Drug intelligence / Profile preview

AZD-3043

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous
01

Overview

AZD-3043 is a short-acting intravenous anesthetic and sedative agent that acts as a positive allosteric modulator of the γ-aminobutyric acid type A (GABA(A)) receptor. It contains a metabolically labile ester moiety, leading to rapid hydrolysis and clearance, which results in a short duration of action even after prolonged infusion. The drug was initially invented by Theravance and later developed by AstraZeneca for use in anesthesia and sedation. Preclinical studies demonstrated that AZD-3043 potentiates GABA(A) receptor-mediated chloride currents, produces hypnosis, and causes electroencephalograph depression in animal models. It also inhibits neuronal nicotinic acetylcholine receptors. Phase I clinical trials were completed in Sweden and the UK for anesthesia; however, further development was discontinued[1][2][4][5][7].

02

Targets

GABA-B (Gamma-aminobutyric acid receptor type B)GABAA (Gamma-aminobutyric acid receptor)Nicotinic Acetylcholine Receptor

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