Delving into the Latest Updates on [(18)F]MNI-617 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms-

Target

PDE4

Action

inhibitors

Mechanism

PDE4 inhibitors(Phosphodieterase 4 inhibitors)

Therapeutic Areas

Nervous System Diseases

Active Indication

Neurodegenerative Diseases

Inactive Indication

AmnesiaDepressive DisorderParkinson Disease

Originator Organization

Molecular NeuroImaging LLC

Active Organization

Molecular NeuroImaging LLC

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Phosphodiesterase (PDE) 4 is the most prevalent PDE in the central nervous system (CNS) and catalyzes hydrolysis of intracellular cAMP, a secondary messenger. By therapeutic inhibition of PDE4, intracellular cAMP levels can be stabilized, and the symptoms of psychiatric and neurodegenerative disorders including depression, memory loss and Parkinson's disease can be ameliorated. Radiotracers targeting PDE4 can be used to study PDE4 density and function, and evaluate new PDE4 therapeutics, in vivo in a non-invasive way, as has been shown using the carbon-11 labeled PDE4 inhibitor R-(-)-rolipram. Herein we describe a small series of rolipram analogs that contain fluoro- or iodo-substituents that could be used as fluorine-18 PET or iodine-123 SPECT PDE4 radiotracers. This series was evaluated with an in vitro binding assay and a 4-(fluoromethyl) derivative of rolipram, MNI-617, was identified, with a five-fold increase in affinity for PDE4 (Kd = 0.26 nM) over R-(-)-rolipram (Kd = 1.6 nM). A deutero-analogue d2 -[(18) F]MNI-617 was radiolabeled and produced in 23% yield with high (>5 Ci/µmol) specific activity and evaluated in non-human primate, where it rapidly entered the brain, with SUVs between 4 and 5, and with a distribution pattern consistent with that of PDE4.

100 Deals associated with [(18)F]MNI-617

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Neurodegenerative Diseases	Preclinical	United States	Molecular NeuroImaging LLC	23 May 2023
Amnesia	Preclinical	United States	Molecular NeuroImaging LLC	22 Mar 2016
Depressive Disorder	Preclinical	United States	Molecular NeuroImaging LLC	22 Mar 2016
Parkinson Disease	Preclinical	United States	Molecular NeuroImaging LLC	22 Mar 2016