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Mefloquine

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Also known as GNF-Pf-5544MefloquinaMefaquinNSC-758233RO-215998WR 142,490melfoquinerac-mefloquineSID11112778SID26748684SID29216385SID174006936MEFLOQUINE HYDROCHLORIDE

Summary

Mefloquine (CHEMBL416956) is an approved small molecule (ATC P01BC02) targeting ADORA1 and ADORA2A; indicated across 9 conditions including malaria and plasmodium falciparum malaria.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: P01BC02
  • Targets: 2 (ADORA1, ADORA2A)
  • Indications: 9 conditions
  • Clinical trials: 34
  • Chemistry: 378.31 Da · C17H16F6N2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL416956
NameMefloquine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4046
ChEBICHEBI:63681
ATCP01BC02
Molecular formulaC17H16F6N2O
Molecular weight378.31
InChIKeyXEEQGYMUWCZPDN-UHFFFAOYSA-N

SMILES: C1CCNC(C1)C(C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O

IUPAC name: [2,8-bis(trifluoromethyl)quinolin-4-yl]-piperidin-2-ylmethanol

ChEBI definition: An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.

Also known as: GNF-Pf-5544, Mefloquina, Mefloquine, Mefaquin, NSC-758233, RO-215998, WR 142,490, mefloquine, melfoquine, rac-mefloquine, SID11112778, SID26748684

Parent form; salt/anhydrous children: CHEMBL535650

Patent coverage: 3,911 distinct patent families (15,549 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 15,528 (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

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
ADORA1A1 receptorAntagonist6.170.3%P30542
ADORA2AA2A receptorAntagonist6.980.4%P29274
Plasmodium falciparum purine nucleoside phosphorylase5.23
VRAC

Broader ChEMBL bioactivity targets: 35 (assay-derived). Sample: Lysine-specific demethylase 4E, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Vasopressin V2 receptor, 5-hydroxytryptamine receptor 2B, Thyrotropin receptor, 5-hydroxytryptamine receptor 1A, Cannabinoid receptor 1, Sodium-dependent noradrenaline transporter, 5-hydroxytryptamine receptor 2A, Adenosine receptor A1, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Prostaglandin G/H synthase 2, Histamine H1 receptor, Mu-type opioid receptor, D(3) dopamine receptor, Kappa-type opioid receptor, Sodium-dependent dopamine transporter, Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 40 potent at pChembl ≥ 5 of 89 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
SLC6A47.05AC5089.8nMCHEMBL_ACT_25150686
SLC6A46.77AC50171nMCHEMBL_ACT_25149894
ADORA2A6.68AC50210nMCHEMBL_ACT_25152831
ADORA2A6.65AC50225.8nMCHEMBL_ACT_25152032
ADORA2A6.31AC50490.5nMCHEMBL_ACT_25152031
Q018276.26AC50547.7nMCHEMBL_ACT_25197393
ADORA2A5.95AC501114nMCHEMBL_ACT_25152218
ADORA15.83AC501465nMCHEMBL_ACT_25133353
KCNH25.8AC501590nMCHEMBL_ACT_25118374
ADORA15.7AC501990nMCHEMBL_ACT_25132567
ADORA2A5.66AC502202nMCHEMBL_ACT_25152219
GLRA15.6EC502500nMCHEMBL_ACT_15241392
KCNH25.58IC502600nMCHEMBL_ACT_1449656
OPRK15.43AC503728nMCHEMBL_ACT_25129019
KCNH25.34AC504587nMCHEMBL_ACT_25117184
HTR2A5.34AC504526nMCHEMBL_ACT_25173737
ADORA15.28AC505200nMCHEMBL_ACT_25132568
KCNH25.26IC505495nMCHEMBL_ACT_5218916
KCNH25.25IC505623nMCHEMBL_ACT_1523705
KCNH25.25IC505623nMCHEMBL_ACT_2358268
HTR2A5.24AC505797nMCHEMBL_ACT_25225903
OPRK15.22AC505987nMCHEMBL_ACT_25129761
KCNH25.21AC506114nMCHEMBL_ACT_25117471
SLC6A25.21AC506220nMCHEMBL_ACT_25145354
KCNH25.2AC506300nMCHEMBL_ACT_25117183
CYP1A25.2AC506310nMCHEMBL_ACT_6051346
ADORA35.15AC507075nMCHEMBL_ACT_25134567
Q639215.14AC507245nMCHEMBL_ACT_25174137
HTR2A5.09AC508113nMCHEMBL_ACT_25173459
KCNH25.08AC508385nMCHEMBL_ACT_25117472
ADORA35.05AC508832nMCHEMBL_ACT_25133758
HTR2A5.05AC509000nMCHEMBL_ACT_25224756
LMNA5.05Potency8912nMCHEMBL_ACT_3649931
HTR1A5.04AC509200nMCHEMBL_ACT_25216587
SLC6A25.02AC509546nMCHEMBL_ACT_25144557
HTR1A5.02AC509500nMCHEMBL_ACT_25217365
HTR2A5AC5010000nMCHEMBL_ACT_25225904
TP535Potency10000nMCHEMBL_ACT_4862176
CYP2D65Potency10000nMCHEMBL_ACT_4981991
CYP2D65AC5010000nMCHEMBL_ACT_6010980

