18F-FPPRGD2 PET/CT: Pilot phase evaluation of breast cancer patients

Andrei Iagaru, Camila Mosci, Bin Shen, Frederick T. Chin, Erik Mittra, Melinda L. Telli, Sanjiv Sam Gambhir

Research output: Contribution to journalArticlepeer-review

43 Scopus citations


Purpose: To present data from the first prospective pilot phase trial of breast cancer participants imaged with fluorine 18 (18F)- 2-fluoropropionyl-labeled PEGylated dimeric arginine-glycine- Aspartic acid (RGD) peptide (PEG3-E[c{RGDyk}]2) (FPPRGD2), a radiopharmaceutical agent used in positron emission tomographic (PET) imaging.

Materials and Methods: The local institutional review board approved the HIPAAcompliant protocol. Written informed consent was obtained from each patient. Eight women (age range, 44-67 years; mean age, 54.3 years±8.8 [standard deviation]) with newly diagnosed or recurrent breast cancer were recruited between November 2010 and February 2011. 18F-FPPRGD2 PET/computed tomographic (CT) and 18F-fluorodeoxyglucose (FDG) PET/CT examinations were performed within 3 weeks of each other. Dynamic 18FFPPRGD2 PET and two whole-body static 18F-FPPRGD2 PET/CT scans were obtained. During this time, vital signs and electrocardiograms were recorded at regular intervals. Blood samples were obtained before the injection of 18F-FPPRGD2 and at 24 hours and 1 week after injection to evaluate for toxicity. A nonparametric version of multivariate analysis of variance was used to assess the safety outcome measures simultaneously across time points. A paired two-sample t test was performed to compare the maximum standardized uptake values (SUVmax).

Results: 18F-FPPRGD2 was well tolerated, without noticeable changes in vital signs, on electrocardiograms, or in laboratory values. A total of 30 lesions were evaluated at 18F-FDG PET/CT and 18F-FPPRGD2 PET/CT. The primary breast lesions had 18F-FPPRGD2 uptake with SUVmax of 2.4-9.4 (mean, 5.6±2.8) 60 minutes after injection, compared with 18F-FDG uptake with SUVmax of 2.8-18.6 (mean, 10.4±7.2). Metastatic lesions also showed 18FFPPRGD2 uptake, with SUVmax of 2.4-9.7 (mean, 5.0±2.3) at 60 minutes, compared with 18F-FDG uptake with SUVmax of 2.2-14.6 (mean, 6.6±4.2).

Conclusion: Data from this pilot phase study suggest that 18F-FPPRGD2 is a safe PET radiopharmaceutical agent. Evaluation of 18F-FPPRGD2 in participants with breast cancer demonstrated significant uptake in the primary lesion and in the metastases. Larger cohorts are required to confirm these preliminary findings.

Original languageEnglish (US)
Pages (from-to)549-559
Number of pages11
Issue number2
StatePublished - Nov 1 2014
Externally publishedYes

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging


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