The main goal of this study is to test two new radioactive drugs, 4-[18F]fluoro-meta-hydroxyphenethylguanidine ([18F]4F-MHPG) and 3-[18F]fluoro-para-hydroxyphenethylguanidine ([18F]3F-PHPG) in human subjects with congestive heart failure.
Evaluations of these imaging agents will include their uptake in heart, lungs and liver, their metabolic breakdown in blood, and their kinetics in the heart. Based on these studies, the better of the two drugs will be chosen for further studies in patients with heart disease. After the better compound is chosen, additional measures of its imaging properties, metabolism and pharmacokinetics will be done in subjects with heart failure.

Start Date01 Dec 2015

Sponsor / Collaborator

University of Michigan

100 Clinical Results associated with 11C-Meta-Hydroxyephedrine

100 Translational Medicine associated with 11C-Meta-Hydroxyephedrine

100 Patents (Medical) associated with 11C-Meta-Hydroxyephedrine

Literatures (Medical) associated with 11C-Meta-Hydroxyephedrine

01 Oct 2023·Journal of Nuclear Cardiology

Pharmacological and metabolic parameters of [18F]flubrobenguane in clinical imaging populations

Article

Author: Dinelle, Katie ; deKemp, Robert A ; Zelt, Jason G E ; Shlik, Jakov ; Adi, Myriam ; Mair, Braeden A ; Robinson, Simon ; Saint-Georges, Zacharie ; Beanlands, Rob S ; Mielniczuk, Lisa M ; Nekesa, Kirabo ; Rotstein, Benjamin H

BACKGROUNDCardiac sympathetic nervous system molecular imaging has demonstrated prognostic value. Compared with meta-[¹¹C]hydroxyephedrine, [¹⁸F]flubrobenguane (FBBG) facilitates reliable estimation of SNS innervation using similar analytical methods and possesses a more convenient physical half-life. The aim of this study was to evaluate pharmacokinetic and metabolic properties of FBBG in target clinical cohorts.METHODSBlood sampling was performed on 20 participants concurrent to FBBG PET imaging (healthy = NORM, non-ischemic cardiomyopathy = NICM, ischemic cardiomyopathy = ICM, post-traumatic stress disorder = PTSD). Image-derived blood time-activity curves were transformed to plasma input functions using cohort-specific corrections for plasma protein binding, plasma-to-whole blood distribution, and metabolism.RESULTSThe plasma-to-whole blood ratio was 0.78 ± 0.06 for NORM, 0.64 ± 0.06 for PTSD and 0.60 ± 0.14 for (N)ICM after 20 minutes. 22 ± 4% of FBBG was bound to plasma proteins. Metabolism of FBBG in (N)ICM was delayed, with a parent fraction of 0.71 ± 0.05 at 10 minutes post-injection compared to 0.53 ± 0.03 for PTSD/NORM. While there were variations in metabolic rate, metabolite-corrected plasma input functions were similar across all cohorts.CONCLUSIONSRapid plasma clearance of FBBG limits the impact of disease-specific corrections of the blood input function for tracer kinetic modeling.

