Drug intelligence / Profile preview

mexazolam

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

Overview

Mexazolam is a benzodiazepine derivative indicated for the treatment of anxiety with or without psychoneurotic conditions. It acts as a positive allosteric modulator at the gamma‑aminobutyric acid type A (GABA_A) receptor by binding to benzodiazepine-type receptors and enhancing GABAergic neurotransmission in the central nervous system. Mexazolam is rapidly metabolized in the liver (primarily via CYP3A4) to active metabolites including chloronordiazepam (delorazepam) and chloroxazepam (lorazepam). The drug is mainly eliminated through bile and feces with less than 10% excreted in urine as metabolites. Its clinical use is generally limited to short-term management of severe anxiety due to risk of tolerance development[1][2][3][4].

Brand names
MelexSedoxil
Other names
10-chloro-11b-(2-chlorophenyl)-3-methyl-2,3,7,11b-tetrahydrobenzo[f]oxazolo[3,2-d][1,4]diazepin-6(5H)-one13-chloro-2-(2-chlorophenyl)-5-methyl-3-oxa-6,9-diazatricyclo[8.4.0.0^2,6]tetradeca‑1(10),11,13-trien‑8-one
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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