Details of the Drug

General Information of Drug (ID: DMWT905)

• Drug Name: Mefloquine
• Synonyms: Lariam; Mefloquin; Mefloquina; Mefloquinone; Mefloquinum; Mephloquine; Racemic mefloquine; Ro 215998; WR 142490; Lariam (Hydrochloride); Lariam (TN); Mefaquin (TN); Mefloquina [INN-Spanish]; Mefloquinum [INN-Latin]; RO 13-7224; RO 13-7225; Ro 21-5998; SPB-80406; WR-142490; Mefloquine (USAN/INN); Mefloquine [USAN:INN:BAN]; RTI1169-1-1; RTI1172-1-1; RTI1173-1-1; RTI1174-1-1; RTI1188-1-1; RTI1189-1-1; Ro 21-5998 (Hydrochloride); WR-142,490; WR-177,602; Ro-21-5998-001; Alpha-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol; Alpha-2-Piperidyl-2,8-bis(trifluoromethyl)quinoline-4-methanol; [2,8-bis(trifluoromethyl)quinolin-4-yl]-piperidin-2-ylmethanol; Erthro-.alpha.-[2-piperidyl]-2,8-bis[trifluoromethyl]-4-quinolinemethanol; (+)-(11R,2'S)-erythro-Mefloquine; (+)-Mefloquine; (+)-Threo-Mefloquine; (-)-(11S,2'R)-erythro-Mefloquine; (-)-Mefloquine; (-)-Threo-Mefloquine; (DL-erythro-alpha-2-Piperidyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol; (R)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2R)-piperidin-2-yl]methanol; (R)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2S)-piperidin-2-yl]methanol; (S)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2R)-piperidin-2-yl]methanol; (S)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2S)-piperidin-2-yl]methanol; (S)-[2,8-bis(trifluoromethyl)quinolin-4-yl][(2R)-piperidin-2-yl]methanol

Indication

Disease Entry	ICD 11	Status	REF
Malaria	1F40-1F45	Approved	[1]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Phase 2	[2]
Middle East Respiratory Syndrome (MERS)	1D64	Preclinical	[3]
Severe acute respiratory syndrome (SARS)	1D65	Preclinical	[3]
Progressive multifocal leukoencephalopathy	8A45.02	Investigative	[4]

• Therapeutic Class: Antimalarials
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 378.31
  Logarithm of the Partition Coefficient (xlogp); 3.6
  Rotatable Bond Count (rotbonds); 2
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 9
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [5]
  Bioavailability: 80% of drug becomes completely available to its intended biological destination(s) [6]
  Elimination: 9% of drug is excreted from urine in the unchanged form [5]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 47.2012 micromolar/kg/day [7]
• Chemical Identifiers:
  Formula: C17H16F6N2O
  IUPAC Name: [2,8-bis(trifluoromethyl)quinolin-4-yl]-piperidin-2-ylmethanol
  Canonical SMILES: C1CCNC(C1)C(C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O
  InChI: InChI=1S/C17H16F6N2O/c18-16(19,20)11-5-3-4-9-10(15(26)12-6-1-2-7-24-12)8-13(17(21,22)23)25-14(9)11/h3-5,8,12,15,24,26H,1-2,6-7H2
  InChIKey: XEEQGYMUWCZPDN-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 4046
  ChEBI ID: CHEBI:63681
  CAS Number: 49752-90-1
  DrugBank ID: DB00358
  TTD ID: D0GQ7K
  VARIDT ID: DR00623
  INTEDE ID: DR1016
  ACDINA ID: D00391
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Plasmodium 80S ribosome (Malaria 80S)	TTT28H3	NOUNIPROTAC	Binder	[8]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[9]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[10]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Mefloquine

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Lumefantrine	DM29GAD	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Lumefantrine.	Malaria [1F40-1F45]	[11]
Halofantrine	DMOMK1V	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Halofantrine.	Malaria [1F40-1F45]	[12]
Hydroxychloroquine	DMSIVND	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Hydroxychloroquine.	Malaria [1F40-1F45]	[13]

Coadministration of a Drug Treating the Disease Different from Mefloquine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Ivosidenib.	Acute myeloid leukaemia [2A60]	[14]
Arn-509	DMT81LZ	Moderate	Increased metabolism of Mefloquine caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[15]
Gilteritinib	DMTI0ZO	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Gilteritinib.	Acute myeloid leukaemia [2A60]	[16]
Mitotane	DMU1GX0	Moderate	Increased metabolism of Mefloquine caused by Mitotane mediated induction of CYP450 enzyme.	Adrenal cancer [2D11]	[15]
Metronidazole	DMTIVEN	Minor	Increased risk of prolong QT interval by the combination of Mefloquine and Metronidazole.	Amoebiasis [1A36]	[11]
