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Atlas / Drug / Lorazepam

Lorazepam

drug
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Also known as AbblorazAtivanLorazLorazepam civLorazepam intensolLorazepam preservative freeLoreev xrNSC-289758TemestaWY-4036SID29215381SID144205222C0164982

Summary

Lorazepam (CHEMBL580) is an approved small molecule (ATC N05BA56) targeting GPR68 and ADRA1B; indicated across 26 conditions including anxiety and epilepsy.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05BA56 (+1 more)
  • Targets: 2 (GPR68, ADRA1B)
  • Indications: 26 conditions
  • Clinical trials: 97
  • Chemistry: 321.2 Da · C15H10Cl2N2O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL580
NameLorazepam
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3958
ATCN05BA56, N05BA06
Molecular formulaC15H10Cl2N2O2
Molecular weight321.2
InChIKeyDIWRORZWFLOCLC-UHFFFAOYSA-N

SMILES: C1=CC=C(C(=C1)C2=NC(C(=O)NC3=C2C=C(C=C3)Cl)O)Cl

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

Also known as: Abbloraz, Ativan, Loraz, Lorazepam, Lorazepam civ, Lorazepam intensol, Lorazepam preservative free, Loreev xr, NSC-289758, Temesta, WY-4036, lorazepam

Patent coverage: 10,809 distinct patent families (39,807 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 39,401 (99%) 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
GPR68GPR68Positive0.2%Q15743
ADRA1Bα1B-adrenoceptorPositive3.80%P35368

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Prelamin-A/C, Progesterone receptor, Gamma-aminobutyric acid receptor subunit alpha-1, Fatty acid-binding protein, liver.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P628138.13AC507.4nMCHEMBL_ACT_25130756

Target pathways

Aggregated over 2 target gene(s): GPR68, ADRA1B.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Class A/1 (Rhodopsin-like receptors)2ADRA1B, GPR68
G alpha (q) signalling events2ADRA1B, GPR68
Signal Transduction1ADRA1B
Signaling by GPCR1ADRA1B
Amine ligand-binding receptors1ADRA1B
GPCR downstream signalling1ADRA1B
Adrenoceptors1ADRA1B
G alpha (12/13) signalling events1ADRA1B
GPCR ligand binding1ADRA1B

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway2
phospholipase C-activating G protein-coupled receptor signaling pathway2
signal transduction2
inflammatory response1
adenylate cyclase-activating G protein-coupled receptor signaling pathway1
insulin secretion1
monocyte differentiation1
response to fluid shear stress1
positive regulation of insulin secretion involved in cellular response to glucose stimulus1
osteoclast development1
negative regulation of monocyte differentiation1
cellular response to pH1
cellular response to acidic pH1
positive regulation of osteoclast development1
positive regulation of insulin secretion1

Indications & clinical

Indications

26 indications (4 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
anxiety4MONDO:0011918EFO:0005230
anxiety disorder4MONDO:0005618EFO:0006788
epilepsy3MONDO:0005027EFO:0000474
schizoaffective disorder3MONDO:0005487EFO:0005411
dementia3MONDO:0001627HP:0000726
depressive disorder3MONDO:0002050MONDO:0002050
alcohol withdrawal2MONDO:0005433EFO:0004777
cocaine dependence2MONDO:0005186EFO:0002610
reflex epilepsy2MONDO:0017768EFO:1001146
visual epilepsy2MONDO:0001386HP:0001250
delirium2MONDO:0045057EFO:0009267
methamphetamine dependence2MONDO:0005419EFO:0004701
alcohol abuse2MONDO:0002046MONDO:0007079
Down syndrome2MONDO:0008608EFO:0001064
drug dependence1MONDO:0005303EFO:0003890
obsessive-compulsive disorder1MONDO:0008114EFO:0004242
voice disorders1MONDO:0043862EFO:0009692
Alzheimer disease1MONDO:0004975MONDO:0004975
epidermolysis bullosa0MONDO:0006541EFO:1000690

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

Clinical trials

Total trials: 97.

