Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00673)
Name
Tiagabine
Synonyms    Click to Show/Hide the Synonyms of This API
tiagabine; 115103-54-3; Gabitril; (R)-Tiagabine; Tiagabina; Tiagabinum; Tiagabinum [INN-Latin]; Tiagabina [INN-Spanish]; Abbott-70569; UNII-Z80I64HMNP; ABBOTT-70569-1; Gabitril (TN); CHEMBL1027; Z80I64HMNP; ABT-569; CHEBI:9586; (-)-(R)-1-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid; A-70569-1; Gabatril; Tiagabine [INN:BAN]; (3R)-1-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]piperidine-3-carboxylic acid; (3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl]piperidine-3-carboxylic acid; (-)-(r)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid; [3H]tiagabine; Tiagabine (INN); (3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid; NCGC00164626-01; NO 328; (R)-1-(4,4-Bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid; HSDB 7527; Gabitril,Tiagabine; Gabitril,Tiagabine HCl; NO050328; (R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)piperidine-3-carboxylic acid hydrochloride; NO 050328; SCHEMBL34653; ABT-569 FREE BASE; BIDD:GT0018; GTPL4685; GTPL4818; DTXSID5023663; ABBOTT-70569 FREE BASE; HMS3885J16; NNC-050328 FREE BASE; NO-050328 FREE BASE; HY-B0696; ZINC3831531; ABBOTT-705691 FREE BASE; BDBM50039251; BDBM50368628; NO050328;NO328;TGB; AKOS016011165; AC-7048; CCG-268358; DB00906; 3-Piperidinecarboxylic acid, 1-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-, (R)-; C07503; D08588; 103T543; Q907219; BRD-K60160658-003-08-8; (R)-(-)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]nipecotic acid; (r)-n-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid; (R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)piperidine-3-carboxylic acid; (R)-1-[4,4-Bis-(3-methyl-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid; (S)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-enyl)piperidine-3-carboxylic acid; 1-[4,4-Bis-(3-methyl-4,5-dihydro-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid; 3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-buten-1-yl]-, (3R)-; (R)-1-[4,4-Bis-(3-methyl-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid; hydrochloride; 1-[4,4-Bis-(3-methyl-thiophen-2-yl)-but-3-enyl]-piperidine-3-carboxylic acid; hydrochloride; 1006863-69-9
Clinical Status
Approved
Disease Indication Epilepsy ICD-11: 8A60 [1]
PubChem CID
60648
Formula
C20H25NO2S2
Canonical SMILES
CC1=C(SC=C1)C(=CCCN2CCC[C@H](C2)C(=O)O)C3=C(C=CS3)C
InChI
1S/C20H25NO2S2/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23)/t16-/m1/s1
InChIKey
PBJUNZJWGZTSKL-MRXNPFEDSA-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=60648"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 375.6 Topological Polar Surface Area 97
XlogP 2.7 Complexity 474
Heavy Atom Count 25 Rotatable Bond Count 6
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 5
Full List of Drug Formulations (DFMs) Containing This API
          Tiagabine 12 mg tablet Click to Show/Hide the Full List of Formulation(s):          3 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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydrogenated cottonseed oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Amneal Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Lactose; D&c yellow no. 10; Ascorbic acid; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Crospovidone, unspecified; Hydrogenated soybean oil; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cephalon
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Tiagabine 16 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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
Stearic acid; Anhydrous lactose; Ascorbic acid; Fd&c blue no. 2; Magnesium stearate; Talc; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydrogenated cottonseed oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Amneal Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; Ascorbic acid; Fd&c blue no. 2; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Crospovidone, unspecified; Hydrogenated soybean oil; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cephalon
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Tiagabine 2 mg tablet Click to Show/Hide the Full List of Formulation(s):          5 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
Stearic acid; Anhydrous lactose; Ascorbic acid; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydrogenated cottonseed oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Amneal Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Anhydrous lactose; Fd&c yellow no. 6; Butylated hydroxyanisole; Talc; Titanium dioxide; Crospovidone; Polysorbate 80; Silicon dioxide; Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sun Pharmaceutical Industries
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Butylhydroxyanisole DIG Info Prostaglandin G/H synthase 2 (IC50 = 2.6 uM) [3]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; Ascorbic acid; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hydrogenated soybean oil; Hydroxypropyl cellulose (1200000 mw); Hypromellose, unspecified; 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
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; Ascorbic acid; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Hydrogenated soybean oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cima Labs
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; Ascorbic acid; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Crospovidone, unspecified; Hydrogenated soybean oil; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cephalon
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Tiagabine 4 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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydrogenated cottonseed oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Amneal Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydrogenated soybean oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Carilion Materials Management
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Crospovidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Silicon dioxide; Crospovidone (15 mpa.s at 5%); Hydrogenated soybean oil; Hydroxypropyl cellulose (1200000 mw); Hypromellose, unspecified; 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
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Hydrogenated soybean oil; Hydroxypropyl cellulose (type h); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cima Labs
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Crospovidone, unspecified; Hydrogenated soybean oil; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cephalon
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Anhydrous lactose; D&c yellow no. 10; Ascorbic acid; Magnesium stearate; Titanium dioxide; Silicon dioxide; Crospovidone, unspecified; Hydrogenated soybean oil; Hydroxypropyl cellulose, unspecified; Hypromellose, unspecified; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Avera McKennan Hospital
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Anhydrous lactose; Lactose monohydrate; D&c yellow no. 10; Butylated hydroxyanisole; Talc; Titanium dioxide; Crospovidone; Silicon dioxide; Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sun Pharmaceutical Industries
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Butylhydroxyanisole DIG Info Prostaglandin G/H synthase 2 (IC50 = 2.6 uM) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Tiagabine Hydrochloride 2mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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
Anhydrous Lactose; Ascorbic Acid; Colloidal Silicon Dioxide; Crospovidone Type A; Hydrogenated Vegetable Oil Type 1 (Cottonseed Oil); Hydroxypropyl Cellulose; Hypromellose; Magnesium Stearate; Microcrystalline Cellulose; Pregelatinized Starch; Stearic Acid; Titanium Dioxide
                   Dosage Form Tablet
                   Company Amneal Pharmaceuticals Ny
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [6]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [4]
             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
Ascorbic Acid; Colloidal Silicon Dioxide; Crospovidone; Hydrogenated Vegetable Oil Wax; Hydroxypropyl Cellulose; Hypromellose; Lactose; Magnesium Stearate; Microcrystalline Cellulose; Pregelatinized Starch; Stearic Acid; Titanium Dioxide
                   Dosage Form Tablet
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [3]
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [6]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Ascorbic acid DIG Info Albendazole monooxygenase (IC50 = 4.1 mg.mL-1) [5]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [4]
References
1 FDA label for approved tiagabine from the official website of the U.S. Food and Drug Administration.
2 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
6 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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