Details of the Drug
General Information of Drug (ID: DMWT905)
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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Indication |
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Therapeutic Class |
Antimalarials
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Drug Type |
Small molecular drug
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Structure | ||||||||||||||||||||
3D MOL | 2D MOL | |||||||||||||||||||
#Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 378.31 | ||||||||||||||||||
Topological Polar Surface Area (xlogp) | 3.6 | |||||||||||||||||||
Rotatable Bond Count (rotbonds) | 2 | |||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 2 | |||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 9 | |||||||||||||||||||
ADMET Property |
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Chemical Identifiers |
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Cross-matching ID | ||||||||||||||||||||
Molecular Interaction Atlas of This Drug
Drug Therapeutic Target (DTT) |
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Drug Transporter (DTP) |
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Drug-Metabolizing Enzyme (DME) |
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Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Same Disease as Mefloquine
Coadministration of a Drug Treating the Disease Different from Mefloquine (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
References
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). | ||||
---|---|---|---|---|---|
2 | The fight against drug-resistant malaria: novel plasmodial targets and antimalarial drugs. Curr Med Chem. 2008;15(2):161-71. | ||||
3 | BDDCS applied to over 900 drugs | ||||
4 | Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches | ||||
5 | 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 | ||||
6 | An ultrastructural study of the effects of mefloquine on malaria parasites. Am J Trop Med Hyg. 1987 Jan;36(1):9-14. | ||||
7 | Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clin Pharmacol Ther. 2004 Jan;75(1):13-33. | ||||
8 | Effect of rifampin on plasma concentrations of mefloquine in healthy volunteers. J Pharm Pharmacol. 2000 Oct;52(10):1265-9. | ||||
9 | Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65. | ||||
10 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
11 | Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75. | ||||
12 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
13 | Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772. | ||||
14 | Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98. | ||||
15 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
16 | The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76. | ||||
17 | Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. | ||||
18 | Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007. | ||||
19 | MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. | ||||
20 | Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64. | ||||
21 | Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31. | ||||
22 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. | ||||
23 | Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. | ||||
24 | Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50. | ||||
25 | Cerner Multum, Inc. "Australian Product Information.". | ||||
26 | 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] | ||||
27 | Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259] | ||||
28 | Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA. | ||||
29 | Product Information. Lariam (mefloquine). Roche Laboratories, Nutley, NJ. | ||||
30 | Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL. | ||||
31 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
32 | Canadian Pharmacists Association. | ||||
33 | Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ. | ||||
34 | Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
35 | Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176] | ||||
36 | Ball P "Quinolone-induced QT interval prolongation: a not-so-unexpected class effect." J Antimicrob Chemother 45 (2000): 557-9. [PMID: 10797074] | ||||
37 | Eggleston W, Clark KH, Marraffa JM "Loperamide abuse associated with cardiac dysrhythmia and death." Ann Emerg Med 69 (2017): 83-6. [PMID: 27140747] | ||||
38 | Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA. | ||||
39 | Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
40 | 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] | ||||
41 | Product Information. Lamprene (clofazimine). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
42 | Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA. | ||||
43 | Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ. | ||||
44 | 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] | ||||
45 | Product Information. Remeron (mirtazapine). Organon, West Orange, NJ. | ||||
46 | Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA. | ||||
47 | Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA. | ||||
48 | EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.". | ||||
49 | Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC. | ||||
50 | Product Information. Sustiva (efavirenz). DuPont Pharmaceuticals, Wilmington, DE. | ||||
51 | Anson BD, Weaver JG, Ackerman MJ, et al. "Blockade of HERG channels by HIV protease inhibitors." Lancet 365 (2005): 682-686. [PMID: 15721475] | ||||
52 | Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ. | ||||
53 | Product Information. Vaprisol (conivaptan). Cumberland Pharmaceuticals Inc, Nashville, TN. | ||||
54 | Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC. | ||||
55 | Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
56 | Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE. | ||||
57 | Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA. | ||||
58 | Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA. | ||||
59 | 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] | ||||
60 | Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO. | ||||
61 | Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
62 | Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
63 | Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ. | ||||
64 | 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] | ||||
65 | Product Information. Anzemet (dolasetron). Hoechst Marion-Roussel Inc, Kansas City, MO. | ||||
66 | Product Information. Wellbutrin XL (buPROPion). GlaxoSmithKline, Philadelphia, PA. | ||||
67 | Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ. | ||||
68 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
69 | Matsuoka LY "Convulsions following application of gamma benzene hexachloride." J Am Acad Dermatol 5 (1981): 98-9. [PMID: 6168673] | ||||
70 | Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC. | ||||
71 | Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA. | ||||
72 | Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA. | ||||
73 | Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL. | ||||
74 | Ansari SR, Chopra N "Gatifloxacin and Prolonged QT Interval." Am J Med Sci 327 (2004): 55-6. [PMID: 14722399] | ||||
75 | Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN. | ||||
76 | Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA. | ||||
77 | 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] | ||||