Ivabradine	DM0L594	Major	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Ivabradine.	Angina pectoris [BA40]	[17]
Bepridil	DM0RKS4	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Bepridil.	Angina pectoris [BA40]	[18]
Dronedarone	DMA8FS5	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Dronedarone.	Angina pectoris [BA40]	[18]
Bedaquiline	DM3906J	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[19]
Levalbuterol	DM5YBO1	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Levalbuterol.	Asthma [CA23]	[20]
Terbutaline	DMD4381	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Terbutaline.	Asthma [CA23]	[21]
Pirbuterol	DMI5678	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Pirbuterol.	Asthma [CA23]	[21]
Salbutamol	DMN9CWF	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Salbutamol.	Asthma [CA23]	[20]
Formoterol	DMSOURV	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Formoterol.	Asthma [CA23]	[21]
Lisdexamfetamine	DM6W8V5	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Lisdexamfetamine.	Attention deficit hyperactivity disorder [6A05]	[17]
Ofloxacin	DM0VQN3	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Ofloxacin.	Bacterial infection [1A00-1C4Z]	[22]
Sulfamethoxazole	DMB08GE	Minor	Increased risk of prolong QT interval by the combination of Mefloquine and Sulfamethoxazole.	Bacterial infection [1A00-1C4Z]	[18]
Sparfloxacin	DMB4HCT	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Sparfloxacin.	Bacterial infection [1A00-1C4Z]	[22]
Gemifloxacin	DMHT34O	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Gemifloxacin.	Bacterial infection [1A00-1C4Z]	[22]
Norfloxacin	DMIZ6W2	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Norfloxacin.	Bacterial infection [1A00-1C4Z]	[22]
Levofloxacin	DMS60RB	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Levofloxacin.	Bacterial infection [1A00-1C4Z]	[22]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Mefloquine caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[15]
Loperamide	DMOJZQ9	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Loperamide.	Bowel habit change [ME05]	[23]
Eribulin	DM1DX4Q	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Eribulin.	Breast cancer [2C60-2C6Y]	[18]
Tucatinib	DMBESUA	Moderate	Decreased metabolism of Mefloquine caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[24]
Toremifene	DMQYUWG	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Toremifene.	Breast cancer [2C60-2C6Y]	[18]
Bosutinib	DMTI8YE	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Bosutinib.	Breast cancer [2C60-2C6Y]	[17]
Grepafloxacin	DMGLX0T	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Grepafloxacin.	Bronchitis [CA20]	[22]
Sotalol	DML60TN	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Sotalol.	Cardiac arrhythmia [BC9Z]	[18]
Secobarbital	DM14RF5	Moderate	Increased metabolism of Mefloquine caused by Secobarbital mediated induction of CYP450 enzyme.	Chronic insomnia [7A00]	[15]
PF-04449913	DMSB068	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[25]
Olodaterol	DM62B78	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Olodaterol.	Chronic obstructive pulmonary disease [CA22]	[21]
Vilanterol	DMF5EK1	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Vilanterol.	Chronic obstructive pulmonary disease [CA22]	[20]
Salmeterol	DMIEU69	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Salmeterol.	Chronic obstructive pulmonary disease [CA22]	[21]
Indacaterol	DMQJHR7	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Indacaterol.	Chronic obstructive pulmonary disease [CA22]	[21]
Arformoterol	DMYM974	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Arformoterol.	Chronic obstructive pulmonary disease [CA22]	[21]
Phenylbutazone	DMAYL0T	Moderate	Increased metabolism of Mefloquine caused by Phenylbutazone mediated induction of CYP450 enzyme.	Chronic pain [MG30]	[15]
Isoproterenol	DMK7MEY	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Isoproterenol.	Conduction disorder [BC63]	[20]
Propofol	DMB4OLE	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Propofol.	Corneal disease [9A76-9A78]	[26]
Sevoflurane	DMC9O43	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Sevoflurane.	Corneal disease [9A76-9A78]	[18]
Clofazimine	DMEBOFW	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Clofazimine.	Crohn disease [DD70]	[27]
Mifepristone	DMGZQEF	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Mifepristone.	Cushing syndrome [5A70]	[18]
Pasireotide	DMHM7JS	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Pasireotide.	Cushing syndrome [5A70]	[18]
Osilodrostat	DMIJC9X	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Osilodrostat.	Cushing syndrome [5A70]	[17]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Mefloquine caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[28]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Mefloquine caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[29]
Escitalopram	DMFK9HG	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Escitalopram.	Depression [6A70-6A7Z]	[18]
Trazodone	DMK1GBJ	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Trazodone.	Depression [6A70-6A7Z]	[30]
Mirtazapine	DML53ZJ	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Mirtazapine.	Depression [6A70-6A7Z]	[31]
Griseofulvin	DMK54YG	Moderate	Increased metabolism of Mefloquine caused by Griseofulvin mediated induction of CYP450 enzyme.	Dermatophytosis [1F28]	[15]
Tetrabenazine	DMYWQ0O	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Tetrabenazine.	Dissociative neurological symptom disorder [6B60]	[18]
Deutetrabenazine	DMUPFLI	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Deutetrabenazine.	Dystonic disorder [8A02]	[32]
Ingrezza	DMVPLNC	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Ingrezza.	Dystonic disorder [8A02]	[33]
Cenobamate	DM8KLU9	Moderate	Increased metabolism of Mefloquine caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[15]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Mefloquine caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[34]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Mefloquine caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[15]
Ketoconazole	DMPZI3Q	Major	Decreased metabolism of Mefloquine caused by Ketoconazole mediated inhibition of CYP450 enzyme.	Fungal infection [1F29-1F2F]	[15]
Cisapride	DMY7PED	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Cisapride.	Gastro-oesophageal reflux disease [DA22]	[18]
Sulfinpyrazone	DMEV954	Moderate	Increased metabolism of Mefloquine caused by Sulfinpyrazone mediated induction of CYP450 enzyme.	Gout [FA25]	[15]
Rifampin	DMA8J1G	Moderate	Increased metabolism of Mefloquine caused by Rifampin mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[15]
Rifapentine	DMCHV4I	Moderate	Increased metabolism of Mefloquine caused by Rifapentine mediated induction of CYP450 enzyme.	HIV-infected patients with tuberculosis [1B10-1B14]	[15]
Fostemsavir	DM50ILT	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[35]
Efavirenz	DMC0GSJ	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Efavirenz.	Human immunodeficiency virus disease [1C60-1C62]	[36]
Saquinavir	DMG814N	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Saquinavir.	Human immunodeficiency virus disease [1C60-1C62]	[37]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Mefloquine caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Lopinavir	DMITQS0	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Lopinavir.	Human immunodeficiency virus disease [1C60-1C62]	[18]
Darunavir	DMN3GCH	Moderate	Decreased metabolism of Mefloquine caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[38]
Conivaptan	DM1V329	Moderate	Decreased metabolism of Mefloquine caused by Conivaptan mediated inhibition of CYP450 enzyme.	Hypo-osmolality/hyponatraemia [5C72]	[39]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Mefloquine caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[40]
Amobarbital	DM0GQ8N	Moderate	Increased metabolism of Mefloquine caused by Amobarbital mediated induction of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[15]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Mefloquine and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[18]
Phenolphthalein	DM5SICT	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Phenolphthalein.	Irritable bowel syndrome [DD91]	[18]
Crizotinib	DM4F29C	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Crizotinib.	Lung cancer [2C25]	[41]
Ceritinib	DMB920Z	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Ceritinib.	Lung cancer [2C25]	[18]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Mefloquine caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[15]
Osimertinib	DMRJLAT	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Osimertinib.	Lung cancer [2C25]	[42]
Selpercatinib	DMZR15V	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Selpercatinib.	Lung cancer [2C25]	[17]
Inotuzumab ozogamicin	DMAC130	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Inotuzumab ozogamicin.	Malignant haematopoietic neoplasm [2B33]	[17]
Idelalisib	DM602WT	Moderate	Decreased metabolism of Mefloquine caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[43]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Mefloquine caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[44]
Arsenic trioxide	DM61TA4	Major	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Arsenic trioxide.	Mature B-cell lymphoma [2A85]	[45]
Vemurafenib	DM62UG5	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Vemurafenib.	Melanoma [2C30]	[18]
LGX818	DMNQXV8	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and LGX818.	Melanoma [2C30]	[46]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Mefloquine caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[15]
Propranolol	DM79NTF	Moderate	Increased risk of bradycardia by the combination of Mefloquine and Propranolol.	Migraine [8A80]	[15]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Mefloquine caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[47]
Panobinostat	DM58WKG	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Panobinostat.	Multiple myeloma [2A83]	[48]
Thalidomide	DM70BU5	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Thalidomide.	Multiple myeloma [2A83]	[11]
Siponimod	DM2R86O	Major	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Siponimod.	Multiple sclerosis [8A40]	[11]
Fingolimod	DM5JVAN	Major	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Fingolimod.	Multiple sclerosis [8A40]	[18]
Ozanimod	DMT6AM2	Major	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Ozanimod.	Multiple sclerosis [8A40]	[49]
Rifabutin	DM1YBHK	Moderate	Increased metabolism of Mefloquine caused by Rifabutin mediated induction of CYP450 enzyme.	Mycobacterium infection [1B10-1B21]	[15]
Fedratinib	DM4ZBK6	Moderate	Decreased metabolism of Mefloquine caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[17]
Nilotinib	DM7HXWT	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Nilotinib.	Myeloproliferative neoplasm [2A20]	[18]
Droperidol	DM0DXA8	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Droperidol.	Nausea/vomiting [MD90]	[18]
Metoclopramide	DMFA5MY	Minor	Altered absorption of Mefloquine due to GI dynamics variation caused by Metoclopramide.	Nausea/vomiting [MD90]	[50]
Dolasetron	DMMG26Z	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Dolasetron.	Nausea/vomiting [MD90]	[51]
Bupropion	DM5PCS7	Major	Increased risk of lowers seizure threshold by the combination of Mefloquine and Bupropion.	Nicotine use disorder [6C4A]	[52]
Entrectinib	DMMPTLH	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Entrectinib.	Non-small cell lung cancer [2C25]	[11]
Levomethadyl Acetate	DM06HG5	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Levomethadyl Acetate.	Opioid use disorder [6C43]	[17]
Pimavanserin	DMR7IVC	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Pimavanserin.	Parkinsonism [8A00]	[53]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Mefloquine caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[54]
Lindane	DMB8CNL	Moderate	Increased risk of lowers seizure threshold by the combination of Mefloquine and Lindane.	Pediculosis [1G00]	[55]
Famotidine	DMRL3AB	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Famotidine.	Peptic ulcer [DA61]	[11]
Macimorelin	DMQYJIR	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Macimorelin.	Pituitary gland disorder [5A60-5A61]	[56]
Lefamulin	DME6G97	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Lefamulin.	Pneumonia [CA40]	[57]
Lonafarnib	DMGM2Z6	Moderate	Decreased metabolism of Mefloquine caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[58]
Ritodrine	DM4V6RL	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Ritodrine.	Preterm labour/delivery [JB00]	[21]
Degarelix	DM3O8QY	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Degarelix.	Prostate cancer [2C82]	[17]
ABIRATERONE	DM8V75C	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and ABIRATERONE.	Prostate cancer [2C82]	[17]
Nilutamide	DMFN07X	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Nilutamide.	Prostate cancer [2C82]	[17]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Mefloquine caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[15]
Flutamide	DMK0O7U	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Flutamide.	Prostate cancer [2C82]	[17]
Relugolix	DMK7IWL	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Relugolix.	Prostate cancer [2C82]	[17]
Bicalutamide	DMZMSPF	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Bicalutamide.	Prostate cancer [2C82]	[17]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Mefloquine and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[59]
Sorafenib	DMS8IFC	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Sorafenib.	Renal cell carcinoma [2C90]	[18]
Gatifloxacin	DMSL679	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Gatifloxacin.	Respiratory infection [CA07-CA4Z]	[60]
Dexamethasone	DMMWZET	Moderate	Increased metabolism of Mefloquine caused by Dexamethasone mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[15]
Nafcillin	DMN9RPO	Moderate	Increased metabolism of Mefloquine caused by Nafcillin mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[15]
Quetiapine	DM1N62C	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Quetiapine.	Schizophrenia [6A20]	[18]
Mesoridazine	DM2ZGAN	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Mesoridazine.	Schizophrenia [6A20]	[18]
Thioridazine	DM35M8J	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Thioridazine.	Schizophrenia [6A20]	[18]
Iloperidone	DM6AUFY	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Iloperidone.	Schizophrenia [6A20]	[18]
Haloperidol	DM96SE0	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Haloperidol.	Schizophrenia [6A20]	[18]
Clozapine	DMFC71L	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Clozapine.	Schizophrenia [6A20]	[18]
Amisulpride	DMSJVAM	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Amisulpride.	Schizophrenia [6A20]	[61]
Asenapine	DMSQZE2	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Asenapine.	Schizophrenia [6A20]	[18]
Pimozide	DMW83TP	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Pimozide.	Schizophrenia [6A20]	[17]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Mefloquine caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[17]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Mefloquine caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[11]
Vandetanib	DMRICNP	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Vandetanib.	Solid tumour/cancer [2A00-2F9Z]	[18]
Triptorelin	DMTK4LS	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Triptorelin.	Solid tumour/cancer [2A00-2F9Z]	[17]
Pitolisant	DM8RFNJ	Moderate	Increased risk of prolong QT interval by the combination of Mefloquine and Pitolisant.	Somnolence [MG42]	[17]
Adenosine	DMM2NSK	Moderate	Increased risk of ventricular arrhythmias by the combination of Mefloquine and Adenosine.	Supraventricular tachyarrhythmia [BC81]	[18]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Mefloquine caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[62]
Cabozantinib	DMIYDT4	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Cabozantinib.	Thyroid cancer [2D10]	[17]
Papaverine	DMCA9QP	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Papaverine.	Tonus and reflex abnormality [MB47]	[63]
Sirolimus	DMGW1ID	Moderate	Increased plasma concentrations of Mefloquine and Sirolimus due to competitive inhibition of the same metabolic pathway.	Transplant rejection [NE84]	[59]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Mefloquine caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[15]
Procainamide	DMNMXR8	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Procainamide.	Ventricular tachyarrhythmia [BC71]	[18]
Amiodarone	DMUTEX3	Major	Increased risk of prolong QT interval by the combination of Mefloquine and Amiodarone.	Ventricular tachyarrhythmia [BC71]	[18]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Calcium alginate	E00576	44630049	Disintegrant; Emulsifying agent; Modified-release agent; Viscosity-controlling agent
Crospovidone	E00626	Not Available	Disintegrant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Poloxamer 188	E00645	Not Available	Emulsifying agent; Solubilizing agent; Surfactant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Mefloquine 250 mg tablet	250 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (NDA) 019578
• [2] ClinicalTrials.gov (NCT04347031) An Open Randomized Study of the Effectiveness of Mefloquine for the Treatment of Patients With COVID19. U.S. National Institutes of Health.
• [3] Repurposing of clinically developed drugs for treatment of Middle East respiratory syndrome coronavirus infection. Antimicrob Agents Chemother. 2014 Aug;58(8):4885-93.
• [4] Mefloquine FDA Label
• [5] BDDCS applied to over 900 drugs
• [6] Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
• [7] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [8] An ultrastructural study of the effects of mefloquine on malaria parasites. Am J Trop Med Hyg. 1987 Jan;36(1):9-14.
• [9] Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clin Pharmacol Ther. 2004 Jan;75(1):13-33.
• [10] Effect of rifampin on plasma concentrations of mefloquine in healthy volunteers. J Pharm Pharmacol. 2000 Oct;52(10):1265-9.
• [11] Cerner Multum, Inc. "Australian Product Information.".
• [12] Abernethy DR, Wesche DL, Barbey JT, et al. "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol 51 (2001): 231-7. [PMID: 11298069]
• [13] Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259]
• [14] Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
• [15] Product Information. Lariam (mefloquine). Roche Laboratories, Nutley, NJ.
• [16] Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
• [17] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [18] Canadian Pharmacists Association.
• [19] Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
• [20] Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
• [21] Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
• [22] Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074]
• [23] Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747]
• [24] Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
• [25] Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [26] Hanci V, Aydin M, Yurtlu BS, et.al "Anesthesia induction with sevoflurane and propofol: evaluation of P-wave dispersion, QT and corrected QT intervals." Kaohsiung J Med Sci 26 (2010): 470-7. [PMID: 20837343]
• [27] Product Information. Lamprene (clofazimine). Novartis Pharmaceuticals, East Hanover, NJ.
• [28] Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
• [29] Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
• [30] Antonelli D, Atar S, Freedberg NA, Rosenfeld T "Torsade de pointes in patients on chronic amiodarone treatment: contributing factors and drug interactions." Isr Med Assoc J 7 (2005): 163-5. [PMID: 15792261]
• [31] Product Information. Remeron (mirtazapine). Organon, West Orange, NJ.
• [32] Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
• [33] Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
• [34] EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
• [35] Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
• [36] Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE.
• [37] Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475]
• [38] Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ.
• [39] Product Information. Vaprisol (conivaptan). Cumberland Pharmaceuticals Inc, Nashville, TN.
• [40] Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
• [41] Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [42] Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
• [43] Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
• [44] Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
• [45] Ohnishi K, Yoshida H, Shigeno K, et al. "Prolongation of the QT interval and ventricular tachycardia in patients treated with arsenic trioxide for acute promyelocytic leukemia." Ann Intern Med 133 (2000): 881-5. [PMID: 11103058]
• [46] Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO.
• [47] Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ.
• [48] Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
• [49] Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
• [50] Bangchang KN, Karbwang J, Bunnag D, et al "The effect of metoclopramide on mefloquine pharmacokinetics." Br J Clin Pharmacol 32 (1991): 640-1. [PMID: 1954082]
• [51] Product Information. Anzemet (dolasetron). Hoechst Marion-Roussel Inc, Kansas City, MO.
• [52] Product Information. Wellbutrin XL (buPROPion). GlaxoSmithKline, Philadelphia, PA.
• [53] Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
• [54] Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
• [55] Matsuoka LY "Convulsions following application of gamma benzene hexachloride." J Am Acad Dermatol 5 (1981): 98-9. [PMID: 6168673]
• [56] Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
• [57] Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
• [58] Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
• [59] Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
• [60] Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399]
• [61] Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.
• [62] Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
• [63] Goto M, Sato M, Kitzazawa H, et.al "Papaverine-induced QT interval prolongation and ventricular fibrillation in a patient with a history of drug-induced QT prolongation." Intern Med 53 (2014): 1629-31. [PMID: 25088875]