99mTc-3PRGD2 SPECT/CT in Esophagus Cancer Patients
99mTc-3PRGD2 SPECT/CT in Esophagus Cancer Patients
This is an open-label single photon emission computed tomography / computed tomography
 (SPECT/CT) study to investigate the safety and diagnostic performance of
 99mTc-HYNIC-3PEG4-E[c(RGDfK)2) (99mTc-3PRGD2) in esophagus cancer patients. A single dose of
 nearly 11.1 MBq/kg body weight of 99mTc-3PRGD2 ( ≤ 20 µg 3PRGD2) will be intravenously
 injected into the patients in suspicion of esophagus cancer. Visual and semiquantitative
 method will be used to assess the whole-body planar and thoracic SPECT/CT images. Any adverse
 events will be collected from the patients.
Integrin αvβ3 is an important member of integrin receptor family and expressed preferentially
 on the activated endothelial cells of angiogenesis and some types of tumor cells, but not or
 very low on the quiescent vessel cells and other normal cells. Therefore, the integrin αvβ3
 receptor is becoming a valuable target for diagnosis and response evaluation of malignant
 tumors.

 The tri-peptide sequence of arginine-glycine-aspartic acid (RGD) can specifically bind to the
 integrin αvβ3 receptor. Accordingly, a variety of radiolabeled RGD-based peptides have been
 developed for non-invasive imaging of integrin αvβ3 expression via single photon emission
 computed tomography (SPECT)or positron emission tomography (PET). Among all the RGD
 radiotracers studied, several RGD monomers have been investigated in clinical trials, and the
 preliminary results demonstrated specific imaging of various types of tumors, and the tumor
 uptake correlated well with the level of integrin αvβ3 expression. Recently, several RGD
 dimeric peptides with PEG linkers have been studied. The new types of RGD peptides showed
 much higher in vitro integrin αvβ3-binding affinity than the single RGD tri-peptide sequence,
 and importantly, they exhibited significantly increased tumor uptake and improved in vivo
 kinetics in animal models. As a representative, 99mTc-3PRGD2 could be easily prepared and
 exhibited excellent in vivo behaviors in animal models. No adverse reactions are observed in
 animal models to date.

 For the further interests in clinical translation of 99mTc-3PRGD2, an open-label SPECT/CT
 study was designed to investigate the safety and diagnostic performance of 99mTc-3PRGD2 in
 esophagus cancer patients. A single dose of nearly 11.1 MBq/kg body weight 99mTc-3PRGD2 ( ≤
 20 µg 3PRGD2) will be intravenously injected into the esophagus cancer patients. Visual and
 semiquantitative method will be used to assess the whole-body planar and thoracic SPECT/CT
 images. Adverse events will also be observed in the patients.
Inclusion Criteria:

 -  Males and females, ≥30 years old

 -  Thoracic CT and/or gastroscopy diagnosis in suspicion of primary or recurrent lung
 cancer.

 -  The lung cancer will be histologically confirmed or results of histology will be
 available.

 Exclusion Criteria:

 -  Females planning to bear a child recently or with childbearing potential

 -  Known severe allergy or hypersensitivity to IV 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.