Drug intelligence / Profile preview

[11C]JMJ-129-d2

Development stage
Phase 1
Lead developer
National Institute of Mental Health
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

`[11C]JMJ-129-d2` is a carbon-11 labeled, deuterated small molecule positron emission tomography (PET) radioligand developed by the National Institute of Mental Health (NIMH) for imaging and quantifying phosphodiesterase-4D (PDE4D) in the brain. PDE4D is an enzyme that hydrolyzes cyclic adenosine monophosphate (cAMP) and is implicated in cognitive function, depression, and neurodegenerative diseases such as Alzheimer's disease. `[11C]JMJ-129-d2` was designed as a deuterated analogue of `[11C]JMJ-129` to overcome the issue of brain-penetrant, lipophilic radiometabolites that interfered with the quantification of PDE4D in human brain imaging. By incorporating deuterium, the rate of oxidative hydroxylation is slowed, reducing the formation of these troublesome radiometabolites and improving the accuracy of PET imaging. The radioligand is currently in Phase 1 clinical development for brain imaging in healthy volunteers.

Other names
[¹¹C]JMJ-129-d2carbon-11 JMJ-129-d2carbon11 JMJ-129-d2carbon 11 JMJ-129-d2
02

Targets

PDE4B (3',5'-cyclic-AMP phosphodiesterase 4B)PDE4D (Phosphodiesterase 4D)

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