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Table 1 Available imaging agents for rheumatoid or experimental arthritis

From: Molecular imaging of rheumatoid arthritis: emerging markers, tools, and techniques

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]
Trial in 10 patients with inflammatory joint disease
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]
Multiple trials in patients with RA
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 [4245]
99mTc-anti-CD3 mAb T cells Trials in 7 patients with RA, 2 psoriatic arthritis patients, and 38 patients with RA [4648]
123I-IL-1Ra Inflammation Trial in 4 patients with active RA [49]
99mTc-anti-TNF-α Inflammation Multiple trials with patients with RA [2, 5052]
Phase 3 study (NCT01590966)
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]
Preclinical, rabbit antigen-induced arthritis
99mTc-/111In-octreotide Endothelium activation and macrophage recruitment (binds to somatostatin receptor) Clinical use for detection of tumors [56]
Trial in 14 patients with RA
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]
Preclinical, CIA
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) [6567]
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]
Preclinical, osteopetrosis, and osteoporosis mouse models
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]
  1. 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.