Targeted Optical Imaging Agents in Cancer: Focus on Clinical Applications

Table 1

Clinical studies of targeted imaging agents. A summary of the ongoing or completed clinical trials, as described online at Clinicaltrials.gov organized by each class of molecular probe.

NCT#	Dates	Cancer	Ligand/target	Fluorophore	Reference
Small molecule
NCT02000778	11/2013–2/2018	Ovary	EC17/Folate-α	FITC	[60, 61]
NCT02769533	09/2015–9/2020	Pituitary	OTL38/Folate-α	ICG	[62]
NCT01778933	05/2013–2/2018	Renal cell	EC17/Folate-α	FITC	[63]
NCT01778920	04/2012–5/2016	Lung	EC17/Folate-α	FITC	[64]
NCT02602119	05/2015–8/2017	Lung	OTL38/Folate-α	ICG	[65]
NCT01994369	05/2014–2/2018	Breast	EC17/Folate-α	FITC	[66]
NCT02653612	01/2016–2/2020	Lung	EC17/Folate-α	FITC	[67]
NCT02645409	12/2015–4/2018	Renal cell	OTL38/Folate-α	ICG	[68, 69]
NCT03085147	03/2015/-3/2019	Head & neck	Olaparib/poly(ADP-ribose) polymerase 1	BODIPY	[70]
NCT03333031	01/2018–2/2020	Breast	HS-196/Hsp90	FITC	[71]
Peptide
NCT02462629	06/2015–2/2016	CNS	BLZ-100/	Cy5.5	[72, 73]
NCT02496065	07/2015–2/2016	Breast	BLZ-100/	Cy5.5	[74]
NCT02464332	09/2015–5/2016	Sarcoma	BLZ-100/	Cy5.5	[75–77]
NCT02234297	10/2014–2/2016	Glioma	BLZ-100/	Cy5.5	[72, 73]
NCT02097875	12/2013–3/2015	Basal/squamous cell	BLZ-100/	Cy5.5	[75–77]
NCT03205501	02/2017–2/2018	Esophagus	EMI-137/c-Met	Cy5	[78]
NCT03360461	12/2017–7/2018	Colon	EMI-137/c-Met	Cy5	[78]
NCT02676050	02/2018–6/2018	Lung	EMI-137, NAP/c-Met	Cy5	[78]
NCT02807597	12/2017–2/2020	Breast	LS301/αVβIII integrins	Cypate	[79]
NCT01722058	02/2013–8/2013	Colon	VRPMPLQ/	Fluorescein	[80]
NCT02156557	06/2014–7/2016	Colon	KCCFPAQ/	FITC	[81]
NCT01391208	02/2011–6/2012	Esophagus	ASYNYDA/	FITC	[82]
NCT01630798	07/2012–9/2013	Esophagus	ASYNYDA/	FITC	[83]
NCT02574858	11/2015–8/2016	Esophagus	QRHKPRE/EGFR	Cy5	[84]
NCT03161418	06/2017–9/2017	Esophagus	KSPNPRF/Her2	IRDye800	[85]
NCT03148119	03/2017–3/2018	Colon	QRHKPRE/EGFR	Cy5	[84]
Affibody
NCT02901925	12/2016–3/2018	Glioma	ABY-029/EGFR	IRDye800	[86–88]
NCT03282461	10/2017–2/2018	Head & neck	ABY-029/EGFR	IRDye800	[86–88]
NCT03154411	08/2017–2/2018	Sarcoma	ABY-029/EGFR	IRDye800	[86–88]
Activatable
NCT02438358	06/2015–9/2016	Breast	LUM015/Enzymes	Cy5	[89]
NCT01626066	06/2012–8/2015	Sarcoma	LUM015/Enzymes	Cy5	[89]
NCT02584244	05/2016–3/2018	Colon, pancreas, esophagus	LUM015/Enzymes	Cy5	[89]
Lectin
NCT03070613	04/2017–3/2018	Colon	Wisteria floribunda/	Fluorescein	[90]
Antibody
NCT02497599	06/2015/-8/2018	Renal cell	Girentuximab/carbo-nic anhydrase IX	IRDye800	[91]
NCT03134846	05/2017–1/2021	Head & neck	Cetuximab/EGFR	IRDye800	[92]
NCT02736578	07/2016/-4/2017	Pancreas	Cetuximab/EGFR	IRDye800	[92]
NCT01987375	11/2015–2/2018	Head & neck	Cetuximab/EGFR	IRDye800	[92]
NCT02415881	04/2015–8/2017	Head & neck	Panitumumab/EGFR	IRDye800	[92]
NCT01372189	01/2011–7/2011	Colon	anti-EGFR mAb	AF488	[93]
NCT02048150	03/2015–9/2016	Prostate	MDX1201/PSMA	AF488	[94]
NCT02743975	09/2016–2/2017	Pancreas	Bevacizumab/VEGF-A	IRDye800	[95, 96]
NCT01972373	10/2013–1/2017	Rectum	Bevacizumab/VEGF-A	IRDye800	[95, 96]
NCT02583568	10/2015/-2/2017	Breast	Bevacizumab/VEGF-A	IRDye800	[95, 96]
NCT02129933	04/2014–1/2016	Esophagus	Bevacizumab/VEGF-A	IRDye800	[95, 96]
NCT02113202	03/2014–0/2015	Colon	Bevacizumab/VEGF-A	IRDye800	[95, 96]

: multiple targets reported including matrix metalloproteinase-2 (MMP-2), membrane type-I MMP, and a transmembrane inhibitor of metalloproteinase-2 (TIMP2), ClC-3 chloride ion channels, and other proteins; –: peptide was screened using unbiased selection and target is unknown; : disaccharides and other glycans.