68Ga-BNOTA-PRGD2 PET/CT in Patients With Rheumatoid Arthritis

Diagnostic Performance and Evaluation Efficacy of 68Ga-BNOTA-PRGD2 PET/CT in Patients With Rheumatoid Arthritis

This is an open-label positron emission tomography/computed tomography ( PET/CT) study to investigate the diagnostic performance and evaluation efficacy of 68Ga-BNOTA-PRGD2 in rheumatoid arthritis (RA) patients. A single dose of nearly 111 MBq 68Ga-BNOTA-PRGD2 (≤ 40 µg BNOTA-PRGD2) will be intravenously injected into patients with RA. Visual and semiquantitative method will be used to assess the PET/CT images. Whole body 18F-FDG PET/CT will be performed for comparison.

The Alpha(v)beta3 integrin, one of the most prominent members of integrin superfamily, is trans-membrane heterodimeric proteins which mediate cell-cell and cell-extracellular matrix adhesion. Integrin alpha(v)beta3 receptor plays an pivotal role in promoting, sustaining and regulating the angiogenesis and was identified as a marker of angiogenic vascular tissue. Cyclic arginine-glycine-aspartic acid (RGD) peptides was identified as a key integrin recognition motif which could strongly bind to integrin alpha(v)beta3 and inhibit new blood vessel formation. Animal study in antigen induced arthritis demonstrated that intra-articular administration of a cyclic RGD antagonist of alpha(v)beta3 leading to inhibition of cell infiltrate, synovial angiogenesis, pannus formation, cartilage erosions and even diminishing arthritis severity. For these properties, RGD peptide-based multimodality molecular probes have been developed for noninvasive imaging by targeting integrin alpha(v)beta3. And compared with 18F-FDG PET/CT, radiolabeled RGD imaging is a promising approach to visualize angiogenesis and provide a therapeutic target for anti-angiogenetic and anti-integrin therapy.

For the further interests in clinical translation of 68Ga-BNOTA-PRGD2, an open-label PET/CT study was designed to investigate the diagnostic performance and evaluation efficacy of 68Ga-BNOTA-PRGD2 in RA patients.

Inclusion Criteria:

• Patients fulfilled the 1987 revised criteria of the American College of Rheumatology (ACR) for RA;
• Males and females, ≥18 years old

Exclusion Criteria:

• Concurrent medical conditions of other autoimmune diseases
• Latent or active joint infection or joint injury
• Renal dysfunction (serum level of creatinine more than 1.2 mg/dL)
• Females planning to bear a child recently or with childbearing potential
• Known severe allergy or hypersensitivity to intravenous radiographic contrast
• Inability to lie still for the entire imaging time because of cough, pain, etc
• Inability to complete the needed examinations due to severe claustrophobia, radiation phobia, etc
• Concurrent severe and/or uncontrolled and/or unstable other medical disease that, in the opinion of the investigator, may significantly interfere with study compliance