Drug intelligence / Profile preview

DP-VPA

Development stage
Preclinical
Lead developer
D-Pharm
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
01

Overview

DP-VPA is a proprietary lipid-modified prodrug of valproic acid (VPA), developed by D-Pharm using their Regulated Activation of Prodrugs (D-RAP) technology. In this formulation, VPA is covalently linked to a phospholipid moiety, creating a compound that remains inactive until it encounters elevated levels of phospholipase A2 (PLA2), an enzyme upregulated in hyperactive neurons during seizures. This targeted activation allows for the preferential release of VPA at sites of epileptic activity, potentially enabling effective seizure control at lower systemic doses and reducing dose-dependent side effects associated with conventional valproic acid therapy. The drug has been investigated primarily for resistant epilepsy but also considered for migraine prophylaxis and bipolar disorder[1][3][5]. Clinical trials have reached Phase 2 in epilepsy and migraine disorders[1][3][6].

02

Targets

GABRR (GABA-A receptor subunit rho)GABA-B (Gamma-aminobutyric acid receptor type B)ABAT (4-aminobutyrate aminotransferase)

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