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Introduction The compound named 4-[10-(4-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)butanamido)decyl]-11-[10-(β, d -glucopyranos-1-yl)-1-oxodecyl]-1,4,8,11-tetraazacyclotetradecane-1,8-diacetic acid is a newly synthesised molecule capable of binding in vivo to albumin to form a bioconjugate. This compound was given the name, GluCAB(glucose-chelator-albumin-binder)-maleimide-1. Radiolabelled GluCAB-maleimide-1 and subsequent bioconjugate is proposed for prospective oncological applications and works on the theoretical dual-targeting principle of tumour localization through the “enhanced permeability and retention (EPR) effect” and glucose metabolism. Methods The precursor, GluCAB-amine-2, and subsequent GluCAB-maleimide-1 was synthesised via sequential regioselective, distal N-functionalisation of a cyclam template with a tether containing a synthetically-derived β-glucoside followed by a second linker to incorporate a maleimide moiety for albumin-binding. GluCAB-amine-2 was radiolabelled with [64Cu]CuCl2 in 0.1 M NH4OAc (pH 3.5, 90 °C, 30 min), purified and converted post-labeling in 0.01 M PBS to [64Cu]Cu-GluCAB-maleimide-1. Serum stability and protein binding studies were completed according to described methods. Healthy BALB/c ice (three groups of n = 5) were injected intravenously with [64Cu]Cu-TETA, [64Cu]Cu-GluCAB-amine-2 or [64Cu]Cu-GluCAB-maleimide-1 and imaged using microPET/CT at 1, 2, 4, 8 and 24 h post-injection. Biodistribution of the compounds were determined ex vivo after 24 h using gamma counting. Results GluCAB-maleimide-1 was synthesised in five consecutive steps with an overall yield of 11%. [64Cu]Cu-GluCAB-amine-2 (97% labelling efficiency) was converted to [64Cu]Cu-GluCAB-maleimide-1 (93% conversion; 90% radiochemical purity). Biodistribution analysis indicated that the control compounds were rapidly and almost completely excreted as compared to [64Cu]Cu-GluCAB-maleimide-1 that exhibited a prolonged biological half-life (6–8 h). Both, [64Cu]Cu-GluCAB-maleimide-1 and -amine-2 were excreted through the hepatobiliary system but a higher hepatic presence of the albumin-bound compound was noted. Conclusions, advances in knowledge and implications for patient care This initial evaluation paves the way for further investigation into the tumour targeting potential of [64Cu]Cu-GluCAB-maleimide-1. An efficient targeted radioligand will allow for further development of a prospective theranostic agent for more personalized patient treatment which potentially improves overall patient prognosis, outcome and health care.

A method to produce (117m)Sn radionuclide using accelerator production route is described. A new method is proposed to separate the (117m)Sn. Specific activities and thick target yield for (116)Cd(α,3n)(117m)Sn reaction at E(α)=35MeV bombarding energy were determined. The estimated production yield of (117m)Sn was 37.5kBq/μAh for 13.16 mg/cm(2) natural cadmium-oxide target and 410 kBq/μAh for 11.07 mg/cm(2) highly enriched (95%) (116)CdO target. The method developed for separation of (117m)Sn from Cd using anion-exchange resin (Dowex -1×8, fluorine form, 400 mesh) can achieve 98% radiochemical yield of (117m)Sn with more than 99% radionuclidic purity. The estimated specific activity is 2.4 GBq/mg that can be reached with the used irradiation conditions.

The use of Auger emitters as potential radiopharmaceuticals is being increasingly investigated. One of the radionuclides of interest is 103m Rh, which can be produced from 103 Ru or 103 Pd in an in vivo generator. A potential problem, however, is the recoil of the 103m Rh out of the carrier molecule and even out of the target cell. In order to determine the likelihood of this happening in the 103 Pd/ 103m Rh, case calculations were made to prove that this does not happen. The equations were generalised for all radionuclides with an atomic mass of 10–240 as a tool for determining the recoil threshold of any β-emitting radionuclide.

The use of Auger emitters as potential radiopharmaceuticals is increasingly investigated. One such radionuclide of interest is (103m)Rh. This can be produced from (103)Ru or from (103)Pd in an in vivo generator. A potential problem with this concept is the recoil of the (103m)Rh out of the carrier molecule and even out of the target cell. In order to determine whether this would happen in the (103)Pd/(103m)Rh case calculations were done to prove that this does not happen. From theoretical considerations it seems that the (103)Pd/(103m)Rh in vivo generator system would be possible.