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The clinical safety, biodistribution and internal radiation dosimetry of flutemetamol (¹⁸F) injection in healthy Japanese adult volunteers.

Senda M, Brooks DJ, Farrar G, Somer EJ, Paterson CL, Sasaki M, McParland BJ - Ann Nucl Med (2015)

Bottom Line: Flutemetamol ((18)F) injection was well tolerated.The mean effective dose was 34.9 μSv/MBq.The clinical safety of [(18)F]flutemetamol demonstrated no differences of clinical significance in the pharmacokinetics, biodistribution and internal radiation dosimetry profiles between Caucasian and Japanese adults.

View Article: PubMed Central - PubMed

Affiliation: Division of Molecular Imaging, Institute of Biomedical Research and Innovation, Kobe, Japan.

ABSTRACT

Objectives: The Phase I safety, biodistribution and internal radiation dosimetry study in adult healthy Japanese males of flutemetamol ((18)F) injection, an in vivo β-amyloid imaging agent, is reported and compared with previously obtained Caucasian data.

Methods: Whole-body PET scans of 6 healthy volunteers (age 51.8-61.7 years) were acquired approximately 4 h post-injection (administered activity 102-160 MBq). Venous blood sampling determined (18)F activity concentrations in whole blood and plasma and high-performance liquid chromatography (HPLC) established the percentages of parent [(18)F]flutemetamol and its metabolites. Voided urine activity was recorded. The decay-corrected and normalised (18)F activity of 14 source organ regions as a function of time was entered into the OLINDA/EXM software to calculate the internal radiation dosimetry and effective dose of each subject following the MIRD schema. The pharmacokinetics, biodistribution and dosimetry profiles were compared to data obtained from a cohort of healthy Caucasian adult volunteers from a previous Phase I study of [(18)F]flutemetamol.

Results: Flutemetamol ((18)F) injection was well tolerated. The highest mean initial uptakes were measured in the liver (15.2%), lungs (10.2%) and brain (6.6%). The highest mean radiation absorbed doses were received by the gallbladder wall (366 μGy/MBq), upper large intestine (138 μGy/MBq) and small intestine (121 μGy/MBq). The mean effective dose was 34.9 μSv/MBq. HPLC analysis demonstrated that at 5-min post-injection about 75% of plasma (18)F radioactivity was in the form of parent [(18)F]flutemetamol, reducing to 8 and 2% at 25 and 90 min, respectively, giving rise to less lipophilic (18)F-labelled metabolites. Comparisons with the Caucasian cohort showed no differences that could be regarded as clinically significant.

Conclusion: The clinical safety of [(18)F]flutemetamol demonstrated no differences of clinical significance in the pharmacokinetics, biodistribution and internal radiation dosimetry profiles between Caucasian and Japanese adults.

No MeSH data available.


Related in: MedlinePlus

Collapsed coronal images of a representative subject following administration of flutemetamol (18F) injection acquired at times of (left to right) 0.10, 0.55, 1.20, 2.57 and 3.94 h post-injection
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Fig1: Collapsed coronal images of a representative subject following administration of flutemetamol (18F) injection acquired at times of (left to right) 0.10, 0.55, 1.20, 2.57 and 3.94 h post-injection

Mentions: Figure 1 shows whole-body PET images of a representative subject at a number of time points following the administration of flutemetamol (18F) injection. Figure 2 shows the mean time–activity curves for liver, brain, urine and intestinal contents.Fig. 1


The clinical safety, biodistribution and internal radiation dosimetry of flutemetamol (¹⁸F) injection in healthy Japanese adult volunteers.

Senda M, Brooks DJ, Farrar G, Somer EJ, Paterson CL, Sasaki M, McParland BJ - Ann Nucl Med (2015)

Collapsed coronal images of a representative subject following administration of flutemetamol (18F) injection acquired at times of (left to right) 0.10, 0.55, 1.20, 2.57 and 3.94 h post-injection
© Copyright Policy - OpenAccess
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4526582&req=5

Fig1: Collapsed coronal images of a representative subject following administration of flutemetamol (18F) injection acquired at times of (left to right) 0.10, 0.55, 1.20, 2.57 and 3.94 h post-injection
Mentions: Figure 1 shows whole-body PET images of a representative subject at a number of time points following the administration of flutemetamol (18F) injection. Figure 2 shows the mean time–activity curves for liver, brain, urine and intestinal contents.Fig. 1

Bottom Line: Flutemetamol ((18)F) injection was well tolerated.The mean effective dose was 34.9 μSv/MBq.The clinical safety of [(18)F]flutemetamol demonstrated no differences of clinical significance in the pharmacokinetics, biodistribution and internal radiation dosimetry profiles between Caucasian and Japanese adults.

View Article: PubMed Central - PubMed

Affiliation: Division of Molecular Imaging, Institute of Biomedical Research and Innovation, Kobe, Japan.

ABSTRACT

Objectives: The Phase I safety, biodistribution and internal radiation dosimetry study in adult healthy Japanese males of flutemetamol ((18)F) injection, an in vivo β-amyloid imaging agent, is reported and compared with previously obtained Caucasian data.

Methods: Whole-body PET scans of 6 healthy volunteers (age 51.8-61.7 years) were acquired approximately 4 h post-injection (administered activity 102-160 MBq). Venous blood sampling determined (18)F activity concentrations in whole blood and plasma and high-performance liquid chromatography (HPLC) established the percentages of parent [(18)F]flutemetamol and its metabolites. Voided urine activity was recorded. The decay-corrected and normalised (18)F activity of 14 source organ regions as a function of time was entered into the OLINDA/EXM software to calculate the internal radiation dosimetry and effective dose of each subject following the MIRD schema. The pharmacokinetics, biodistribution and dosimetry profiles were compared to data obtained from a cohort of healthy Caucasian adult volunteers from a previous Phase I study of [(18)F]flutemetamol.

Results: Flutemetamol ((18)F) injection was well tolerated. The highest mean initial uptakes were measured in the liver (15.2%), lungs (10.2%) and brain (6.6%). The highest mean radiation absorbed doses were received by the gallbladder wall (366 μGy/MBq), upper large intestine (138 μGy/MBq) and small intestine (121 μGy/MBq). The mean effective dose was 34.9 μSv/MBq. HPLC analysis demonstrated that at 5-min post-injection about 75% of plasma (18)F radioactivity was in the form of parent [(18)F]flutemetamol, reducing to 8 and 2% at 25 and 90 min, respectively, giving rise to less lipophilic (18)F-labelled metabolites. Comparisons with the Caucasian cohort showed no differences that could be regarded as clinically significant.

Conclusion: The clinical safety of [(18)F]flutemetamol demonstrated no differences of clinical significance in the pharmacokinetics, biodistribution and internal radiation dosimetry profiles between Caucasian and Japanese adults.

No MeSH data available.


Related in: MedlinePlus