Drug intelligence / Profile preview

PF-06372865 + lorazepam

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-06372865 + lorazepam is an experimental combination of two central nervous system agents: PF-06372865, a selective positive allosteric modulator (PAM) of the γ-aminobutyric acid type A (GABA-A) receptor targeting the α2/3/5 subunits, and lorazepam, a classical benzodiazepine acting as a non-selective positive allosteric modulator at GABA-A receptors. PF-06372865 is designed to enhance GABA signaling with reduced sedative and cognitive side effects by selectively sparing α1 subunit activity, while lorazepam provides broad anxiolytic, anticonvulsant, and sedative properties. The combination has been studied for the suppression of epileptic activity, especially in photoepilepsy models, and both agents independently showed significant decreases in epileptiform EEG activity compared to placebo, with tolerability established in short trial settings. PF-06372865 was developed by Pfizer, and lorazepam was originally developed by Wyeth.

Brand names
AtivanLoreev
Other names
lorazepamo-Chlorooxazepamo-Chloroxazepam
02

Targets

GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)α5-GABAAR (Gamma-aminobutyric acid type A receptor alpha5beta2gamma2 subtype (GABAA receptor alpha5beta2gamma2 subtype))GABRR (GABA-A receptor subunit rho)

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