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Meclizine

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Also known as MeclozinaMeclozineNSC-169189monamineMECLIZINE HYDROCHLORIDE

Summary

Meclizine (CHEMBL1623) is an approved small molecule (ATC R06AE55) targeting NR1I3; indicated across 5 conditions including allergic disease and motion sickness.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: R06AE55 (+1 more)
  • Targets: 1 (NR1I3)
  • Indications: 5 conditions
  • Clinical trials: 8
  • Chemistry: 390.9 Da · C25H27ClN2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL1623
NameMeclizine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4034
ATCR06AE55, R06AE05
Molecular formulaC25H27ClN2
Molecular weight390.9
InChIKeyOCJYIGYOJCODJL-UHFFFAOYSA-N

SMILES: CC1=CC(=CC=C1)CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(C=C4)Cl

IUPAC name: 1-[(4-chlorophenyl)-phenylmethyl]-4-[(3-methylphenyl)methyl]piperazine

Also known as: Meclizine, Meclozina, Meclozine, NSC-169189, meclizine, monamine, MECLIZINE, MECLIZINE HYDROCHLORIDE, meclozine

Parent form; salt/anhydrous children: CHEMBL1085765, CHEMBL1200590, CHEMBL1324020, CHEMBL3989555

Patent coverage: 5,582 distinct patent families (20,272 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 19,677 (97%) 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
NR1I3Constitutive androstane receptorAntagonist7.160.2%Q14994

Broader ChEMBL bioactivity targets: 24 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Histamine H2 receptor, D(1A) dopamine receptor, Serine protease hepsin, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, D(2) dopamine receptor, Cannabinoid receptor 1.

Bioactivity

ChEMBL activities: 20 potent at pChembl ≥ 5 of 28 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HTR2A6.38AC50413.3nMCHEMBL_ACT_25173462
KCNH26.11AC50777.5nMCHEMBL_ACT_25117194
DRD36.02AC50950nMCHEMBL_ACT_25193089
HRH15.96AC501100nMCHEMBL_ACT_25212061
HTR2B5.94AC501138nMCHEMBL_ACT_25163994
HRH25.84AC501454nMCHEMBL_ACT_25114338
CNR15.74AC501840nMCHEMBL_ACT_25181367
HPN5.7IC502020nMCHEMBL_ACT_17720153
ADRA1A5.69AC502062nMCHEMBL_ACT_25137668
DRD25.51AC503100nMCHEMBL_ACT_25139886
SLC6A25.49AC503239nMCHEMBL_ACT_25145756
DRD45.37AC504240nMCHEMBL_ACT_25127297
ADRA1A5.36AC504413nMCHEMBL_ACT_25138338
ADRA2A5.31AC504867nMCHEMBL_ACT_25156185
ADRA2C5.26AC505500nMCHEMBL_ACT_25147426
SLC6A35.22AC505990nMCHEMBL_ACT_25124715
ADORA35.12AC507608nMCHEMBL_ACT_25198524
CNR15.1AC508000nMCHEMBL_ACT_25230448
OPRK15.03AC509278nMCHEMBL_ACT_25129028
DRD15.01AC509831nMCHEMBL_ACT_25114966

Target pathways

Aggregated over 1 target gene(s): NR1I3.

Top Reactome pathways

1 total, by targets touching each:

PathwayTargetsGenes
Nuclear Receptor transcription pathway1NR1I3

Dominant GO biological processes

GO termTargets
negative regulation of transcription by RNA polymerase II1
osteoblast differentiation1
signal transduction1
cell differentiation1
intracellular receptor signaling pathway1
positive regulation of transcription by RNA polymerase II1
regulation of DNA-templated transcription1
negative regulation of DNA-templated transcription1

Indications & clinical

Indications

5 indications (1 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
allergic disease4MONDO:0005271MONDO:0005271
motion sickness2MONDO:0008015EFO:0006928
hepatocellular carcinoma1MONDO:0007256EFO:0000182

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

Clinical trials

Total trials: 8.

