Dataset Information

Biodistribution and radiation dosimetry of the carbonic anhydrase IX imaging agent [(18)?F]VM4-037 determined from PET/CT scans in healthy volunteers.

ABSTRACT: PURPOSE:[(18)?F]VM4-037 has been developed as a positron emission tomography (PET) imaging marker to detect carbonic anhydrase IX (CA-IX) overexpression and is being investigated for use as a surrogate marker for tissue hypoxia. The purpose of this study was to determine the biodistribution and estimate the radiation dose from [(18)?F]VM4-037 using whole-body PET/CT scans in healthy human volunteers. PROCEDURES:Successive whole-body PET/CT scans were performed after intravenous injection of [(18)?F]VM4-037 in four healthy humans. The radiotracer uptakes in different organs were determined from the analysis of the PET scans. Human radiation doses were estimated using OLINDA/EXM software. RESULTS:High uptake of [(18)?F]VM4-037 was observed in the liver and kidneys, with little clearance of activity during the study period, with mean standardized uptake values of ~35 in liver and ~22 in kidneys at ~1 h after injection. The estimated effective dose was 28?±?1 ?Sv/MBq and the absorbed doses for the kidneys and liver were 273?±?31 and 240?±?68 ?Gy/MBq, respectively, for the adult male phantom. Hence, the effective dose would be 10?±?0.5 mSv for the anticipated injected activity of 370 MBq, and the kidney and liver doses would be 101?±?11 and 89?±?25 mGy, respectively. CONCLUSIONS:[(18)?F]VM4-037 displayed very high uptake in the liver and kidneys with little clearance of activity during the study period, resulting in these organs receiving the highest radiation doses among all bodily organs. Though the effective dose and the organ doses are within the limits considered as safe, the enhanced uptake of [(18)?F]VM4-037 in the kidneys and liver will make the compound unsuitable for imaging overexpression of CA-IX in those two organs. However, the tracer may be suitable for imaging overexpression of CA-IX in lesions in other regions of the body such as in the lungs or head and neck region.

SUBMITTER: Doss M

PROVIDER: S-EPMC7640365 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature

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Biodistribution and radiation dosimetry of the carbonic anhydrase IX imaging agent [(18) F]VM4-037 determined from PET/CT scans in healthy volunteers.

Doss Mohan M Kolb Hartmuth C HC Walsh Joseph C JC Mocharla Vani P VP Zhu Zhihong Z Haka Michael M Alpaugh R Katherine RK Chen David Y T DY Yu Jian Q JQ

Molecular imaging and biology 20141001 5

<h4>Purpose</h4>[(18) F]VM4-037 has been developed as a positron emission tomography (PET) imaging marker to detect carbonic anhydrase IX (CA-IX) overexpression and is being investigated for use as a surrogate marker for tissue hypoxia. The purpose of this study was to determine the biodistribution and estimate the radiation dose from [(18) F]VM4-037 using whole-body PET/CT scans in healthy human volunteers.<h4>Procedures</h4>Successive whole-body PET/CT scans were performed after intravenous in ...[more]

PMID: 24696183

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Project description:UNLABELLED:(18)F-CP-18, or (18S,21S,24S,27S,30S)-27-(2-carboxyethyl)-21-(carboxymethyl)-30-((2S,3R,4R,5R,6S)-6-((2-(4-(3-F18-fluoropropyl)-1H-1,2,3-triazol-1-yl)acetamido)methyl)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxamido)-24-isopropyl-18-methyl-17,20,23,26,29-pentaoxo-4,7,10,13-tetraoxa-16,19,22,25,28-pentaazadotriacontane-1,32-dioic acid, is being evaluated as a tissue apoptosis marker for PET imaging. The purpose of this study was to determine the biodistribution and estimate the normal-organ radiation-absorbed doses and effective dose from (18)F-CP-18. METHODS:Successive whole-body PET/CT scans were obtained at approximately 7, 45, 90, 130, and 170 min after intravenous injection of (18)F-CP-18 in 7 healthy human volunteers. Blood samples and urine were collected between the PET/CT scans, and the biostability of (18)F-CP-18 was assessed using high-performance liquid chromatography. The PET scans were analyzed to determine the radiotracer uptake in different organs. OLINDA/EXM software was used to calculate human radiation doses based on the biodistribution of the tracer. RESULTS:(18)F-CP-18 was 54% intact in human blood at 135 min after injection. The tracer cleared rapidly from the blood pool with a half-life of approximately 30 min. Relatively high (18)F-CP-18 uptake was observed in the kidneys and bladder, with diffuse uptake in the liver and heart. The mean standardized uptake values (SUVs) in the bladder, kidneys, heart, and liver at around 50 min after injection were approximately 65, 6, 1.5, and 1.5, respectively. The calculated effective dose was 38 ± 4 ?Sv/MBq, with the urinary bladder wall having the highest absorbed dose at 536 ± 61 ?Gy/MBq using a 4.8-h bladder-voiding interval for the male phantom. For a 1-h voiding interval, these doses were reduced to 15 ± 2 ?Sv/MBq and 142 ± 15 ?Gy/MBq, respectively. For a typical injected activity of 555 MBq, the effective dose would be 21.1 ± 2.2 mSv for the 4.8-h interval, reduced to 8.3 ± 1.1 mSv for the 1-h interval. CONCLUSION:(18)F-CP-18 cleared rapidly through the renal system. The urinary bladder wall received the highest radiation dose and was deemed the critical organ. Both the effective dose and the bladder dose can be reduced by frequent voiding. From the radiation dosimetry perspective, the apoptosis imaging agent (18)F-CP-18 is suitable for human use.

Dataset Information

Biodistribution and radiation dosimetry of the carbonic anhydrase IX imaging agent [(18)?F]VM4-037 determined from PET/CT scans in healthy volunteers.

Publications

Biodistribution and radiation dosimetry of the carbonic anhydrase IX imaging agent [(18) F]VM4-037 determined from PET/CT scans in healthy volunteers.

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