Target pathways

Aggregated over 2 target gene(s): ADORA1, ADORA2A.

Top Reactome pathways

16 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction2ADORA1, ADORA2A
Signaling by GPCR2ADORA1, ADORA2A
Class A/1 (Rhodopsin-like receptors)2ADORA1, ADORA2A
GPCR downstream signalling2ADORA1, ADORA2A
Adenosine P1 receptors2ADORA1, ADORA2A
Nucleotide-like (purinergic) receptors2ADORA1, ADORA2A
GPCR ligand binding2ADORA1, ADORA2A
Signaling by NTRKs1ADORA2A
Activation of TRKA receptors1ADORA2A
NGF-independant TRKA activation1ADORA2A
Signaling by NTRK1 (TRKA)1ADORA2A
Metabolism of proteins1ADORA2A
G alpha (s) signalling events1ADORA2A
G alpha (i) signalling events1ADORA1
Surfactant metabolism1ADORA2A
Signaling by Receptor Tyrosine Kinases1ADORA2A

Dominant GO biological processes

GO termTargets
phagocytosis2
inflammatory response2
signal transduction2
G protein-coupled receptor signaling pathway2
cell-cell signaling2
negative regulation of cell population proliferation2
response to purine-containing compound2
vasodilation2
excitatory postsynaptic potential2
apoptotic signaling pathway2
G protein-coupled adenosine receptor signaling pathway2
negative regulation of inflammatory response2
temperature homeostasis1
response to hypoxia1
regulation of respiratory gaseous exchange by nervous system process1

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
malaria4MONDO:0005136EFO:0001068

8 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
Plasmodium falciparum malaria3MONDO:0005920EFO:0007444
urinary schistosomiasis3MONDO:0006001EFO:0007530
viral pneumonia2MONDO:0006012EFO:0007541
respiratory failure2MONDO:0021113EFO:0009686
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
progressive multifocal leukoencephalopathy1MONDO:0016318EFO:0007455
gliosarcoma1MONDO:0016681EFO:1001465
glioblastoma1MONDO:0018177EFO:0000519

Clinical trials

Total trials: 34.

