Drug Information
| Drug General Information | Top | |||
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| Drug ID |
D0GQ7K
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| Former ID |
DAP001310
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| Drug Name |
Mefloquine
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| 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
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| Drug Type |
Small molecular drug
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| Indication | Malaria [ICD-11: 1F40-1F45; ICD-10: B50-B64, B54] | Approved | [1], [2] | |
| Therapeutic Class |
Antimalarials
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| Company |
Hoffmann-La Roche pharmaceutical company
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| Structure |
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Download2D MOL |
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| Formula |
C17H16F6N2O
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| Canonical SMILES |
C1CCNC(C1)C(C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O
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| 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
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| InChIKey |
XEEQGYMUWCZPDN-UHFFFAOYSA-N
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| CAS Number |
CAS 49752-90-1
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| PubChem Compound ID | ||||
| PubChem Substance ID |
9835, 603007, 8176741, 14877790, 26755467, 29216385, 34706437, 47206659, 49681220, 50042965, 50071333, 51051233, 53788688, 56310966, 56313823, 57312460, 85154870, 93166754, 93167184, 103446060, 104040016, 104335053, 124892361, 135004437, 135240375, 135611150, 135727482, 137236385, 140239432, 175269604, 178101069, 179116766, 223533437, 223712526, 226410988, 243866056, 252401319, 252655885
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| ChEBI ID |
CHEBI:63681
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| ADReCS Drug ID | BADD_D01369 ; BADD_D01370 | |||
| SuperDrug ATC ID |
P01BC02
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| SuperDrug CAS ID |
cas=053230107
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| Interaction between the Drug and Microbe | Top | |||
|---|---|---|---|---|
| The Metabolism of Drug Affected by Studied Microbe(s) | ||||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Eggerthellales | ||||
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Studied Microbe: Eggerthella lenta ATCC 25559
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[3] | |||
| Hierarchy | ||||
| Experimental Method | High-throughput screening | |||
| Description | Mefloquine can be metabolized by Eggerthella lenta ATCC 25559 (log2FC = -0.995; p = 0.012). | |||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Enterobacterales | ||||
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Studied Microbe: Escherichia coli BW25113
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|
[3] | |||
| Hierarchy | ||||
| Experimental Method | High-throughput screening | |||
| Description | Mefloquine can be metabolized by Escherichia coli BW25113 (log2FC = -0.977; p = 0.034). | |||
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Studied Microbe: Providencia alcalifaciens DSM 30120
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|
[3] | |||
| Hierarchy | ||||
| Experimental Method | High-throughput screening | |||
| Description | Mefloquine can be metabolized by Providencia alcalifaciens DSM 30120 (log2FC = -0.464; p = 0.035). | |||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Eubacteriales | ||||
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Studied Microbe: Roseburia intestinalis L1-82
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|
[3] | |||
| Hierarchy | ||||
| Experimental Method | High-throughput screening | |||
| Description | Mefloquine can be metabolized by Roseburia intestinalis L1-82 (log2FC = -0.658; p = 0.016). | |||
| The Abundace of Studied Microbe(s) Regulated by Drug | ||||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Bacteroidales | ||||
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Studied Microbe: Bacteroides fragilis nontoxigenic
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Bacteroides fragilis nontoxigenic was decreased by Mefloquine hydrochloride (adjusted p-values: 8.62E-03). | |||
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Studied Microbe: Bacteroides thetaiotaomicron
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Bacteroides thetaiotaomicron was decreased by Mefloquine hydrochloride (adjusted p-values: 7.50E-03). | |||
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Studied Microbe: Bacteroides uniformis
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Bacteroides uniformis was decreased by Mefloquine hydrochloride (adjusted p-values: 7.71E-03). | |||
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Studied Microbe: Bacteroides vulgatus
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Bacteroides vulgatus was decreased by Mefloquine hydrochloride (adjusted p-values: 5.81E-03). | |||
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Studied Microbe: Odoribacter splanchnicus
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|
[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Odoribacter splanchnicus was decreased by Mefloquine hydrochloride (adjusted p-values: 7.33E-04). | |||
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Studied Microbe: Parabacteroides distasonis
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Parabacteroides distasonis was decreased by Mefloquine hydrochloride (adjusted p-values: 2.02E-06). | |||
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Studied Microbe: Prevotella copri
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Prevotella copri was decreased by Mefloquine hydrochloride (adjusted p-values: 4.35E-05). | |||
| The Order in the Taxonomic Hierarchy of the following Microbe(s): Eubacteriales | ||||
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Studied Microbe: Coprococcus comes
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|
[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Coprococcus comes was decreased by Mefloquine hydrochloride (adjusted p-values: 2.96E-04). | |||
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Studied Microbe: Dorea formicigenerans
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Dorea formicigenerans was decreased by Mefloquine hydrochloride (adjusted p-values: 3.61E-04). | |||
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Studied Microbe: Eubacterium rectale
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Eubacterium rectale was decreased by Mefloquine hydrochloride (adjusted p-values: 2.77E-03). | |||
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Studied Microbe: Roseburia hominis
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Roseburia hominis was decreased by Mefloquine hydrochloride (adjusted p-values: 1.03E-04). | |||
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Studied Microbe: Roseburia intestinalis
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Roseburia intestinalis was decreased by Mefloquine hydrochloride (adjusted p-values: 6.13E-04). | |||
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Studied Microbe: Ruminococcus gnavus
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[4] | |||
| Hierarchy | ||||
| Abundance Change | Decrease | |||
| Experiment Method | High-throughput screening | |||
| Description | The abundance of Ruminococcus gnavus was decreased by Mefloquine hydrochloride (adjusted p-values: 4.74E-04). | |||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Plasmodium 80S ribosome (Malaria 80S) | Target Info | Binder | [5] |
| References | Top | |||
|---|---|---|---|---|
| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4252). | |||
| REF 2 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | |||
| REF 3 | Mapping human microbiome drug metabolism by gut bacteria and their genes. Nature. 2019 Jun;570(7762):462-467. | |||
| REF 4 | Extensive impact of non-antibiotic drugs on human gut bacteria. Nature. 2018 Mar 29;555(7698):623-628. | |||
| REF 5 | An ultrastructural study of the effects of mefloquine on malaria parasites. Am J Trop Med Hyg. 1987 Jan;36(1):9-14. | |||
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