A Phase I Study: PET Imaging of Cancer Patients Using [18F] 4-L-Fluoroglutamine (2S,4R)

Arms (1)

1. type

   EXPERIMENTAL

   label

   [18F] 4-L-Fluoroglutamine (2S,4R)

   description

   This pilot, first in-human microdose PET trial of the positron-emitting agent \[18F\] 4-L-Fluoroglutamine (2S,4R) will be an open-label study. The \[18F\] 4-L-Fluoroglutamine (2S,4R) agent will be administered by bolus intravenous injection. In all study patients, the pharmacokinetics, metabolism, and biodistribution of \[18F\] 4-L-Fluoroglutamine (2S,4R) will be evaluated by non-invasive blood- and PET-based assays, at multiple time points (see Table 1,) during one day. Eligible patients optionally can participate in the study twice, on a separate date, receiving a second radiotracer microdose of \[18F\] 4-L-Fluoroglutamine (2S,4R), followed by non-invasive blood- and PET-based assays. At the discretion of the investigator, scan 3 can be waived.

   interventionNames

   1. Drug: [18F] 4-L-Fluoroglutamine (2S,4R)

Primary outcomes (1)

1. measure

   pharmacokinetic profiles

   timeFrame

   2 years

   description

   The trial-design follows standard guidelines on collecting pharmacokinetic (PK) data for investigational radioactive drugs.1, 29-36 Animal \[18F\] 4-L-of \[18F\] 4-L-Fluoroglutamine (2S,4R). Fluoroglutamine (2S,4R) PK data provided a basis for the trial design. Sampling time-points were chosen (1) by anticipated exponential PK; with (2) allometry-based interspecies extrapolation of time-scales.37 As data is available from the first patients, suitability of the time-points will be re-examined. Blood samples will be centrifuged and the plasma pipetted, weighed and counted to determine the plasma time activity concentration curves (% injected dose/liter), as well as for metabolite analysis of the \[18F\] 4-L-Fluoroglutamine (2S,4R) compound (by radio-HPLC or other fit-for-purpose methodology).