Phase distribution

PhaseTrials
PHASE12
Not specified2
PHASE41
PHASE31
PHASE21
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04482985PHASE4UNKNOWNMeclizine Plasma Levels in Responders and Non-responders
NCT02112578PHASE3COMPLETEDNon Inferiority of Meclin® (Meclizine Chlorhydrate) Versus Dramin® (Dimenhydrinate) in Control of Acute Vertigo Symptoms From Peripheral Origin
NCT01443858PHASE2COMPLETEDMeclizine as a Potential Smoking Cessation Treatment
NCT04564144PHASE1/PHASE2UNKNOWNEvaluation of Meclizine Orodispersible Tablet Pharmacokinetic in Human Volunteers
NCT01537471PHASE1COMPLETEDThe Effects of Antihistamines on Pre-Pulse Inhibition
NCT03253289PHASE1COMPLETEDMeclizine for Hepatocellular Carcinoma
NCT00641797Not specifiedCOMPLETEDTreating Benign Paroxysmal Positional Vertigo (BPPV) in ED Patients
NCT02625181Not specifiedCOMPLETEDReal-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis

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.

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.

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

MoleculeSourceStatusShared targets
ACETAMINOPHENChEMBL + PubChemPhase 4 (approved)NR1I3
AMOXICILLINChEMBL + PubChemPhase 4 (approved)NR1I3
BOSENTANChEMBL + PubChemPhase 4 (approved)NR1I3
CLOTRIMAZOLEChEMBL + PubChemPhase 4 (approved)NR1I3
CYCLOSPORINEChEMBL + PubChemPhase 4 (approved)NR1I3
DICLOFENACChEMBL + PubChemPhase 4 (approved)NR1I3
ETHINYL ESTRADIOLChEMBL + PubChemPhase 4 (approved)NR1I3
OLANZAPINEChEMBL + PubChemPhase 4 (approved)NR1I3
REGORAFENIBChEMBL + PubChemPhase 4 (approved)NR1I3
REPAGLINIDEChEMBL + PubChemPhase 4 (approved)NR1I3
ROSIGLITAZONEChEMBL + PubChemPhase 4 (approved)NR1I3
SIMVASTATINChEMBL + PubChemPhase 4 (approved)NR1I3
TOLCAPONEChEMBL + PubChemPhase 4 (approved)NR1I3
VERAPAMILChEMBL + PubChemPhase 4 (approved)NR1I3
ZAFIRLUKASTChEMBL + PubChemPhase 4 (approved)NR1I3
EPALRESTATChEMBLPhase 4 (approved)NR1I3
GLIMEPIRIDEChEMBLPhase 4 (approved)NR1I3
IBUPROFENChEMBLPhase 4 (approved)NR1I3
KETOCONAZOLEChEMBLPhase 4 (approved)NR1I3
LUMIRACOXIBChEMBLPhase 4 (approved)NR1I3
RACECADOTRILChEMBLPhase 4 (approved)NR1I3
RIMONABANTChEMBLPhase 4 (approved)NR1I3
TROGLITAZONEChEMBLPhase 4 (approved)NR1I3
GLIQUIDONEChEMBLPhase 2NR1I3
TIRACIZINEChEMBLPhase 2NR1I3
AllantoinPubChemApprovedNR1I3
AlprostadilPubChemApprovedNR1I3
anhydrous citric acidPubChemApprovedNR1I3
argininePubChemApprovedNR1I3
ascorbic acidPubChemApprovedNR1I3
AtorvastatinPubChemApprovedNR1I3
Benzoic AcidPubChemApprovedNR1I3
BiotinPubChemApprovedNR1I3
BorneolPubChemApprovedNR1I3
Caffeic AcidPubChemApprovedNR1I3
CaffeinePubChemApprovedNR1I3
CannabidiolPubChemApprovedNR1I3
caprylic acidPubChemApprovedNR1I3
CarprofenPubChemApprovedNR1I3
Chlorogenic AcidPubChemApprovedNR1I3
Cinnamic AcidPubChemApprovedNR1I3
CoumarinPubChemApprovedNR1I3
DoconexentPubChemApprovedNR1I3
eucalyptolPubChemApprovedNR1I3
EugenolPubChemApprovedNR1I3
Folic AcidPubChemApprovedNR1I3
Gallic AcidPubChemApprovedNR1I3
glyceryl lauratePubChemApprovedNR1I3
IcosapentPubChemApprovedNR1I3
IsoniazidPubChemApprovedNR1I3
Lauric AcidPubChemApprovedNR1I3
limonene, (+)-PubChemApprovedNR1I3
niacinPubChemApprovedNR1I3
OxycodonePubChemApprovedNR1I3
OxymorphonePubChemApprovedNR1I3
Palmitic AcidPubChemApprovedNR1I3
PhenobarbitalPubChemApprovedNR1I3
phytonadionePubChemApprovedNR1I3
prasteronePubChemApprovedNR1I3
PyrazinamidePubChemApprovedNR1I3

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