Phase distribution

PhaseTrials
Not specified9
PHASE37
PHASE45
PHASE2/PHASE35
PHASE14
PHASE23
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00978172PHASE4COMPLETEDSafety and Efficacy Study of Artesunate and Mefloquin in Children With Uncomplicated Malaria
NCT01976780PHASE4COMPLETEDIn Vivo and In Vitro Efficacy of Artemisinin Combination Therapy
NCT02084602PHASE4COMPLETEDAssessment of Artesunate/Mefloquine in the Peruvian Amazon
NCT02324738PHASE4COMPLETEDPharmacokinetic and Pharmacodynamic Study of Mefloquine and Dihydroartemisinin-Piperaquine in Healthy Subjects
NCT02653898PHASE4UNKNOWNMalaria Elimination Pilot Study in Military Forces in Cambodia
NCT00082576PHASE2/PHASE3COMPLETEDAzithromycin Plus Chloroquine Versus Mefloquine for the Treatment of Uncomplicated Malaria in Africa
NCT00158574PHASE2/PHASE3COMPLETEDKilimanjaro IPTi Drug Options Trial
NCT00274235PHASE3COMPLETEDIntermittent Preventive Treatment During Pregnancy in Benin
NCT00367653PHASE3COMPLETEDAzithromycin Plus Chloroquine Versus Mefloquine In the Treatment of Uncomplicated P. Falciparum Malaria.
NCT00373607PHASE3COMPLETEDEfficacy and Safety of Dihydroartemisinin/Piperaquine (Artekin®) for the Treatment of Uncomplicated Malaria in Peru
NCT00936767PHASE2/PHASE3WITHDRAWNArtemisone for the Treatment of Uncomplicated Falciparum Malaria in Western Cambodia
NCT00970879PHASE3COMPLETEDPrevention of Pregnancy-associated Malaria in HIV-infected Women: Cotrimoxazole Prophylaxis Versus Mefloquine
NCT01082718PHASE2/PHASE3WITHDRAWNPharmacokinetics of Mefloquine-Artesunate in Pregnant Women With Uncomplicated Plasmodium Falciparum Infection
NCT02974348PHASE3COMPLETEDAntimalaria Drugs Susceptibility Testing for an Effective Management of Infected Patients in Sub-Sahara Africa
NCT03452475PHASE3COMPLETEDComparison of Arterolane-piperaquine Versus Arterolane-piperaquine+Mefloquine Versus Artemether-lumefantrine in Kenyan Children
NCT03893097PHASE3COMPLETEDEvaluation of Artesunate-mefloquine as a Novel Alternative Treatment for Schistosomiasis in African Children
NCT04347031PHASE2/PHASE3COMPLETEDA Study of the Effectiveness of an Off Label Mefloquine Use for the Treatment of Patients With COVID19
NCT00746941PHASE1/PHASE2TERMINATEDStudy to Explore the Effect of Mefloquine in Participants With Progressive Multifocal Leukoencephalopathy (PML)
NCT01132248PHASE2COMPLETEDActivity of Mefloquine Against Urinary Schistosomiasis
NCT02488902PHASE2COMPLETEDA Randomized, Double-blind, Placebo-controlled Evaluation of Increasing Doses of Weekly Tafenoquine for Chemosuppression of Plasmodium Falciparum
NCT02488980PHASE2COMPLETEDAn Evaluation of Weekly Tafenoquine
NCT00931697PHASE1COMPLETEDStudy to Investigate the Safety, Tolerability and Pharmacokinetics of AD 452 [(+)-Mefloquine] Compared With Racemic Mefloquine
NCT01430351PHASE1TERMINATEDTemozolomide, Memantine Hydrochloride, Mefloquine, and Metformin Hydrochloride in Treating Patients With Glioblastoma Multiforme After Radiation Therapy
NCT02524444PHASE1COMPLETEDA Comparative Study of Mefloquine and S-P as Prophylaxis Against Malaria in Pregnant HIV + Patients
NCT02612545PHASE1COMPLETEDEfficacy, Safety, and Tolerability of Dihydroartemisinin-piperaquine + Mefloquine Compared to Dihydroartemisinin-piperaquine or Artesunate-mefloquine in Patients With Uncomplicated Falciparum Malaria in Cambodia
NCT00127998Not specifiedCOMPLETEDAntimalarial Drug Resistance in Mali
NCT00373048Not specifiedCOMPLETEDMefloquine Prophylaxis in HIV-1 Individuals: a Randomized Placebo-controlled Trial
NCT00493363Not specifiedCOMPLETEDClinical Investigation of In-vivo Susceptibility of P.Falciparum to Artesunate in Western Cambodia
NCT00499876Not specifiedCOMPLETEDThe Effect of Malaria on Disease Progression of HIV/AIDS
NCT00761020Not specifiedCOMPLETEDMerozoite Surface Protein 1 Antibody Response in Asymptomatic Human Malaria Infection
NCT00811421Not specifiedCOMPLETEDEvaluation of Alternative Antimalarial Drugs for Malaria in Pregnancy
NCT01422954Not specifiedCOMPLETEDImmunization With Plasmodium Falciparum Sporozoites Under Chloroquine Versus Mefloquine Prophylaxis
NCT01640587Not specifiedTERMINATEDCompare the Effectiveness Between Existing Treatment and New Treatment
NCT01659281Not specifiedCOMPLETEDEfficacy of Artesunate-Mefloquine Combination Therapy in Trat Province, Thailand

