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Radiation Dosimetry, Plasma Pharmacokinetics, Biodistribution, Safety and Diagnostic Performance of 68Ga-BNOTA-PRGD2 in Healthy Volunteers and Lung Cancer Patients

Phase 0
30 Years
Open (Enrolling)
Lung Cancer

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Trial Information

Radiation Dosimetry, Plasma Pharmacokinetics, Biodistribution, Safety and Diagnostic Performance of 68Ga-BNOTA-PRGD2 in Healthy Volunteers and Lung Cancer Patients

Integrin αⅤβ3 is an important member of this receptor family and expressed preferentially on
various types of tumor cells and the activated endothelial cells of tumor angiogenesis, 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 positron emission
tomography (PET) or single photon emission computed tomography (SPECT). Among all the RGD
radiotracers studied, two PET imaging agents, 18F-Galacto-RGD and 18F-AH111585, have been
investigated in clinical trials, and the results demonstrated that both radiotracers allowed
the specific imaging of various types of tumors, and the tumor uptake correlated well with
the expression of integrin αⅤβ3. Recently, series of 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, 68Ga-BNOTA-PRGD2 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 68Ga-BNOTA-PRGD2, a open-label dynamic
whole-body PET/CT study was designed to investigate radiation dosimetry, plasma
pharmacokinetics, biodistribution, safety and diagnostic performance of 68Ga-BNOTA-PRGD2 in
healthy volunteers and lung cancer patients. A single dose of nearly 111 MBq
68Ga-BNOTA-PRGD2 ( ≤ 40 µg BNOTA-PRGD2) will be intravenously injected into healthy
volunteers and lung cancer patients. Visual and semiquantitative method will be used to
assess the PET/CT images. Changes of blood pressure, pulse, respiration, temperature,
routine blood and urine tests, serum alanine aminotransferase, albumin, and creatinine, and
any adverse events will be collected from the volunteers. Adverse events will also be
observed in the patients.

Inclusion Criteria:

- Healthy volunteers:

- Males and females, ≥30 and ≤ 70 years old

- Cancer patients:

- Males and females, ≥30 years old

- CT and/or 18F-FDG PET/CT diagnosis in suspicion of primary or recurrent lung

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

Exclusion Criteria:

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

- Renal function: serum creatinine >3.0 mg/dL (270 μM/L)

- Liver function: any hepatic enzyme level more than 5 times upper limit of normal.

- Known severe allergy or hypersensitivity to IV radiographic contrast.

- Patients not able to enter the bore of the PET/CT scanner.

- 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.

Type of Study:


Study Design:

Endpoint Classification: Safety/Efficacy Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Diagnostic

Outcome Measure:

Visual and semiquantitative assessment of lesions and biodistribution

Outcome Description:

Visual analysis will be performed by consensus reading by at least 3 experienced nuclear medicine physician. The semiquantitative analysis will be performed by the same person for all the cases, and the standardized uptake values (SUVs) of tumor and organs will be measured.

Outcome Time Frame:

One year

Safety Issue:


Principal Investigator

Fang Li, MD

Investigator Role:

Study Chair

Investigator Affiliation:

Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Science


China: National Natural Science Foundation

Study ID:




Start Date:

December 2011

Completion Date:

March 2014

Related Keywords:

  • Lung Cancer
  • lung cancer
  • integrin receptor
  • 68Ga-BNOTA-PRGD2
  • PET/CT
  • efficacy and safety
  • Lung Neoplasms