An Open-Label Study to Investigate the Total Body Distribution and Radiation Dosimetry of the Positron Emission Tomography Ligand 18F-JNJ-64326067 in Healthy Subjects

The purpose of this study is to measure the whole-body distribution and radiation dosimetry of 18F-JNJ-64326067 in healthy participants.

Start Date11 Jul 2018

Sponsor / Collaborator

Janssen Research & Development LLC

NCT03239561 / CompletedEarly Phase 1

Phase 0 Exploratory Study of [18F]MNI-1020 (Also Known as [18F]JNJ-64326067) as an Imaging Marker for Tau Protein in the Brain of Subjects With Alzheimer's Disease Compared to Healthy Subjects

The primary objectives of this study are to characterize [18F]molecular neuroimaging (MNI)-1020, a positron emission tomography (PET) radioligand for imaging tau pathology, to visually and quantitatively assess and compare brain uptake and pharmacokinetics of [18F]MNI-1020 in participants with probable Alzheimer's disease (AD) and compare with age matched healthy participants, to evaluate the safety of a single injection of [18F]MNI-1020 and to compare the distribution of tau (using [18F]MNI-1020) and amyloid beta (using florbetapir) in participants with probable AD.

Start Date06 Sep 2017

Sponsor / Collaborator

Janssen Research & Development LLC

100 Clinical Results associated with 18F-JNJ-64326067

100 Translational Medicine associated with 18F-JNJ-64326067

100 Patents (Medical) associated with 18F-JNJ-64326067

Literatures (Medical) associated with 18F-JNJ-64326067

01 Dec 2020·European Journal of Nuclear Medicine and Molecular ImagingQ1 · MEDICINE

Clinical evaluation of [18F] JNJ-64326067, a novel candidate PET tracer for the detection of tau pathology in Alzheimer’s disease

Q1 · MEDICINE

Article

Author: Rombouts, Frederik J R ; Timmers, Maarten ; Constantinescu, Cristian C ; Janssens, Luc ; Schmidt, Mark E ; Kolb, Hartmuth ; Russell, David S ; Madonia, Jennifer ; Sandiego, Christine M ; Barret, Olivier ; Moechars, Diederik

AbstractPurposeThe accumulation of misfolded tau is a common feature of several neurodegenerative disorders, with Alzheimer’s disease (AD) being the most common. Earlier we identified JNJ-64326067, a novel isoquinoline derivative with high affinity and selectivity for tau aggregates from human AD brain. We report the dosimetry of [18F] JNJ-64326067 and results of a proof-of-concept study comparing subjects with probable Alzheimer’s disease to age-matched healthy controls.Methods[18F] JNJ-64326067 PET scans were acquired for 90 min and then from 120 to 180 min in 5 participants with [18F]-florbetapir PET amyloid positive probable AD (73 ± 9 years) and 5 [18F]-florbetapir PET amyloid negative healthy controls (71 ± 7 years). Whole-body [18F] JNJ-64326067 PET CT scans were acquired in six healthy subjects for 5.5 h in 3 scanning sessions. Brain PET scans were visually reviewed. Regional quantification included kinetic analysis of distribution volume ration (DVR) estimated by Logan graphical analysis over the entire scan and static analysis of SUVr in late frames. Both methods used ventral cerebellar cortex as a reference region.ResultsOne of the healthy controls had focal areas of PET signal in occipital and parietal cortex underlying the site of a gunshot injury as an adolescent; the other four healthy subjects had no tau brain signal. Four of the 5 AD participants had visually apparent retention of [18F] JNJ-64326067 in relevant cortical regions. One of the AD subjects was visually negative. Cortical signal in visually positive subjects approached steady state by 120 min. Temporal and frontal cortical SUVr/DVR values in visually positive AD subjects ranged from 1.21 to 3.09/1.2 to 2.18 and from 0.92 to 1.28/0.91 to 1.16 in healthy controls. Whole-body effective dose was estimated to be 0.0257 mSv/MBq for females and 0.0254 mSv/MBq for males.Conclusions[18F] JNJ-64326067 could be useful for detection and quantitation of tau aggregates.

28 Mar 2019·Journal of Medicinal ChemistryQ1 · MEDICINE

Discovery of N-(4-[¹⁸F]Fluoro-5-methylpyridin-2-yl)isoquinolin-6-amine (JNJ-64326067), a New Promising Tau Positron Emission Tomography Imaging Tracer

Q1 · MEDICINE

Article

Author: Leenaerts, Joseph E. ; te Riele, Paula ; Iturrino, Laura ; Xia, Chunfang A. ; Song, Fengbin ; Vandenberghe, Rik ; Rombouts, Frederik J. R. ; Kolb, Hartmuth ; Andres, Jose-Ignacio ; Bormans, Guy ; Wuyts, Stijn ; Bottelbergs, Astrid ; Declercq, Lieven ; Wintmolders, Cindy ; Moechars, Diederik ; Chen, Lu ; Marien, Jonas

In Alzheimer's disease, the density and spread of aggregated tau protein track well with neurodegeneration and cognitive decline, making the imaging of aggregated tau a compelling biomarker. A structure-activity relationship exploration around an isoquinoline hit, followed by an exploration of tolerated fluorination positions, allowed us to identify 9 (JNJ-64326067), a potent and selective binder to aggregated tau with a favorable pharmacokinetic profile and no apparent off-target binding. This was confirmed in rat and monkey positron emission tomography studies using [¹⁸F]9.

100 Deals associated with 18F-JNJ-64326067

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 3	US	Janssen Research & Development LLC	06 Sep 2017
Diagnostic agents	Phase 1	-	Facultés Universitaires Catholiques de Mons	-
Diagnostic agents	Phase 1	-	Janssen Global Services LLC	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

18F-JNJ-64326067

Overview

Basic Info

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation