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Florbetapir f-18: a histopathologically validated Beta-amyloid positron emission tomography imaging agent.
Semin Nucl Med. 2011 Jul; 41(4):300-4.SN

Abstract

Florbetapir F-18 is a molecular imaging agent combining high affinity for β-amyloid, pharmacokinetic properties that allow positron emission tomography (PET) imaging within a convenient time after dose administration, and the wide availability of the radionuclide fluorine-18. Florbetapir F-18 is prepared by nucleophilic radiofluorination in approximately 60 minutes with a decay-corrected yield of 20%-40% and with a specific activity typically exceeding 100 Ci/mmol. The florbetapir F-18 dissociation constant (K(d)) for binding to β-amyloid in brain tissue from Alzheimer's disease (AD) patients was 3.7 ± 0.3 nmol/L, and the maximum binding capacity (B(max)) was 8800 ± 1600 fmol/mg protein. Autoradiography studies have shown that florbetapir F-18 selectively binds to β-amyloid aggregates in AD patient brain tissue, and the binding intensity is correlated with the density of β-amyloid quantified by standard neuropathologic techniques. Studies in animals revealed no safety concerns and rapid and transient normal brain uptake (6.8% injected dose/g at 2 minutes and 1.9% injected dose/g at 60 minutes in the mouse). Florbetapir F-18 has been well-tolerated in studies of more than 2000 human subjects. Biodistribution studies in humans revealed predominantly hepatobiliary excretion. The whole body effective dose was 7 mSv from a dose of 370 MBq. The pharmacokinetic of florbetapir F-18 make it possible to obtain a PET image with a brief (10 minutes) acquisition time within a convenient time window of 30-90 minutes after dose administration. Clinical studies have demonstrated a clear correlation between in vivo PET imaging with florbetapir F-18 and postmortem histopathologic quantitation of β-amyloid in the brain.

Authors+Show Affiliations

Avid Radiopharmaceuticals, Philadelphia, PA. listerjames@avidrp.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Validation Study

Language

eng

PubMed ID

21624563

Citation

Lister-James, John, et al. "Florbetapir F-18: a Histopathologically Validated Beta-amyloid Positron Emission Tomography Imaging Agent." Seminars in Nuclear Medicine, vol. 41, no. 4, 2011, pp. 300-4.
Lister-James J, Pontecorvo MJ, Clark C, et al. Florbetapir f-18: a histopathologically validated Beta-amyloid positron emission tomography imaging agent. Semin Nucl Med. 2011;41(4):300-4.
Lister-James, J., Pontecorvo, M. J., Clark, C., Joshi, A. D., Mintun, M. A., Zhang, W., Lim, N., Zhuang, Z., Golding, G., Choi, S. R., Benedum, T. E., Kennedy, P., Hefti, F., Carpenter, A. P., Kung, H. F., & Skovronsky, D. M. (2011). Florbetapir f-18: a histopathologically validated Beta-amyloid positron emission tomography imaging agent. Seminars in Nuclear Medicine, 41(4), 300-4. https://doi.org/10.1053/j.semnuclmed.2011.03.001
Lister-James J, et al. Florbetapir F-18: a Histopathologically Validated Beta-amyloid Positron Emission Tomography Imaging Agent. Semin Nucl Med. 2011;41(4):300-4. PubMed PMID: 21624563.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Florbetapir f-18: a histopathologically validated Beta-amyloid positron emission tomography imaging agent. AU - Lister-James,John, AU - Pontecorvo,Michael J, AU - Clark,Chris, AU - Joshi,Abhinay D, AU - Mintun,Mark A, AU - Zhang,Wei, AU - Lim,Nathaniel, AU - Zhuang,Zhiping, AU - Golding,Geoff, AU - Choi,Seok Rye, AU - Benedum,Tyler E, AU - Kennedy,Paul, AU - Hefti,Franz, AU - Carpenter,Alan P, AU - Kung,Hank F, AU - Skovronsky,Daniel M, PY - 2011/6/1/entrez PY - 2011/6/1/pubmed PY - 2011/9/17/medline SP - 300 EP - 4 JF - Seminars in nuclear medicine JO - Semin Nucl Med VL - 41 IS - 4 N2 - Florbetapir F-18 is a molecular imaging agent combining high affinity for β-amyloid, pharmacokinetic properties that allow positron emission tomography (PET) imaging within a convenient time after dose administration, and the wide availability of the radionuclide fluorine-18. Florbetapir F-18 is prepared by nucleophilic radiofluorination in approximately 60 minutes with a decay-corrected yield of 20%-40% and with a specific activity typically exceeding 100 Ci/mmol. The florbetapir F-18 dissociation constant (K(d)) for binding to β-amyloid in brain tissue from Alzheimer's disease (AD) patients was 3.7 ± 0.3 nmol/L, and the maximum binding capacity (B(max)) was 8800 ± 1600 fmol/mg protein. Autoradiography studies have shown that florbetapir F-18 selectively binds to β-amyloid aggregates in AD patient brain tissue, and the binding intensity is correlated with the density of β-amyloid quantified by standard neuropathologic techniques. Studies in animals revealed no safety concerns and rapid and transient normal brain uptake (6.8% injected dose/g at 2 minutes and 1.9% injected dose/g at 60 minutes in the mouse). Florbetapir F-18 has been well-tolerated in studies of more than 2000 human subjects. Biodistribution studies in humans revealed predominantly hepatobiliary excretion. The whole body effective dose was 7 mSv from a dose of 370 MBq. The pharmacokinetic of florbetapir F-18 make it possible to obtain a PET image with a brief (10 minutes) acquisition time within a convenient time window of 30-90 minutes after dose administration. Clinical studies have demonstrated a clear correlation between in vivo PET imaging with florbetapir F-18 and postmortem histopathologic quantitation of β-amyloid in the brain. SN - 1558-4623 UR - https://www.unboundmedicine.com/medline/citation/21624563/Florbetapir_f_18:_a_histopathologically_validated_Beta_amyloid_positron_emission_tomography_imaging_agent_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0001-2998(11)00035-3 DB - PRIME DP - Unbound Medicine ER -