Drug intelligence / Profile preview

cilostamide

Development stage
Preclinical
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
In Vitro
01

Overview

Cilostamide is a potent and selective small molecule inhibitor of phosphodiesterase 3 (PDE3), an enzyme that regulates intracellular levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by catalyzing their hydrolysis. By specifically blocking PDE3, cilostamide increases cAMP concentrations, which modulates various downstream signaling pathways. In experimental cardiology, it is frequently used to enhance or 'unmask' the positive inotropic effects of G-protein coupled receptor (GPCR) agonists in human and animal atrial tissues. In reproductive biology, it is utilized as a research tool to maintain meiotic arrest in cumulus-oocyte complexes during in vitro culture, supporting oocyte development and fertility preservation techniques. Recent preclinical research has also identified cilostamide as a potential therapeutic agent for preventing liver injury during long-term supercooling preservation by inhibiting the PDE3B-cAMP-autophagy axis.

Other names
N-cyclohexyl-N-methyl-4-(1,2-dihydro-2-oxo-6-quinolyloxy)butyramideN-cyclohexyl-N-methyl-4-[(2-oxo-1,2-dihydroquinolin-6-yl)oxy]butanamide
02

Targets

PDE3A (Phosphodiesterase 3A)PDE3B (Phosphodiesterase 3B)

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