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Substance P (SP) is a small peptide commonly known as a preferential endogenous ligand for the transmembrane neurokinin-1 receptor. Nuclear Medicine procedures currently involve radiolabeled SP derivatives in peptide radioligand endotherapy of inoperable glioblastoma. Promising clinical results sparked the demand for facile production strategies for a functionalized 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-[Thi 8 , Met(O 2 ) 11 ]-SP to allow for rapid Gallium-68 or Bismuth-213 complexation. Therefore, we provide a simple kit-like radiotracer preparation method that caters for the gallium-68 activity eluted from a SnO 2 generator matrix as well as preliminary results on the adaptability to produce [ 213 Bi]Bi-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP from the same vials containing the same starting material. Following a phase of radioanalysis for complexation of gallium-68 to DOTA-[Thi 8 , Met(O 2 ) 11 ]SP and assessing the radiolabeling parameters, the vials containing appropriate kit-prototype material were produced in freeze-dried batches. The facile radiolabeling performance was tested and parameters for future human application were calculated to meet the criteria for theranostic loco-regional co-administration of activity doses comprising [ 68 Ga]Ga-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP mixed with [ 213 Bi]Bi-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP. [ 68 Ga]Ga-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP was prepared quantitatively from lyophilized starting material within 25 min providing the required molar activity (18 ± 4 GBq/µmol) and activity concentration (98 ± 24 MBq/mL), radiochemical purity (&gt;95%) and sustained radiolabeling performance (4 months at &gt;95% LE) as well as acceptable product quality (&gt;95% for 120 min). Additionally, vials of the same starting materials were successfully adapted to a labeling strategy available for preparation of [ 213 Bi]Bi-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP providing sufficient activity for 1-2 human doses. The resultant formulation of [ 68 Ga]Ga-/[ 213 Bi]Bi-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP activity doses was considered of adequate radiochemical quality for administration. This investigation proposes a simple kit-like formulation of DOTA-[Thi 8 , Met(O 2 ) 11 ]SP-a first-line investigation into a user friendly, straightforward tracer preparation that would warrant efficient clinical investigations in the future. Quantitative radiolabeling was accomplished for [ 68 Ga]Ga-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP and [ 213 Bi]Bi-DOTA-[Thi 8 , Met(O 2 ) 11 ]SP preparations; a key requirement when addressing the specific route of catheter-assisted co-injection directly into the intratumoral cavities.

pharmaceutics

Towards Facile Radiolabeling and Preparation of Gallium-68-/Bismuth-213-DOTA-[Thi8, Met(O2)11]-Substance P for Future Clinical Application: First Experiences