01 Aug 2004·Endocrine ReviewsQ1 · MEDICINE

Functional Imaging of Endocrine Tumors: Role of Positron Emission Tomography

Q1 · MEDICINE

Review

Author: Goldstein, David S. ; Eisenhofer, Graeme ; Pacak, Karel

This article provides an update on functional imaging approaches for diagnostic localization of endocrine tumors, with emphasis on positron emission tomography (PET). [18F]Fluorodeoxyglucose PET scanning is now a widely accepted imaging approach in clinical oncology. Benefits include improved patient outcome facilitated by staging and monitoring of disease and better treatment planning. [18F]Fluorodeoxyglucose PET is also useful in some endocrine tumors, particularly in recurrent or metastatic thyroid cancer where the degree of accumulation of the radionuclide has prognostic value. However, this imaging approach does not take full advantage of the unique characteristics of endocrine tumors. Endocrine tumor cells take up hormone precursors, express receptors and transporters, and synthesize, store, and release hormones. These characteristics offer highly specific targets for PET. Radiopharmaceuticals developed for such approaches include 6-[18F]fluorodopamine, and [11C]hydroxyephedrine for localization of pheochromocytomas, [11C]5-hydroxytryptophan and [11C]L-dihydroxyphenylalanine for carcinoid tumors, and [11C]metomidate for adrenocortical tumors. These functional imaging approaches are not meant to supplant conventional imaging modalities but should be used conjointly to better identify specific characteristics of endocrine tumors. This represents a relatively new and evolving approach to imaging that promises to answer specific questions about the behavior and growth of endocrine tumors, their malignant potential, and responsiveness to different treatment modalities.

01 Aug 1998·Journal of nuclear medicine : official publication, Society of Nuclear Medicine

Quantitation of presynaptic cardiac sympathetic function with carbon-11-meta-hydroxyephedrine.

Article

Author: Li, Z ; Caldwell, J H ; Kroll, K ; Link, J M ; Krohn, K A ; Seymour, K

The purpose of this study was to validate an axially distributed blood-tissue exchange model for the quantitation of cardiac presynaptic sympathetic nervous system function that could be applied to PET images. The model accounts for heterogeneity in myocardial blood flow, differences in transport rates of 11C-meta-hydroxyephedrine (mHED) across the capillary endothelium and/or neuronal membranes, the virtual volumes of distribution in the interstitial space and neuron and retention of mHED in the neuronal vesicles.METHODSMultiple indicator outflow dilution and residue detection methods were used to measure the kinetics of radiolabeled intravascular space and interstitial space markers and 11C-mHED in isolated perfused rat heart at baseline and during norepinephrine neuronal transporter blockade with desipramine (DMI). The outflow dilution and residue detection data were modeled with a multiple pathway, four-region, axially distributed model of blood-tissue exchange describing flow in the capillary and exchange between regions using permeability-surface area products with units of clearance of milliliters per minute per gram. Meta-hydroxyephedrine may enter the nerve terminal via membrane transport, where it may be sequestered by first-order unidirectional uptake within vesicles. Release of mHED from the vesicles is modeled via exchange with the interstitial space.RESULTSAfter intracoronary injection, mHED transport across the capillary endothelium and in the interstitial space closely followed that of sucrose. Subsequently, mHED was retained in the heart, whereas sucrose washed out rapidly. With DMI the outflow dilution curves more closely resembled those of sucrose. Model parameters reflecting capillary-interstitial kinetics and volumes of distribution were unchanged by DMI, whereas parameters reflecting the neuronal transporter process and volumes of distribution in the nerve terminal and vesicular sequestration were markedly decreased by DMI. Application of the model to a pilot set of canine PET images of mHED suggests the feasibility of this approach.CONCLUSIONMeta-hydroxyephedrine kinetics in the heart can be quantitated using an axially distributed, blood-tissue exchange model that accounts for heterogeneity of flow, reflects changes in neuronal function and is applicable to PET images.

100 Deals associated with 11C-Meta-Hydroxyephedrine

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Heart Failure	Phase 1	-	Mayo Clinic	-
Heart Failure	Phase 1	-	Central State University Of New York Inc	-
Myocardial Ischemia	Phase 1	-	University of Michigan College of Engineering	-
Myocardial Ischemia	Phase 1	-	Central State University Of New York Inc	-
Myocardial Ischemia	Phase 1	-	Mayo Clinic	-
Myocardial Ischemia	Phase 1	-	The University of Ottawa Heart Institute	-
Sleep Apnea Syndromes	Phase 1	-	Mayo Clinic	-
Sleep Apnea Syndromes	Phase 1	-	The University of Ottawa Heart Institute	-
Sleep Apnea Syndromes	Phase 1	-	University of Michigan College of Engineering	-
Sleep Apnea Syndromes	Phase 1	-	Central State University Of New York Inc	-

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