Drug intelligence / Profile preview

gacyclidine

Development stage
Phase 3
Lead developer
Otonomy
Modality
Small Molecules
Administration
Intratympanic, Intravenous
01

Overview

Gacyclidine is a psychoactive small molecule drug and a derivative of phencyclidine (PCP), specifically related to tenocyclidine (TCP). It acts as a noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, thereby inhibiting excitotoxicity by reducing excessive glutamate-induced calcium influx into neurons. Gacyclidine has neuroprotective properties and has been investigated for reducing damage to the brain or spinal cord in conditions such as traumatic brain injury, spinal cord injury, stroke, convulsions, and tinnitus. Preclinical studies demonstrated its ability to reduce lesion size and improve functional recovery after neural trauma. A lipid-based intratympanic formulation (OTO‑313) has been studied for tinnitus treatment. Despite promising animal data, clinical trials in humans have not shown significant benefit for acute spinal cord injury or other indications[1][4][5][6][7].

Other names
gacyclidine [INN]1-[(1R,2S)-2-methyl-1-thiophen-2-ylcyclohexyl]piperidine
02

Targets

GLUD1 (Glutamate dehydrogenase 1, mitochondrial)GRIN2B (N-methyl-D-aspartate Receptor Subunit Combination: NR1a/NR2B)

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