Lormetazepam

drug
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Also known as ChlorotemazepamLorametMethyllorazepamWY-4082Lormetazepan

Summary

Lormetazepam (CHEMBL22097) is an approved small-molecule sedative (ATC N05CD06); indicated across 5 conditions including anxiety and dementia.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05CD06
  • Indications: 5 conditions
  • Clinical trials: 4
  • Chemistry: 335.2 Da · C16H12Cl2N2O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL22097
NameLormetazepam
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID13314
ChEBICHEBI:52993
ATCN05CD06
Molecular formulaC16H12Cl2N2O2
Molecular weight335.2
InChIKeyFJIKWRGCXUCUIG-UHFFFAOYSA-N

SMILES: CN1C2=C(C=C(C=C2)Cl)C(=NC(C1=O)O)C3=CC=CC=C3Cl

IUPAC name: 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1-methyl-3H-1,4-benzodiazepin-2-one

ChEBI definition: A 1,4-benzodiazepinone compound having a methyl substituent at the 1-position, a hydroxy substituent at the 3-position, a 2-chlorophenyl group at the 5-position and a chloro substituent at the 7-position.

Pharmacological roles (ChEBI): sedative.

Also known as: Chlorotemazepam, Loramet, Lormetazepam, Methyllorazepam, WY-4082, Lormetazepan, LORMETAZEPAM, lormetazepam

Patent coverage: 1,576 distinct patent families (6,421 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 6,394 (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: 5 (assay-derived). Sample: Alpha-2A adrenergic receptor, Muscarinic acetylcholine receptor M2, Kappa-type opioid receptor, 3’,5’-cyclic-AMP phosphodiesterase 4D, Gamma-aminobutyric acid receptor subunit alpha-1.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P628138.85AC501.4nMCHEMBL_ACT_25130812
PDE4D5.25AC505600nMCHEMBL_ACT_25185546
OPRK15.09AC508100nMCHEMBL_ACT_25129631

Target pathways

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

Indications & clinical

Indications

5 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).

IndicationTrial phaseMONDOEFO
anxiety3MONDO:0011918EFO:0005230
dementia3MONDO:0001627HP:0000726
depressive disorder3MONDO:0002050MONDO:0002050
sleep disorder3MONDO:0100081EFO:0008568

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

Clinical trials

Total trials: 4.

Phase distribution

PhaseTrials
PHASE33
PHASE41

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02022592PHASE4COMPLETEDComparison of Lormetazepam and Midazolam Used as Sedatives for Patients That Require Intensive Care
NCT00679900PHASE3COMPLETEDComparison of Eplivanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties
NCT00788515PHASE3TERMINATEDComparison of Volinanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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