Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00595)
Name
Riluzole
Synonyms    Click to Show/Hide the Synonyms of This API
riluzole; 1744-22-5; Rilutek; 2-Amino-6-(trifluoromethoxy)benzothiazole; 6-(trifluoromethoxy)benzo[d]thiazol-2-amine; 6-(trifluoromethoxy)-1,3-benzothiazol-2-amine; RP-54274; 2-amino-6-trifluoromethoxybenzothiazole; 2-Benzothiazolamine, 6-(trifluoromethoxy)-; 2-amino-6-(trifluoromethoxy)benzo[d]thiazole; PK-26124; RP 54274; C8H5F3N2OS; 2-Benzothiazolamine,6-(trifluoromethoxy)-; UNII-7LJ087RS6F; Riluzole (Rilutek); Amino-2 trifluoromethoxy-6 benzothiazole; MLS000069369; 6-Trifluoromethoxy-benzothiazol-2-ylamine; 2-Amino-6-(trifluoromethoxy)-benzothiazole; MFCD00210213; CHEMBL744; SMR000058231; 7LJ087RS6F; CHEBI:8863; Riluzol; 2-amino-6-(trifluoromethoxy)-1,3-benzothiazole; BENZOTHIAZOLE, 2-AMINO-6-TRIFLUOROMETHOXY-; Riluzole, 98%; 6-(trifluoromethoxy)benzothiazol-2-amine; NCGC00015882-09; Riluzolum; Riluzol [INN-Spanish]; Riluzolum [INN-Latin]; DSSTox_CID_25192; DSSTox_RID_80739; DSSTox_GSID_45192; Rilutek (TN); CAS-1744-22-5; 6-(trifluoromethoxy)benzothiazole-2-ylamine; Amino-2 trifluoromethoxy-6 benzothiazole [French]; 2-amino-6-(trifluoromethoxyl)benzothiazole; Riluzole, solid; Riluzole [USAN:USP:INN:BAN]; ALBB-006046; Riluzole(Rilutek)/; Prestwick-03A08; 6-(trifluoromethoxy)-2-benzothiazolamine; PubChem14501; Tocris-0768; 6-trifluoromethoxybenzothiazole-2-yl-amine; Opera_ID_548; Lopac-R-116; Prestwick0_000167; Prestwick1_000167; Prestwick2_000167; Prestwick3_000167; Spectrum2_000550; Biomol-NT_000245; Rilutek, Teglutik,Riluzole; cid_5070; Riluzole (JAN/USP/INN); Lopac0_001064; SCHEMBL78905; BSPBio_000033; BIDD:GT0055; SPBio_000599; SPBio_001954; ACMC-209e89; BPBio1_000037; BPBio1_000837; GTPL2326; ZINC6481; DTXSID3045192; BDBM30705; Bio1_000416; Bio1_000905; Bio1_001394; HMS1773G08; HMS2089O19; HMS2094G07; HMS2233E14; HMS3263E10; HMS3371A09; HMS3657E13; Pharmakon1600-01505348; BCP02142; BHV-0223; HY-B0211; Riluzole - CAS 1744-22-5; Tiglutik (thickened oral suspension); Tox21_110252; Tox21_501064; ABP000632; AC-730; ANW-22711; BBL013272; CCG-39528; NSC753433; NSC759823; SBB012436; STK503686; AKOS000265071; Tox21_110252_1; DB00740; KS-5231; LP01064; MCULE-9362288181; NSC-753433; NSC-759823; SDCCGSBI-0051034.P003; 2-amino-6-trifluoromethoxy-benzothiazole; 6-trifluoromethoxy-2-amino-benzothiazole; NCGC00015882-01; NCGC00015882-02; NCGC00015882-03; NCGC00015882-04; NCGC00015882-05; NCGC00015882-06; NCGC00015882-07; NCGC00015882-08; NCGC00015882-10; NCGC00015882-11; NCGC00015882-12; NCGC00015882-13; NCGC00015882-15; NCGC00015882-28; NCGC00023141-02; NCGC00023141-04; NCGC00023141-05; NCGC00023141-06; NCGC00261749-01; 6-(trifluoromethoxy)-2-aminobenzothiazole; 6-trifluoromethoxybenzo[d]thiazol-2-amine; AK-59567; ST038494; ST068834; SBI-0051034.P002; 2-Amino-6-(Trifluoromethoxy) Benzothiazole; 6-(Trifluoromethoxy)-2-amino-benzothiazole; AB0012884; DB-030335; EU-0101064; FT-0611194; SW196805-4; EN300-23782; 6-trifluoromethoxy-1,3-benzothiazol-2-ylamine; A-5766; C07937; D00775; J10184; J10441; VU0239571-11; 744R225; Q415744; SR-01000002997-3; BRD-K21283037-001-02-5; BRD-K21283037-003-03-9; BRD-K21283037-003-06-2; F3282-0020; Z166605314; Rilutek; Rilutor; 6-(Trifluoromethoxy)-2-benzothiazolamine; Riluzole, United States Pharmacopeia (USP) Reference Standard
Clinical Status
Approved
Disease Indication Amyotrophic lateral sclerosis ICD-11: 8B60 [1]
PubChem CID
5070
Formula
C8H5F3N2OS
Canonical SMILES
C1=CC2=C(C=C1OC(F)(F)F)SC(=N2)N
InChI
1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)
InChIKey
FTALBRSUTCGOEG-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=5070"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 234.2 Topological Polar Surface Area 76.4
XlogP 3.6 Complexity 238
Heavy Atom Count 15 Rotatable Bond Count 1
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 7
Full List of Drug Formulations (DFMs) Containing This API
          Riluzole 50 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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 400; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Ascend Laboratories; Kaiser Foundation Hospitals
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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
Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 6000; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company AvKARE; Rising Pharmaceuticals
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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
Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Povidone k30; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Kaiser Foundation Hospitals; Sun Pharmaceutical Industries
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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
Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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
Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Glenmark Pharmaceutials
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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
Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Talc; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company American Health Packaging
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
             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
Magnesium stearate; Talc; Titanium dioxide; Triacetin; Croscarmellose sodium; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polydextrose; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Global Pharmaceuticals
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
             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
Magnesium stearate; Dibasic calcium phosphate dihydrate; Talc; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Hypromellose 2910 (6 mpa.s); Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Apotex
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
References
1 FDA label for approved riluzole from the official website of the U.S. Food and Drug Administration.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.