Pharmacokinetic evaluation of [18F]PR04.MZ for PET/CT imaging and quantification of dopamine transporters in the human brain

Kramer, Vasko; Juri, Carlos; Riss, Patrick J.; Pruzzo, Rossana; Soza‐Ried, Cristian; Flores, Jonathan; Hurtado, Ana; Rösch, Frank; Chaná-Cuevas, Pedro; Amaral, Horacio

doi:10.1007/s00259-019-04594-z

Cited by 13 publications

(12 citation statements)

References 22 publications

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“…F]PR04.MZ showed high specific uptake in striatal and midbrain regions [13] and showed very promising results for the evaluation of the dopaminergic, nigro-striatal integrity in patients with movement disorders such as Holmes Tremor [14] PS [15]. In combination with the excellent imaging properties, the dosimetry profile of [ 18 F]PR04.MZ supports clinical applications in larger groups of patients being evaluated for movement disorders.…”

Section: Discussionmentioning

confidence: 86%

“…Since [ 18 F]PR04.MZ provides a higher selectivity for DAT [11], the contribution of SERT and NET binding to the absorbed dose for the urinary bladder wall may be lower. In addition, no polar metabolites other MZ which would be primarily cleared via the kidneys and bladder [13]. It can further be assumed that the absorbed dose to bone surface was higher in the current study because cortical and trabecular bone were explicitly used as source organs compared to other 18 F-labelled DAT PET tracers where bone was included in the remainder body [22,23].…”

Section: Discussionmentioning

confidence: 99%

“…Subjects fasted on the day of imaging until the end of the study. [ 18 F]PR04.MZ was produced under GMP-compliant conditions as previously described [ 13 ].…”

Section: Methodsmentioning

confidence: 99%

“…[ 18 F]PR04.MZ is a new, innovative PET imaging agent with an improved affinity and selectivity profile, which further allows for quantification of extra-striatal DAT, for example in the substantia nigra pars compacta [ 11 , 12 ]. The pharmacokinetic evaluation of [ 18 F]PR04.MZ showed very high specific uptake in striatal and midbrain regions, excellent imaging contrast and robust quantification outcomes [ 13 ]. Following the clinical translation, the diagnostic potential of this new tracer was highlighted by the excellent imaging properties in a case study of Holmes Tremor [ 14 ] and the clinical validation for detection of nigro-striatal degeneration in patients under evaluation for movement disorders [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

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Whole-body biodistribution and radiation dosimetry of [18F]PR04.MZ: a new PET radiotracer for clinical management of patients with movement disorders

Lehnert

Riss

Mendoza³

et al. 2022

EJNMMI Res

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Purpose [18F]PR04.MZ is a new PET imaging agent for dopamine transporters, providing excellent image quality and allowing for the evaluation of patients with movement disorders such as Parkinson’s disease. The objective of this study was to evaluate the biodistribution and radiation dosimetry of [18F]PR04.MZ by serial PET imaging. Methods Six healthy subjects (n = 3 males, n = 3 females) were enrolled in this study. A series of 14 whole-body PET/CT scans were acquired until 5.5 h post-injection of 200 ± 11 MBq of [18F]PR04.MZ. After rigid co-registration, volumes of interest were outlined either on CT or PET images. Time-integrated activity coefficients were calculated for selected source organs. Organ absorbed doses, and the effective dose were calculated using IDAC-Dose 2.1. Results Physiological uptake of [18F]PR04.MZ was mainly observed in the striatum, brain, liver, gall bladder, intestine, red marrow and cortical bone. [18F]PR04.MZ was primarily excreted via hepatobiliary clearance and, to a lower extent, via renal clearance. The normalized absorbed doses were highest in gall bladder wall (32.2 ± 6.4 µGy/MBq), urinary bladder wall (27.2 ± 4.5 µGy/MBq), red marrow (26.5 ± 1.4 µGy/MBq), cortical bone surface (26.3 ± 2.5 µGy/MBq), liver (22.5 ± 1.8 µGy/MBq) and kidneys (21.8 ± 1.1 µGy/MBq). The effective dose according to ICRP 60 and 103 was 16.3 ± 1.1 and 16.6 ± 1.5 µSv/MBq, respectively. Conclusion [18F]PR04.MZ has a favourable dosimetry profile, comparable to those of other 18F-labelled PET tracers, and is suitable for larger clinical applications. Trial registration CEC SSM Oriente, Santiago, Chile, permit 20140520.

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Section: Discussionmentioning

confidence: 86%

Section: Discussionmentioning

confidence: 99%

“…Subjects fasted on the day of imaging until the end of the study. [ 18 F]PR04.MZ was produced under GMP-compliant conditions as previously described [ 13 ].…”

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Whole-body biodistribution and radiation dosimetry of [18F]PR04.MZ: a new PET radiotracer for clinical management of patients with movement disorders

Lehnert

Riss

Mendoza³

et al. 2022

EJNMMI Res

Self Cite

View full text Add to dashboard Cite

show abstract

“…This might be the reason why studies with [ 99m Tc]Tc-TRODAT-1 are mostly performed in Asia and South America (Ferraz, 2014;Hossein-Tehrani et al, 2020;Hwang et al, 2004;Sasannezhad et al, 2017;Sood et al, 2021). (Appel et al, 2015), 40-50 min for [ 18 F]PR04.MZ (Juri et al, 2021;Kramer, Juri, et al, 2020), >80 min for [ 11 C]RTI-32 (Guttman et al, 1997), and 3-4 h for [ 18 F]CFT (Laakso et al, 1998).…”

Section: Dopamine Transporter Activitymentioning

confidence: 99%