Cristin-resultat-ID: 1893941
Sist endret: 26. februar 2021, 10:00

Synthesis and evaluation of radiopharmaceuticals for targeted radionuclide therapy

  • Karoline Hartvig



Kjemisk Institutt, Universitetet i Oslo

Om resultatet

Publiseringsår: 2020


Fagfelt (NPI)

Fagfelt: Kjemi
- Fagområde: Realfag og teknologi

Beskrivelse Beskrivelse


Synthesis and evaluation of radiopharmaceuticals for targeted radionuclide therapy


Nowadays, radionuclides play an important role in oncology, especially in the developing field of targeted radionuclide therapy (TRT). In this master thesis, the focus is to evaluate different radiolabeled targeting molecules for human epidermal growth factor receptor 2 (HER2) positive breast cancer and metastatic castration-resistant prostate cancer (mCRPC). The chosen targeting molecules are Herceptin® (trastuzumab) and PSMA-617, which will specifically target HER2- and PSMA-receptors, respectively. The HER2- and PSMA-receptors are excellent targets for use in targeted radionuclide therapy and should be explored further to achieve better and more efficient treatments than current treatments and for obtaining more personalized treatment regimens for patients. The β-emitter lutetium-177 (177Lu) has been thoroughly investigated with both trastuzumab and PSMA-617, but the use of the α-emitter actinium-225 (225Ac) is less studied with these targeting molecules. Although the 225Ac-PSMA-617 has been tested in patients, there is still a need for more knowledge about actinium-225, and a deeper understanding of the use of 225Ac in PSMA-617 and trastuzumab with regard to radiolabeling conditions, stability and their effects on cancer cells. This work has resulted in a successful synthesis of 225Ac-DOTA-trastuzumab, 225Ac-PSMA-617, [177Lu]Lu-DOTA-trastuzumab and [177Lu]Lu-PSMA-617 with high radiochemical yields (> 90 %). A new radiolabeling routine was obtained for 225Ac-PSMA-617 giving a yield of 98 % with good reproducibility. Furthermore, the stability of each radiolabeled conjugate has been thoroughly investigated and showed that all radiolabeled conjugates had a shelf-life of five days in the temperature range of 5-37 °C, except for 225Ac-DOTA-trastuzumab which only showed high stability over two days. Moreover, radiolysis effects were not observed for 225Ac-PSMA-617 samples with specific activities up to 216 kBq/µg, showing high stabilities over two weeks with approximately 90 % radiochemical purity. For 225Ac-DOTA-trastuzumab, only the samples with the lowest specific activities (


Karoline Hartvig

  • Tilknyttet:
    ved Kjemisk institutt ved Universitetet i Oslo

Patrick Johannes Riss

Bidragsyterens navn vises på dette resultatet som Patrick Riss
  • Tilknyttet:
    ved Organisk kjemi ved Universitetet i Oslo

Olaug Hjelstuen

  • Tilknyttet:
    ved Institutt for energiteknikk

Ellen Mengshoel Brevik

  • Tilknyttet:
    ved Radiofarmasøytisk FoU ved Institutt for energiteknikk
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