Drug intelligence / Profile preview

PT-3902

Development stage
Preclinical
Lead developer
Path Therapeutics
Modality
Small Molecules
01

Overview

PT-3902 is a selective allosteric inhibitor of cAMP-specific 3',5'-cyclic phosphodiesterase 4B (PDE4B) being developed by Path Therapeutics as a potential anti-seizure treatment for Dravet Syndrome. Discovered using the MitoREAD machine-learning-derived screening platform, PT-3902 was synthesized de novo to target a novel allosteric binding pocket within the PDE4 active site. In vitro assays show that PT-3902 inhibits PDE4B with an IC50 of 27 nM and exhibits a 200-fold selectivity for PDE4B over PDE4D. This subtype selectivity is designed to offer improved tolerability compared to traditional pan-PDE4 inhibitors, which are often limited by dose-dependent adverse effects like nausea and emesis.

02

Targets

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

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