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Upregulation of the human epidermal growth factor receptor type 3 (HER3) is a common mechanism to bypass HER-targeted cancer therapy. Affibody-based molecular imaging has the potential for detecting and monitoring HER3 expression during treatment. In this study, we compared the imaging properties of newly generated  68 Ga-labeled anti-HER3 affibody molecules (HE) 3 -Z HER3 -DOTA and (HE) 3 -Z HER3 -DOTAGA with previously reported [ 68 Ga]Ga-(HE) 3 -Z HER3 -NODAGA. We hypothesized that increasing the negative charge of the gallium-68/chelator complex would reduce hepatic uptake, which could lead to improved contrast of anti-HER3 affibody-based PET-imaging of HER3 expression. (HE) 3 -Z HER3 -X (X = DOTA, DOTAGA) were produced and labeled with gallium-68. Binding of the new conjugates was specific in HER3 expressing BxPC-3 and DU145 human cancer cells. Biodistribution and  in vivo  specificity was studied in BxPC-3 xenograft bearing Balb/c nu/nu mice 3 h pi. DOTA- and DOTAGA-containing conjugates had significantly higher concentration in blood than [ 68 Ga]Ga-(HE) 3 -Z HER3 -NODAGA. Presence of the negatively charged  68 Ga-DOTAGA complex reduced the unspecific hepatic uptake, but did not improve overall biodistribution of the conjugate. [ 68 Ga]Ga-(HE) 3 -Z HER3 -DOTAGA and [ 68 Ga]Ga-(HE) 3 -Z HER3 -NODAGA had similar tumor-to-liver ratios, but [ 68 Ga]Ga-(HE) 3 -Z HER3 -NODAGA had the highest tumor uptake and tumor-to-blood ratio among the tested conjugates. In conclusion, [ 68 Ga]Ga-(HE) 3 -Z HER3 -NODAGA remains the favorable variant for PET imaging of HER3 expression.

scientific reports

Increase in negative charge of 68Ga/chelator complex reduces unspecific hepatic uptake but does not improve imaging properties of HER3-targeting affibody molecules