Phase distribution

PhaseTrials
PHASE425
Not specified19
PHASE117
PHASE215
PHASE314
PHASE2/PHASE33
EARLY_PHASE13
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02078336PHASE4ACTIVE_NOT_RECRUITINGOptimization of Procedural Sedation Protocol Used for Dental Care Delivery in People With Mental Disability
NCT04240626PHASE4ACTIVE_NOT_RECRUITINGMultimodal Analgesia Effect on Post Surgical Patient
NCT05599126PHASE4RECRUITINGA Study of Mianserin in Combination With SSRIs in Depression With Sleep Problems
NCT06004115PHASE4RECRUITINGProcesses and Circuitry Underlying Threat Sensitivity as a Treatment Target for Co-morbid Anxiety and Depression
NCT06799494PHASE4RECRUITINGHPV Vaccine Reduced Dose
NCT07428681PHASE4NOT_YET_RECRUITINGLorazepam for Delirium Prevention in Critically Ill Patients With High Anttila-Index
NCT00000441PHASE4COMPLETEDDrug Therapy for Alcohol Detoxification
NCT00044642PHASE4COMPLETEDLorazepam-Induced Toxicity in the Aged
NCT00158873PHASE4COMPLETEDPharmaco-Economic Study Of Ultiva In Intensive Care Unit(ICU)Subjects
NCT00249366PHASE4COMPLETEDTreatment of Alcohol Withdrawal in Hospital Patients
NCT00457366PHASE4COMPLETEDA Comparison Study of the Efficacy of Quetiapine and Haloperidol in Agitated Adults in Emergency Room
NCT00624780PHASE4COMPLETEDSafety and Efficacy Evaluation Of Pregabalin (Lyrica) With Patients With Generalized Anxiety Disorder
NCT01121055PHASE4UNKNOWNEffect of Additive Lorazepam on Patient Satisfaction as a Premedication in Diagnostic Flexible Bronchoscopy
NCT01330459PHASE4COMPLETEDHydrocodone For Pain Control in First Trimester Surgical Abortion
NCT01441843PHASE4COMPLETEDResistance Under the Microscope
NCT01889602PHASE4COMPLETEDCharacterizing and Predicting Drug Effects on Cognition
NCT02367755PHASE4UNKNOWNTherapeutic Hypothermia With Propofol in Survival and Neurological Prognoses After Cardiac Arrest
NCT02407704PHASE4COMPLETEDA Multi-level Life-span Characterization of Adult-depression and Effects of Medication and Exercise
NCT03090620PHASE4COMPLETEDTreatment of Adolescent Antimuscarinic (Anticholinergic) Toxidrome
NCT03110900PHASE4TERMINATEDInhaled Loxapine vs Intramuscular (IM) Haloperidol + Lorazepam for Agitation
NCT03235531PHASE4UNKNOWNAssessment of Valproate on Ethanol Withdrawal
NCT03788889PHASE4WITHDRAWNAlcohol Withdrawal Syndrome Treated With Adjunctive Phenobarbital or Ketamine
NCT04004416PHASE4COMPLETEDMulti-modal Assessment of Gamma-aminobutyric Acid (GABA) Function in Psychosis
NCT04156464PHASE4UNKNOWNPhenobarbital vs Ativan for Alcohol Withdrawal in the Intensive Care Unit
NCT06093451PHASE4UNKNOWNEvaluating Sublingual Dexmedetomidine For Moderate To Severe Agitation In Inpatients With Schizophrenia Or Bipolar Disorder
NCT03743649PHASE2/PHASE3ACTIVE_NOT_RECRUITINGHaloperidol and Lorazepam in Controlling Symptoms of Persistent Agitated Delirium in Patients With Advanced Cancer Undergoing Palliative Care
NCT06752616PHASE2/PHASE3RECRUITINGAcute Agitation in Emergency Psychiatry
NCT07017452PHASE3NOT_YET_RECRUITINGTrial to Assess the Efficacy and Safety During Convective Radiofrequency Water Vapor Thermal Therapy (REZUM) for Benign Prostate Hyperplasia
NCT00004297PHASE3COMPLETEDPhase III Randomized Study of Diazepam Vs Lorazepam Vs Placebo for Prehospital Treatment of Status Epilepticus
NCT00109395PHASE2/PHASE3COMPLETEDLorazepam Sedation for Critically Ill Children
NCT00116064PHASE3COMPLETEDIntranasal Lorazepam Versus Intramuscular Paraldehyde in Paediatric Convulsions
NCT00343096PHASE3TERMINATEDRandomized Trial Comparing 3 Routes of Delivering Lorazepam to Children.
NCT00735527PHASE3COMPLETEDNasal Versus Venous Lorazepam for Control of Acute Seizures in Children
NCT01827293PHASE3COMPLETEDPromethazine vs. Lorazepam for Treatment of Vertigo
NCT01870024PHASE3COMPLETEDComparison Between Lorazepam, Clonazepam and Clonazepam + Fosphenytoin for the Treatment of Out-of-hospital Generalized Status Epilepticus
NCT01901003PHASE3COMPLETEDSedative Premedication: Efficacy On Patient Experience
NCT02134366PHASE3TERMINATEDClobazam Use in Epilepsia Partialis Continua - Pilot Study
NCT02147548PHASE3COMPLETEDEvaluation of the Effects of Etifoxine 100 mg and Lorazepam 2 mg on Vigilance and Cognitive Functions in the Elderly
NCT02239380PHASE3COMPLETEDLorazepam for the Treatment of Status Epilepticus or Repetitive Status Epilepticus in Japan
NCT02305797PHASE3COMPLETEDEDG004 Treatment of Adult Patients With Generalized Anxiety Disorder (GAD)

