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. 2019 Sep 1;11(9):443. doi: 10.3390/pharmaceutics11090443

Table 5.

Structure and potential application of NK1R therapeutic radioligands based on SP and its analogues or derivatives.

NK1R Radioligand Molecules Biological Properties and Potential Applications Reference
[177Lu]Lu-DOTA-SP • Animal tests: biodistribution studies on mice bearing AR42J pancreatic tumour, high uptake in kidneys, satisfactory uptake in tumour, significant uptake in intestine and stomach;
• In vitro study: high specific uptake and internalisation using LN319 cells isolated directly from the tumours;		 [133]
[177Lu]Lu-DOTAGA-SP
[90Y]Y-DOTAGA-SP
[213Bi]Bi-DOTAGA-SP		 Medical experiments: well tolerated therapy of critically located gliomas, low toxicity; [134]
[90Y]Y-DOTAGA-SP Medical experiments: recorded completed encapsulation of the tumour in patients administered with the highest dose; [135]
[213Bi]Bi-DOTA-[Thi8,Met(O2)11]SP [111In]In-DOTA-[Thi8,Met(O2)11]SP Medical experiments: treatment of critically located gliomas; well tolerated and safe for patients; complete necrosis of small tumours and necrosis only in the nearness of the implanted catheters in the case of large tumours; [55]
[213Bi]Bi-DOTA-[Thi8,Met(O2)11]SP [68Ga]Ga-DOTA-[Thi8,Met(O2)11]SP Medical experiments: treatment of patients with secondary GBM (after surgery, chemo- and radiotherapy); very low accumulation in kidneys, urine, bladder and blood; no side effects, necrosis and demarcation of the tumours; [127]
[213Bi]Bi-DOTA-[Thi8,Met(O2)11]SP Medical experiments: higher efficiency of radiolabelled NK1R ligands application and local brain tumours treatment in patients suffering from secondary GBM compared to standard treatment options; [136]
[225Ac]Ac-DOTA-[Thi8,Met(O2)11]SP • In vitro study: high affinity to glioblastoma cancer cells: T98G, U87MG, U138MG and glioblastoma stem cells (GSC); significant reduction in glioblastoma cell viability in comparison to the conventional treatment with temozolomide; high cytotoxicity towards GBM stem cells; [139]
• Medical experiments: safe and well-tolerated therapy without side effects; [144]
[177Lu]Lu-DOTA-SP(4–11) [177Lu]Lu-DOTA-SP(5–11) [177Lu]Lu-DOTA-[Thi8,Met(O2)11]SP(5–11) In vitro study: radiobioconjugates characterized with higher lipophilicity and lower molecular weight than those based on analogue [Thi8,Met(O2)11]SP—changes in physicochemical properties of radiobioconjugates leading to their deeper diffusion into the cavity walls after surgical resection of the tumour. [145]