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 8 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.

121 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
ADENOSINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
AMPHETAMINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
CAFFEINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
CLOFARABINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
CLOTRIMAZOLEChEMBLPhase 4 (approved)ADORA1, ADORA2A
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)ADORA1, ADORA2A
ECONAZOLEChEMBLPhase 4 (approved)ADORA1, ADORA2A
EPALRESTATChEMBLPhase 4 (approved)ADORA1, ADORA2A
FEDRATINIBChEMBLPhase 4 (approved)ADORA1, ADORA2A
IBUDILASTChEMBLPhase 4 (approved)ADORA1, ADORA2A
ISTRADEFYLLINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
MICONAZOLEChEMBLPhase 4 (approved)ADORA1, ADORA2A
NEVIRAPINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
NIFEDIPINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
NIMESULIDEChEMBLPhase 4 (approved)ADORA1, ADORA2A
NISOLDIPINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
NITAZOXANIDEChEMBLPhase 4 (approved)ADORA1, ADORA2A
PENTOSTATINChEMBLPhase 4 (approved)ADORA1, ADORA2A
PYRVINIUMChEMBLPhase 4 (approved)ADORA1, ADORA2A
REGADENOSONChEMBLPhase 4 (approved)ADORA1, ADORA2A
RIFAMPINChEMBLPhase 4 (approved)ADORA1, ADORA2A
RIFAXIMINChEMBLPhase 4 (approved)ADORA1, ADORA2A
SILDENAFILChEMBLPhase 4 (approved)ADORA1, ADORA2A
SUNITINIBChEMBLPhase 4 (approved)ADORA1, ADORA2A
TAMOXIFENChEMBLPhase 4 (approved)ADORA1, ADORA2A
THEOPHYLLINEChEMBLPhase 4 (approved)ADORA1, ADORA2A
APADENOSONChEMBLPhase 3ADORA1, ADORA2A
BINODENOSONChEMBLPhase 3ADORA1, ADORA2A
DIACEREINChEMBLPhase 3ADORA1, ADORA2A
NAMODENOSONChEMBLPhase 3ADORA1, ADORA2A
PRELADENANTChEMBLPhase 3ADORA1, ADORA2A
ROLOFYLLINEChEMBLPhase 3ADORA1, ADORA2A
TONAPOFYLLINEChEMBLPhase 3ADORA1, ADORA2A
TOZADENANTChEMBLPhase 3ADORA1, ADORA2A
TRABODENOSONChEMBLPhase 3ADORA1, ADORA2A
CIFORADENANTChEMBLPhase 2ADORA1, ADORA2A
DERENOFYLLINEChEMBLPhase 2ADORA1, ADORA2A
ENPROFYLLINEChEMBLPhase 2ADORA1, ADORA2A
ETRUMADENANTChEMBLPhase 2ADORA1, ADORA2A
GENISTEINChEMBLPhase 2ADORA1, ADORA2A
IMARADENANTChEMBLPhase 2ADORA1, ADORA2A
METRIFUDILChEMBLPhase 2ADORA1, ADORA2A
NOCODAZOLEChEMBLPhase 2ADORA1, ADORA2A
SONEDENOSONChEMBLPhase 2ADORA1, ADORA2A
TECADENOSONChEMBLPhase 2ADORA1, ADORA2A
TOFIMILASTChEMBLPhase 2ADORA1, ADORA2A
VIPADENANTChEMBLPhase 2ADORA1, ADORA2A
AfatinibPubChemApprovedADORA1, ADORA2A
ApixabanPubChemApprovedADORA1, ADORA2A
BinimetinibPubChemApprovedADORA1, ADORA2A
BosentanPubChemApprovedADORA1, ADORA2A
chenodiolPubChemApprovedADORA1, ADORA2A
DihydroergotaminePubChemApprovedADORA1, ADORA2A
FidaxomicinPubChemApprovedADORA1, ADORA2A
FulvestrantPubChemApprovedADORA1, ADORA2A
ImipenemPubChemApprovedADORA1, ADORA2A
LinagliptinPubChemApprovedADORA1, ADORA2A
PropoxyphenePubChemApprovedADORA1, ADORA2A
PyrazinamidePubChemApprovedADORA1, ADORA2A
TafamidisPubChemApprovedADORA1, ADORA2A
ALLOPURINOLChEMBLPhase 4 (approved)ADORA2A
ALPIDEMChEMBLPhase 4 (approved)ADORA1
AMILORIDEChEMBLPhase 4 (approved)ADORA2A
BALSALAZIDEChEMBLPhase 4 (approved)ADORA2A
BENZIODARONEChEMBLPhase 4 (approved)ADORA1
BITHIONOLChEMBLPhase 4 (approved)ADORA2A
BROMFENACChEMBLPhase 4 (approved)ADORA1
DANTROLENEChEMBLPhase 4 (approved)ADORA1
DAUNORUBICINChEMBLPhase 4 (approved)ADORA2A
DOXYCYCLINEChEMBLPhase 4 (approved)ADORA1
ENASIDENIBChEMBLPhase 4 (approved)ADORA1
ERLOTINIBChEMBLPhase 4 (approved)ADORA2A
ETHINYL ESTRADIOLChEMBLPhase 4 (approved)ADORA2A
ETRAVIRINEChEMBLPhase 4 (approved)ADORA1
GENTIAN VIOLETChEMBLPhase 4 (approved)ADORA2A
GLAFENINEChEMBLPhase 4 (approved)ADORA2A
HALOPROGINChEMBLPhase 4 (approved)ADORA1
HEXACHLOROPHENEChEMBLPhase 4 (approved)ADORA2A
HYDROXOCOBALAMINChEMBLPhase 4 (approved)ADORA1
IBRUTINIBChEMBLPhase 4 (approved)ADORA2A
IMIQUIMODChEMBLPhase 4 (approved)ADORA2A
INDOCYANINE GREEN ACID FORMChEMBLPhase 4 (approved)ADORA1
LANSOPRAZOLEChEMBLPhase 4 (approved)ADORA1
LIOTHYRONINEChEMBLPhase 4 (approved)ADORA1
LOVASTATINChEMBLPhase 4 (approved)ADORA1
MALATHIONChEMBLPhase 4 (approved)ADORA1
NINTEDANIBChEMBLPhase 4 (approved)ADORA2A
OLAPARIBChEMBLPhase 4 (approved)ADORA1
OSIMERTINIBChEMBLPhase 4 (approved)ADORA2A
PEXIDARTINIBChEMBLPhase 4 (approved)ADORA1
PHENAZOPYRIDINEChEMBLPhase 4 (approved)ADORA1
PRANLUKASTChEMBLPhase 4 (approved)ADORA1
RABEPRAZOLEChEMBLPhase 4 (approved)ADORA1
RALOXIFENEChEMBLPhase 4 (approved)ADORA2A
RIBAVIRINChEMBLPhase 4 (approved)ADORA1
THIOTHIXENEChEMBLPhase 4 (approved)ADORA2A
TOLCAPONEChEMBLPhase 4 (approved)ADORA1
TRIOXSALENChEMBLPhase 4 (approved)ADORA2A
VALDECOXIBChEMBLPhase 4 (approved)ADORA1
VARDENAFILChEMBLPhase 4 (approved)ADORA1

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
v1.1.4
BioBTree
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Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot