Study and synthesis of PSMA with therapuetical radionuclides
Studium a příprava PSMA s terapeutickými radionuklidy
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České vysoké učení technické v Praze
Czech Technical University in Prague
Czech Technical University in Prague
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V úvodnej časti bakalárskej práce bola vykonaná literárna rešerš, v ktorej bola popísaná problematika PSMA, cielenej rádionuklidovej terapie, chemické vlastnosti rádionuklidov 177Lu, 225Ac a 161Tb, ich využitia pre terapeutické účely karcinómu prostaty a metodiky značenia. Experimentálna časť zahŕňala prípravu rádiofarmák [161Tb]Tb- PSMA-617 a [68Ga]Ga-PSMA-11 metódou nepriameho značenia molekuly PSMA- 617, resp. PSMA-11 rádionuklidom 161Tb, resp. 68Ga cez chelátotvorné činidlá. Rádionuklid 68Ga bol zvolený ako modelový s výhodou jeho krátkeho polčasu premeny a zároveň jeho možnej elúcie z 68Ge/68Ga generátoru. V prípade rádiofarmaka [161Tb]Tb- PSMA-617 bolo cieľom nájsť optimálne podmienky značenia, teda vhodný pomer ligandu a kovu; pH a reakčnú dobu. Značenie bolo vykonané v rozmedzí pH 3-6. U pripravených rádiofarmák bola overená rádiochemická čistota pomocou metód TLC a HPLC. Výťažky značenia pre [161Tb]Tb-PSMA-617, pripraveného za optimálnych podmienok, a [68Ga]Ga-PSMA-11 mali hodnotu >99 %, teda značenie bolo efektívne.
In the introductory part of the bachelor's thesis, a literature search was carried out, in which the issue of PSMA, targeted radionuclide therapy, chemical properties of radionuclides 177Lu, 225Ac and 161Tb, their use for the therapeutic purposes of prostate cancer and labeling methodology were described. The experimental part included the preparation of radiopharmaceuticals [161Tb]Tb-PSMA-617 and [68Ga]Ga-PSMA-11 by the method of indirect labeling of the PSMA-617, resp. PSMA-11 molecule with radionuclide 161Tb, resp. 68Ga through chelating agents. The radionuclide 68Ga was chosen based on its short half-life and at the same time its possible elution from the 68Ge/68Ga generator. In the case of the radiopharmaceutical [161Tb]Tb-PSMA-617, the goal was to find optimal labeling conditions, i.e. a suitable ratio of ligand and metal; pH and reaction time. Labeling was performed in the pH range 3-6. The radiochemical purity of the prepared radiopharmaceuticals was verified using TLC and HPLC methods. Labeling yields for [161Tb]Tb-PSMA-617, prepared under optimal conditions, and [68Ga]Ga-PSMA-11 were >99 %, thus radiolabeling was efficient.
In the introductory part of the bachelor's thesis, a literature search was carried out, in which the issue of PSMA, targeted radionuclide therapy, chemical properties of radionuclides 177Lu, 225Ac and 161Tb, their use for the therapeutic purposes of prostate cancer and labeling methodology were described. The experimental part included the preparation of radiopharmaceuticals [161Tb]Tb-PSMA-617 and [68Ga]Ga-PSMA-11 by the method of indirect labeling of the PSMA-617, resp. PSMA-11 molecule with radionuclide 161Tb, resp. 68Ga through chelating agents. The radionuclide 68Ga was chosen based on its short half-life and at the same time its possible elution from the 68Ge/68Ga generator. In the case of the radiopharmaceutical [161Tb]Tb-PSMA-617, the goal was to find optimal labeling conditions, i.e. a suitable ratio of ligand and metal; pH and reaction time. Labeling was performed in the pH range 3-6. The radiochemical purity of the prepared radiopharmaceuticals was verified using TLC and HPLC methods. Labeling yields for [161Tb]Tb-PSMA-617, prepared under optimal conditions, and [68Ga]Ga-PSMA-11 were >99 %, thus radiolabeling was efficient.
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Vysokoškolská závěrečná práce je dílo chráněné autorským zákonem. Je možné pořizovat z něj na své náklady a pro svoji osobní potřebu výpisy, opisy a rozmnoženiny. Jeho využití musí být v souladu s autorským zákonem v platném znění.
Vysokoškolská závěrečná práce je dílo chráněné autorským zákonem. Je možné pořizovat z něj na své náklady a pro svoji osobní potřebu výpisy, opisy a rozmnoženiny. Jeho využití musí být v souladu s autorským zákonem v platném znění.