Drug intelligence / Profile preview

Indiplon

Development stage
Preclinical
Lead developer
Neurocrine Biosciences
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Indiplon is a novel, investigational nonbenzodiazepine hypnotic sedative of the pyrazolopyrimidine class developed for the treatment of insomnia. It was designed in two oral formulations—immediate-release for sleep onset and modified-release for sleep maintenance. Indiplon acts as a positive allosteric modulator at GABA-A receptors, with high affinity and selectivity for alpha1 subunit-containing GABA-A receptors, enhancing the inhibitory action of gamma-aminobutyric acid (GABA) in the brain. The drug has a short elimination half-life (1.5–2 hours), making it suitable for minimizing next-day residual effects. Despite demonstrating efficacy and tolerability in clinical trials involving over 7,500 participants, development was discontinued after an FDA approvable letter requested additional data[1][2][3][5][6][8].

Brand names
Indiplon
Other names
Indiplon-d3Indiplon-d-3Indiplon-d 3325715-02-4
02

Targets

GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)

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