Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00391)
Name
Mefloquine
Synonyms    Click to Show/Hide the Synonyms of This API
mefloquine; Lariam; 49752-90-1; GNF-Pf-5544; 53230-10-7; alpha-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol; CHEMBL416956; CHEBI:63681; Racemic mefloquine; [2,8-bis(trifluoromethyl)quinolin-4-yl]-piperidin-2-ylmethanol; [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol; Mefloquinone; (2,8-bis(trifluoromethyl)quinolin-4-yl)(piperidin-2-yl)methanol; [2,8-bis(trifluoromethyl)quinolin-4-yl](piperidin-2-yl)methanol; Ro 21-5998; WR-142490; WR 142,490; melfoquine; Mefaquin; rac-mefloquine; EINECS 256-468-3; Spectrum_001312; Prestwick0_000126; Prestwick1_000126; Prestwick2_000126; Prestwick3_000126; Spectrum2_001516; Spectrum3_000953; Spectrum4_001066; Spectrum5_001122; Ro-21-5998-001; SCHEMBL21782; BSPBio_000172; KBioGR_001392; KBioSS_001792; DivK1c_000790; SPECTRUM1503070; SPBio_001591; SPBio_002111; BPBio1_000190; GTPL4252; HMS502H12; KBio1_000790; KBio2_001792; KBio2_004360; KBio2_006928; KBio3_002046; NINDS_000790; HMS1922C09; 4-Quinolinemethanol, .alpha.-(2R)-2-piperidinyl-2,8-bis(trifluoromethyl)-, (.alpha.S)-rel-; alpha-2-Piperidyl-2,8-bis(trifluoromethyl)quinoline-4-methanol; BCP09262; BDBM50022889; CCG-39182; STL581681; DB00358; Ro-215998; IDI1_000790; NCGC00094994-01; NCGC00094994-02; NCGC00094994-03; NCGC00094994-04; NCGC00094994-06; Ro-21-5998; SBI-0051761.P002; AB00052310; FT-0628185; AB00052310_09; Q736270; BRD-A89585551-003-03-4; BRD-A89585551-003-08-3; (2,8-Bis-trifluoromethyl-quinolin-4-yl)-piperidin-2-yl-methanol; 4-Quinolinemethanol, alpha-2-piperidinyl-2,8-bis(trifluoromethyl)-; alpha-(2-piperidinyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol; rel-(2,8-bis(trifluoromethyl)quinolin-4-yl)(piperidin-2-yl)methanol; (2,8-Bis-trifluoromethyl-quinolin-4-yl)-(1-methyl-piperidin-2-yl)-methanol; (S)-(2,8-Bis-trifluoromethyl-quinolin-4-yl)-(R)-piperidin-2-yl-methanol; (S)-(2,8-Bis-trifluoromethyl-quinolin-4-yl)-piperidin-2-yl-methanol; [(R*,S*)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol; 2-[(2,8-Bis-trifluoromethyl-quinolin-4-yl)-hydroxy-methyl]-piperidinium; (2,8-Bis-trifluoromethyl-quinolin-4-yl)-piperidin-2-yl-methanol( Mefloquine); (2,8-Bis-trifluoromethyl-quinolin-4-yl)-piperidin-2-yl-methanol; (Mefloquine or MF); (DL-erythro-.alpha.-2-Piperidyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol; 2,8-di(trifluoromethyl)-4-quinolyl-hexahydro-2-pyridinylmethanol(Mefloquine); 4-Quinolinemethanol, .alpha.-2-piperidinyl-2,8-bis(trifluoromethyl)-, (R*,S*)-(.+/-.)-
Clinical Status
Approved
Disease Indication Malaria ICD-11: 1F40 [1]
PubChem CID
4046
Formula
C17H16F6N2O
Canonical SMILES
C1CCNC(C1)C(C2=CC(=NC3=C2C=CC=C3C(F)(F)F)C(F)(F)F)O
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
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=4046"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 378.31 Topological Polar Surface Area 45.2
XlogP 3.6 Complexity 483
Heavy Atom Count 26 Rotatable Bond Count 2
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 9
Full List of Drug Formulations (DFMs) Containing This API
          Mefloquine 250 mg tablet Click to Show/Hide the Full List of Formulation(s):          8 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Crospovidone; Polysorbate 80; Povidone k30; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Rebel Distributors; West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Crospovidone; Poloxamer 188; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 188 DIG Info Albendazole monooxygenase (IC50 = 60 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Crospovidone; Polysorbate 80; Povidone k30; Cellulose, microcrystalline; Colloidal silicon dioxide; Starch, corn
                   Dosage Form Oral Tablet
                   Company H. J. Harkins Company
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Poloxamer 188; Silicon dioxide; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Starch, corn
                   Dosage Form Oral Tablet
                   Company Preferred Pharamaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 188 DIG Info Albendazole monooxygenase (IC50 = 60 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Poloxamer 188; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 188 DIG Info Albendazole monooxygenase (IC50 = 60 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Poloxamer 124; Starch, corn; Starch, corn
                   Dosage Form Oral Tablet
                   Company Rebel Distributors
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 7 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Talc; Crospovidone; Cellulose, microcrystalline; Hydroxypropyl cellulose, low substituted; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care; Sandoz
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             Drug Formulation 8 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Calcium alginate; Silicon dioxide; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Poloxamer 331; Povidone k29/32; Propylene glycol alginate; Starch, corn
                   Dosage Form Oral Tablet
                   Company West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved mefloquine from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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