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 5 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

77 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)ADRA1B
ALFUZOSINChEMBLPhase 4 (approved)ADRA1B
AMLODIPINEChEMBLPhase 4 (approved)ADRA1B
APRACLONIDINEChEMBLPhase 4 (approved)ADRA1B
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRA1B
ASENAPINEChEMBLPhase 4 (approved)ADRA1B
ATENOLOLChEMBLPhase 4 (approved)ADRA1B
AZELASTINEChEMBLPhase 4 (approved)ADRA1B
BREXPIPRAZOLEChEMBLPhase 4 (approved)ADRA1B
BRIMONIDINEChEMBLPhase 4 (approved)ADRA1B
BUSPIRONEChEMBLPhase 4 (approved)ADRA1B
CARIPRAZINEChEMBLPhase 4 (approved)ADRA1B
CINACALCETChEMBLPhase 4 (approved)ADRA1B
CISAPRIDEChEMBLPhase 4 (approved)ADRA1B
CLONIDINEChEMBLPhase 4 (approved)ADRA1B
CLOZAPINEChEMBLPhase 4 (approved)ADRA1B
DEXMEDETOMIDINEChEMBLPhase 4 (approved)ADRA1B
DOPAMINEChEMBLPhase 4 (approved)ADRA1B
DOXAZOSINChEMBLPhase 4 (approved)ADRA1B
EBASTINEChEMBLPhase 4 (approved)ADRA1B
EPINEPHRINEChEMBLPhase 4 (approved)ADRA1B
FENOLDOPAMChEMBLPhase 4 (approved)ADRA1B
FENTANYLChEMBLPhase 4 (approved)ADRA1B
HALOPERIDOLChEMBLPhase 4 (approved)ADRA1B
INDACATEROLChEMBLPhase 4 (approved)ADRA1B
INDORAMINChEMBLPhase 4 (approved)ADRA1B
ISOPROTERENOLChEMBLPhase 4 (approved)ADRA1B
LABETALOLChEMBLPhase 4 (approved)ADRA1B
LOPERAMIDEChEMBLPhase 4 (approved)ADRA1B
LUMATEPERONE TOSYLATEChEMBLPhase 4 (approved)ADRA1B
MOXISYLYTEChEMBLPhase 4 (approved)ADRA1B
NAFTOPIDILChEMBLPhase 4 (approved)ADRA1B
NEFAZODONEChEMBLPhase 4 (approved)ADRA1B
NOREPINEPHRINEChEMBLPhase 4 (approved)ADRA1B
OLANZAPINEChEMBLPhase 4 (approved)ADRA1B
OXYMETAZOLINEChEMBLPhase 4 (approved)ADRA1B
PHENTOLAMINEChEMBLPhase 4 (approved)ADRA1B
PHENYLEPHRINEChEMBLPhase 4 (approved)ADRA1B
PRAZOSINChEMBLPhase 4 (approved)ADRA1B
QUETIAPINEChEMBLPhase 4 (approved)ADRA1B
RISPERIDONEChEMBLPhase 4 (approved)ADRA1B
SERTINDOLEChEMBLPhase 4 (approved)ADRA1B
SILODOSINChEMBLPhase 4 (approved)ADRA1B
TAMSULOSINChEMBLPhase 4 (approved)ADRA1B
TEGASERODChEMBLPhase 4 (approved)ADRA1B
TERAZOSINChEMBLPhase 4 (approved)ADRA1B
TERFENADINEChEMBLPhase 4 (approved)ADRA1B
TOLAZOLINEChEMBLPhase 4 (approved)ADRA1B
VERAPAMILChEMBLPhase 4 (approved)ADRA1B
VILAZODONEChEMBLPhase 4 (approved)ADRA1B
XYLOMETAZOLINEChEMBLPhase 4 (approved)ADRA1B
ZIPRASIDONEChEMBLPhase 4 (approved)ADRA1B
BUNAZOSINChEMBLPhase 3ADRA1B
IDAZOXANChEMBLPhase 3ADRA1B
LATREPIRDINEChEMBLPhase 3ADRA1B
MEDETOMIDINEChEMBLPhase 3ADRA1B
VOLINANSERINChEMBLPhase 3ADRA1B
YOHIMBINEChEMBLPhase 3ADRA1B
ABANOQUILChEMBLPhase 2ADRA1B
ATIPAMEZOLEChEMBLPhase 2ADRA1B

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot