Mark Lubberink, Talakad G Lohith, Zoltan Derdak, Paul Wilkens, Emilia Palmér, Alexandra Ramolli, Mélodie Ferrat, Thuy A Tran, Bogdan Mitran, Ayman Abouyzayed, Lars Johansson, Haakan Wennbo, Fredrik Rorsman, Johan Vessby, Olof Eriksson
[68Ga]Ga-ATH001 demonstrates a dosimetry and safety profile that supports further clinical development as a repeatable, non-invasive PET marker of active fibrosis in tissue.
PURPOSE: [68Ga]Ga-ATH001 is an Affibody molecule targeting PDGFRβ in development as a Positron Emission Tomography (PET) tracer for non-invasive imaging of active fibrosis. Here we present first-in-human [68Ga]Ga-ATH001 biodistribution and radiation dosimetry data.
METHODS: Radiation dosimetry of [68Ga]Ga-ATH001 was evaluated in healthy participants (n = 3) and participants with metabolic dysfunction-associated steatohepatitis (MASH) (n = 3). Each participant was intravenously administered ~ 2.5 MBq/kg [68Ga]Ga-ATH001 and imaged by whole-body PET for up to 3 h post-injection. Absorbed dose coefficients and effective doses according to ICRP 103 were calculated using IDAC DOSE 2.1.
RESULTS: The effective dose of [68Ga]Ga-ATH001 was 0.028 ± 0.002 mSv/MBq with kidneys as the dose-limiting organ. Administration of a target dose of 2 MBq/kg would result in a sex-averaged effective dose of 4.1 mSv. Subjects tolerated the tracer administration well.
CONCLUSION: [68Ga]Ga-ATH001 demonstrates a dosimetry and safety profile that supports further clinical development as a repeatable, non-invasive PET marker of active fibrosis in tissue.