. 2014 Apr 15;16(2):208. doi: 10.1186/ar4542

Table 1.

Available imaging agents for rheumatoid or experimental arthritis

Tracer	Target	Developmental phase	Reference
General tracers
¹⁸ F-fluoro-2-deoxy-D-glucose	Glucose metabolism, inflammation	Clinical use for detection of inflammation and cancer	[1,35]
^99mTc-diphosphonates	Alterations in bone metabolism, osteoblastic activity	Clinical use for bone scanning	[33,34]
¹¹C-choline	Cell membrane synthesis, inflammation	Clinical use for detection of prostate cancer	[36,37]
¹¹C-choline	Cell membrane synthesis, inflammation	Trial in 10 patients with inflammatory joint disease	[36,37]
⁶⁷Ga-citrate	Circulating blood plasma proteins and leukocytes, inflammation	Clinical use for detection of inflammation	[14]
^99mTc-polyclonal human immunoglobulin G	Increase in vascular permeability, hyperemia, inflammation	Multiple trials in patients with rheumatic disorders	[38,39]
^99mTc-/¹¹¹In-labeled leukocytes	Influx of leukocytes into inflamed tissue	Clinical use for infectious and inflammatory disorders	[40]
^99mTc-/¹¹¹In-labeled leukocytes	Influx of leukocytes into inflamed tissue	Multiple trials in patients with RA	[40]
^99mTc-RP128	Leukocytes (binds to receptors on neutrophils and mononuclear phagocytes)	Trial with 10 patients with RA	[41]
Radiolabeled biologicals
^99mTc-anti-CD4 mAb	T cells	Case study in 1 patient with RA, trial in 6 patients with RA	[42-45]
^99mTc-anti-CD3 mAb	T cells	Trials in 7 patients with RA, 2 psoriatic arthritis patients, and 38 patients with RA	[46-48]
¹²³I-IL-1Ra	Inflammation	Trial in 4 patients with active RA	[49]
^99mTc-anti-TNF-α	Inflammation	Multiple trials with patients with RA	[2,50-52]
^99mTc-anti-TNF-α	Inflammation	Phase 3 study (NCT01590966)	[2,50-52]
^99mTc-/¹²⁴I-anti-CD20 mAb	B cells	Trials in 6 patients with RA and 20 patients with chronic inflammatory autoimmune disease	[53,54]
Specific molecular markers
^99mTc-acetylated poly-(1,3)-D-galactoside	Mononuclear phagocyte trafficking (binds CD14 and CD11b)	Trials for tumoral, inflammatory and infectious diseases	[55]
^99mTc-acetylated poly-(1,3)-D-galactoside	Mononuclear phagocyte trafficking (binds CD14 and CD11b)	Preclinical, rabbit antigen-induced arthritis	[55]
^99mTc-/¹¹¹In-octreotide	Endothelium activation and macrophage recruitment (binds to somatostatin receptor)	Clinical use for detection of tumors	[56]
^99mTc-/¹¹¹In-octreotide		Trial in 14 patients with RA	[56]
¹¹C-(R)-PK11195	Monocytes and macrophages (binds to peripheral benzodiazepine receptors)	Trials in 11 patients with RA, 6 patients with RA, and 29 patients with arthralgia	[57,58]
¹¹¹In-E-selectin-binding peptide	Activated vascular endothelium	Preclinical, rat adjuvant arthritis	[59]
^99mTc-anti-E-selectin Fab/(Fab′)₂ fragment	Activated vascular endothelium	Trial in 26 patients with RA	[60]
NIR-anti-E-selectin Ab	Activated vascular endothelium	Preclinical, CIA, and TNF-α-induced paw edema	[61]
^99mTc-annexin V	Apoptosis (binds to phosphatidylserine)	Multiple trials in cancer patients	[62]
^99mTc-annexin V	Apoptosis (binds to phosphatidylserine)	Preclinical, CIA	[62]
Cy5.5-anti-F4/80	Macrophages	Preclinical, AIA	[63]
^99mTc-anti-IL-6R	Inflammation	Preclinical, murine arthritis model	[64]
^99mTc-folic acid (EC20)	Activated macrophages, folate receptor	Phase 2 study in patients with autoimmune disease (NCT00588393)	[65-67]
NIR2-folate	Activated macrophages, folate receptor	Mouse arthritis models	[68]
¹⁸ F-PEG-folate	Activated macrophages, folate receptor	Preclinical, methylated bovine serum albumin-induced arthritis	[69]
⁶⁴Cu-/¹⁸ F-galacto-arginine-glycine-aspartic acid	Activated macrophages, osteoclasts, endothelial cells	Clinical use, tumor angiogenesis	[70]
⁶⁴Cu-/¹⁸ F-galacto-arginine-glycine-aspartic acid	Activated macrophages, osteoclasts, endothelial cells	Preclinical, osteopetrosis, and osteoporosis mouse models	[70]
NIR-matrix metalloproteinase-specific probe	Sites of matrix degradation and inflammation	Preclinical, CIA, rat OA	[71]
^99mTc-anti-macrophage mannose receptor	Subset of macrophages	Preclinical, CIA	[72]

^99mTc, ^99mtechnetium; Ab, antibody; AIA, antigen-induced arthritis; CIA, collagen-induced arthritis; IL, interleukin; mAb, monoclonal antibody; NIR, near-infrared; OA, osteoarthritis; RA, rheumatoid arthritis; TNF-α, tumor necrosis factor-alpha.