Radiation Dosimetry of F-AzaFol: A First In-human Use of a Folate Receptor PET Tracer

Overview

Journal EJNMMI Res

Date 2020 Apr 10

PMID 32270313

Citations 15

Authors

Silvano Gnesin

Joachim Muller

Irene A Burger

Alexander Meisel

Marco Siano

Martin Fruh

Matthias Choschzick

Cristina Muller

Roger Schibli

Simon M Ametamey

Philipp A Kaufmann

Valerie Treyer

John O Prior

Niklaus Schaefer

Affiliations

Soon will be listed here.

Abstract

Background: The folate receptor alpha (FRα) is an interesting target for imaging and therapy of different cancers. We present the first in-human radiation dosimetry and radiation safety results acquired within a prospective, multicentric trial (NCT03242993) evaluating the F-AzaFol (3'-aza-2'-[F]fluorofolic acid) as the first clinically assessed PET tracer targeting the FRα.

Material And Methods: Six eligible patients presented a histologically confirmed adenocarcinoma of the lung with measurable lesions (≥ 10 mm according to RECIST 1.1). TOF-PET images were acquired at 3, 11, 18, 30, 40, 50, and 60 min after the intravenous injection of 327 MBq (range 299-399 MBq) of F-AzaFol to establish dosimetry. Organ absorbed doses (AD), tumor AD, and patient effective doses (E) were assessed using the OLINDA/EXM v.2.0 software and compared with pre-clinical results.

Results: No serious related adverse events were observed. The highest AD were in the liver, the kidneys, the urinary bladder, and the spleen (51.9, 45.8, 39.1, and 35.4 μGy/MBq, respectively). Estimated patient and gender-averaged E were 18.0 ± 2.6 and 19.7 ± 1.4 μSv/MBq, respectively. E in-human exceeded the value of 14.0 μSv/MBq extrapolated from pre-clinical data. Average tumor AD was 34.8 μGy/MBq (range 13.6-60.5 μGy/MBq).

Conclusions: F-Azafol is a PET agent with favorable dosimetric properties and a reasonable radiation dose burden for patients which merits further evaluation to assess its performance.

Trial Registration: ClinicalTrial.gov, NCT03242993, posted on August 8, 2017.

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