GIGA researchers have developed the 18F-FB-mini-PEG-E[c(RGDyK)](2), 18F-FPRGD2, a radiopharmaceutical targeting the integrin αvβ3, a transmembrane heterodimeric receptor regulating cell interaction with the extracellular matrix (ECM). The interaction site of integrin αvβ3 with ECM is a tripeptide sequence arginine-glycine-aspartic acid (RGD) present in a wide range of ECM molecules including fibronectin, fibrinogen, von Willebrand factor, thrombospondin, vitronectin, tenascin, osteopontin and bone sialoprotein.

They have recently reported the osteoarticular uptake of 18F-FPRGD2 in a large cohort of 61 patients primarily studied for oncologic purposes. The results were the first showing the systematic analysis 18F-FPRGD2 uptake in the musculoskeletal system. Their data clearly identified a homogeneous binding of the 18F-FPRGD2 within structures that anatomically correspond to the cartilage surrounding the femoral head of an osteoarthritic hip. They have observed similar global fixation of the tracer on the entire degenerated disc.

Highlighting the role of integrins in osteoarthritis development opens the door to osteoarthritis diagnosis using in vivo non-invasive and quantitative imaging technology.

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