Brotizolam

Summary

Brotizolam (CHEMBL32479) is an approved small-molecule anticonvulsant (ATC N05CD09); indicated across 6 conditions including insomnia and anxiety.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05CD09
• Indications: 6 conditions
• Clinical trials: 6
• Chemistry: 393.7 Da · C15H10BrClN4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL32479
Name	Brotizolam
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2451
ChEBI	CHEBI:31308
ATC	N05CD09
Molecular formula	C15H10BrClN4S
Molecular weight	393.7
InChIKey	UMSGKTJDUHERQW-UHFFFAOYSA-N

SMILES: CC1=NN=C2N1C3=C(C=C(S3)Br)C(=NC2)C4=CC=CC=C4Cl

IUPAC name: 4-bromo-7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene

ChEBI definition: A thienotriazolodiazepine that is 6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine substituted by bromo, 2-chlorophenyl, and methyl groups at positions 2, 4, and 9, respectively. It is used as a hypnotic in the management of insomnia.

Pharmacological roles (ChEBI): sedative, anticonvulsant, anxiolytic drug, muscle relaxant, GABAA receptor agonist.

Also known as: Brotizolam, Lendorm, Lendormin, Mederantil, Nimbisan, Sintonal, WE 941, WE-941, BROTIZOLAM, SID144207150

Patent coverage: 1,689 distinct patent families (7,289 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 7,270 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Platelet-activating factor receptor.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PTAFR	6.52	IC50	300	nM	CHEMBL_ACT_999180

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

6 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
insomnia	3	MONDO:0013600	EFO:0004698
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050
sleep disorder	3	MONDO:0100081	EFO:0008568

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE3	3
PHASE1	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00347295	PHASE3	COMPLETED	Randomised, Double-blind Study to Investigate the Safety and Efficacy of Brotizolam in Insomnia Outpatients.
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT02776228	PHASE3	UNKNOWN	Treatment With Benzodiazepine After Cardiac Surgery
NCT01361022	PHASE1	COMPLETED	To Assess the Bioequivalence of Brotizolam Tablets 250 Mcg vs. Lendormin Tablets 250 Mcg Administered to Healthy Adult Volunteers
NCT02218645	PHASE1	COMPLETED	Bioequivalence Between WE 941 OD and Brotizolam (Lendormin®) Taken With Water in Healthy Adult Males
NCT02218658	PHASE1	COMPLETED	Bioequivalence Between WE 941 OD and Brotizolam (Lendormin®) in Healthy Adult Males

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).