
Murine biotinylated antibody CEA, tenascin Avidin + streptavidin DOTA-Biotin Yttrium-90 Clinical radioimmunotherapy of brain tumours (Heskamp et al. 2017)
Pros: targeting efficacy, high tumour/non-tumour ratio
Cons: complexity (4 compounds), immunogenicity of avidin/streptavidin
Murine and chimeric bispecific antibody CEA None Indium-EDTA haptens Indium-111 Clinical immunoscintigraphy (Goldenberg 1997)
Pros: high tumour/non-tumour ratio, tumour imaging in the liver
Cons: low tumour uptake, moderate sensitivity
Murine and chimeric bispecific antibody (chemically conjugated Fab) CEA None Bivalent haptens Indium-111 Clinical immunoscintigraphy, radioimmunotherapy (Le Doussal et al. 1993; Lütje et al. 2015; McBride et al. 2009; Paganelli et al. 2001)
Iodine-131 Pros: targeting efficacy, high tumour/non-tumour ratio, evidence of therapeutic effect in the clinic
Cons: difficulties in the production of bispecific antibodies
Humanized bispecific antibody (Dock and Lock) CEA, CD20, Trop2 None Bivalent haptens Gallium-68 Clinical immunoscintigraphy, radioimmunotherapy and immuno-PET, preclinical alpha-radioimmunotherapy (Schoffelen et al. 2010; Schoffelen et al. 2013; Schoffelen et al. 2014; Sharkey et al. 2003; Sharkey et al. 2005)
Lutetium-177 Pros: high tumour/non-tumour contrast ratio in PET imaging
Bismuth-213 Cons: Insufficient tumour irradiation for lutetium-177 therapy
Murine antibody-oligonucleotide conjugate Carcinoembryonic antigen None Complementary Morpholino oligonucleotide Technetium-99 m Preclinical targeting studies (Halpern & Dillman 1987)
Pros: good tumour/non-tumour contrast ratio
Cons: preparation of antibody-oligonucleotide conjugates
Affibody-oligonucleotide conjugate HER2 None DOTA-peptide nucleic acid Indium-111 Preclinical targeting and imaging studies (Yao et al. 2004)
Pros: very good tumour/non-tumour contrast ratio
Cons: preparation of antibody-oligonucleotide conjugates
Humanized antibody-trans-cyclo-octene conjugate TAG72, GPA33, CA19.9 None or tetrazine-conjugated albumin attached to galactose or polystyrene beads DOTA-PEG7-tetrazine Indium-111, copper-64, lutetium-177, zirconium-89 Preclinical targeting; immunoscintigraphy, PET imaging and dosimetry studies (van Duijnhoven et al. 2015; van Essen et al. 2014; van Schaijk et al. 2005)
Pros: good tumour uptake and tumour/non-tumour contrast ratios, easy preparation of the reagents
Cons: need for a chase step to achieve excellent results
Diabody- or Affibody-trans-cyclo-octene conjugate TAG72, HER2 None DOTA-PEG10-tetrazine Lutetium-177 Preclinical targeting and imaging studies (Vugts et al. 2013; Yao et al. 1995)
Pros: good tumour uptake and tumour/non-tumour contrast ratios, easy preparation of the reagents, no need for a chase step
Cons: possible problem of kidney uptake for therapy