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000289902 245__ $$aHuman ABC and SLC Transporters: The Culprit Responsible for Unspecific PSMA-617 Uptake?
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000289902 520__ $$a[177Lu]Lu-PSMA-617 has recently been successfully approved by the FDA, the MHRA, Health Canada and the EMA as Pluvicto®. However, salivary gland (SG) and kidney toxicities account for its main dose-limiting side-effects, while its corresponding uptake and retention mechanisms still remain elusive. Recently, the presence of different ATP-binding cassette (ABC) transporters, such as human breast cancer resistance proteins (BCRP), multidrug resistance proteins (MDR1), multidrug-resistance-related proteins (MRP1, MRP4) and solute cassette (SLC) transporters, such as multidrug and toxin extrusion proteins (MATE1, MATE2-K), organic anion transporters (OAT1, OAT2v1, OAT3, OAT4) and peptide transporters (PEPT2), has been verified at different abundances in human SGs and kidneys. Therefore, our aim was to assess whether [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 are substrates of these ABC and SLC transporters. For in vitro studies, the novel isotopologue ([α,β-3H]Nal)Lu-PSMA-617 was used in cell lines or vesicles expressing the aforementioned human ABC and SLC transporters for inhibition and uptake studies, respectively. The corresponding probe substrates and reference inhibitors were used as controls. Our results indicate that [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 are neither inhibitors nor substrates of the examined transporters. Therefore, our results show that human ABC and SLC transporters play no central role in the uptake and retention of [177Lu]Lu-PSMA-617 and [225Ac]Ac-PSMA-617 in the SGs and kidneys nor in the observed toxicities.
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000289902 650_7 $$2Other$$aPSMA
000289902 650_7 $$2Other$$aPSMA-617
000289902 650_7 $$2Other$$aefflux transporters
000289902 650_7 $$2Other$$akidney toxicity
000289902 650_7 $$2Other$$aprostate cancer
000289902 650_7 $$2Other$$asalivary gland toxicity
000289902 650_7 $$2Other$$aside-effects
000289902 650_7 $$2Other$$atargeted alpha therapy
000289902 650_7 $$2Other$$atargeted radionuclide therapy
000289902 650_7 $$2Other$$auptake transporters
000289902 7001_ $$0P:(DE-He78)34d44e4a0656d0957d8fda31b5edb619$$aBakos, Gabor$$b1$$udkfz
000289902 7001_ $$0P:(DE-He78)033d979f00729281e709b85fe6cae972$$aBauder-Wüst, Ulrike$$b2$$udkfz
000289902 7001_ $$0P:(DE-He78)3373acf5d3b93adfd9ea973cf2d218aa$$aSchäfer, Martin$$b3$$udkfz
000289902 7001_ $$0P:(DE-He78)7391d5b7c56f3a52656bfb12636b333f$$aRemde, Yvonne$$b4$$udkfz
000289902 7001_ $$0P:(DE-He78)1a25bc9516a97a13551ebd083356d24f$$aRoscher, Mareike$$b5$$udkfz
000289902 7001_ $$0P:(DE-He78)0f034e05cefb010f991ef8b96009d95c$$aBenesova-Schäfer, Martina$$b6$$eLast author$$udkfz
000289902 773__ $$0PERI:(DE-600)2193542-7$$a10.3390/ph17040513$$gVol. 17, no. 4, p. 513 -$$n4$$p513$$tPharmaceuticals$$v17$$x1424-8247$$y2024
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