Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00183)
Name
Tolterodine
Synonyms    Click to Show/Hide the Synonyms of This API
(+)-Tolterodine; Detrusitol; Tolterodinum; Tolterodine tartrate; Kabi 2234; Urotrol; S-(-)-Tolterodine; Tolterodina; Tolterodinum [INN-Latin]; UNII-WHE7A56U7K; Tolterodina [INN-Spanish]; Kabi-2234; CHEMBL1382; WHE7A56U7K; Tolterodine L-Tartrate; (R)-(+)-Tolterodine; CHEBI:9622; 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol; (+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol; 2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol; 124937-51-5 (free base); Tolterodine [INN]; NCGC00159519-02; Unidet; DSSTox_CID_3687; DSSTox_RID_77147; DSSTox_GSID_23687; (r)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol; 2-[3-[Bis(1-Methylethyl)Amino]-1-Phenylpropyl]-4-Methyl Phenol Monohydrobromide; SMR000596518; CAS-124937-51-5; MFCD07771985; PHA-686464B; PNU 200583; tolterodin; (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol; Tolterodine [USAN:INN:BAN]; 2-[(1R)-3-(di(propan-2-yl)amino)-1-phenylpropyl]-4-methylphenol; (R)-2,3-BIS(1-METHYLETHYL)AMINO-1-PHENYLPROPYL-4-METHYLPHENOL; Phenol, 2-((1R)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-methyl-; Phenol, 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-methyl-; TolterodineL-tartrate; Tolterondine Tartrate; PubChem20792; Tolterodine (USAN/INN); SCHEMBL3064; GTPL360; MLS001195620; MLS001304745; BIDD:GT0318; DTXSID3023687; HMS2230E24; ZINC968336; ACT04387; AMY17772; HY-A0024; tolterodine extended release capsules; Tox21_111737; 2-{(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl}-4-methylphenol; BDBM50165008; AKOS015841711; AKOS015895578; Tox21_111737_1; AC-3472; CS-1799; DB01036; KS-5165; NCGC00159519-04; NCGC00263557-01; C07750; D00646; 27817-EP2269989A1; 27817-EP2298767A1; 27817-EP2314587A1; AB00698547-12; AB00698547_13; 937T515; Q424312; J-005184; Q-200223; 2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-methylphenol; 2-[(1r)3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-methylphenol; (+)-(R)-3-(2-hydroxy-5-methylphenyl)-N,N-diisopropyl-3-phenylpropylamine; 2-[(1R)-3-[BIS(1-METHYLETHYL)AMINO]-1-PHENYLPROPYL]-4-METHYL-PHENOL TARTRATE
Clinical Status
Approved
Disease Indication Overactive bladder ICD-11: GC50 [1]
PubChem CID
443879
Formula
C22H31NO
Canonical SMILES
CC1=CC(=C(C=C1)O)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2
InChI
1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1
InChIKey
OOGJQPCLVADCPB-HXUWFJFHSA-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=443879"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 325.5 Topological Polar Surface Area 23.5
XlogP 5.6 Complexity 340
Heavy Atom Count 24 Rotatable Bond Count 7
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Tolterodine 2 mg capsule Click to Show/Hide the Full List of Formulation(s):          9 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
Butyl alcohol; Ethyl acrylate; Fd&c blue no. 2; Isopropyl alcohol; Ammonia; Ferric oxide yellow; Methyl methacrylate; Potassium hydroxide; Propylene glycol; Talc; Titanium dioxide; Alcohol; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Ethylcelluloses; Gelatin; Hypromelloses; Methylene chloride; Shellac
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Camber Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Ethyl acrylate DIG Info NFE2-related factor 2 (EC50 = 5110 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             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
Oleic acid; Fd&c blue no. 2; Ammonia; Ferric oxide yellow; Potassium hydroxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Medium-chain triglycerides; Ethylcellulose, unspecified; Gelatin, unspecified; Hypromellose 2910 (5 mpa.s); Microcrystalline cellulose; Shellac
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Oleic acid; Fd&c blue no. 2; Ferric oxide yellow; Sucrose; Hypromellose; Medium-chain triglycerides; Ethylcellulose; Gelatin
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Sodium lauryl sulfate; Fd&c blue no. 2; Ferric oxide yellow; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Ethylcelluloses; Gelatin; Hypromelloses; Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Aphena Pharma Solutions-Tennessee; Golden State Medical Supply; Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [10]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             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
Oleic acid; Fd&c blue no. 2; Ferric oxide yellow; Sucrose; Medium-chain triglycerides; Ethylcellulose, unspecified; Gelatin, unspecified; Hypromellose, unspecified
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Greenstone; Pharmacia and Upjohn Company
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Oleic acid; Fd&c blue no. 2; Ferric oxide yellow; Sucrose; Medium-chain triglycerides; Ethylcelluloses; Gelatin; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Avera McKennan Hospital
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Oleic acid; Fd&c blue no. 2; Ferric oxide yellow; Sucrose; Medium-chain triglycerides; Ethylcellulose, unspecified; Gelatin, unspecified; Hypromellose, unspecified; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Cardinal Health
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
D&c yellow no. 10; Ferrosoferric oxide; Propylene glycol; Sucrose; Titanium dioxide; Triethyl citrate; Ethylcellulose (7 mpa.s); Fd&c green no. 3; Gelatin, unspecified; Hydroxypropyl cellulose (200000 mw); Hypromellose 2910 (6 mpa.s); Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Teva Pharmaceuticals
                   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]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             Drug Formulation 9 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
Oleic acid; Sucrose; Talc; Medium-chain triglycerides; Cellulose, microcrystalline; Ethylcelluloses; Gelatin; Hypromellose 2910 (5 mpa.s)
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Major Pharmaceuticals; Torrent Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
          Tolterodine 4 mg capsule Click to Show/Hide the Full List of Formulation(s):        10 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
Butyl alcohol; Ethyl acrylate; Fd&c blue no. 2; Isopropyl alcohol; Ammonia; Methyl methacrylate; Potassium hydroxide; Propylene glycol; Talc; Titanium dioxide; Alcohol; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Ethylcelluloses; Gelatin; Hypromelloses; Methylene chloride; Shellac
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Camber Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Ethyl acrylate DIG Info NFE2-related factor 2 (EC50 = 5110 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             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
Oleic acid; Fd&c blue no. 2; Ammonia; Potassium hydroxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Medium-chain triglycerides; Ethylcellulose, unspecified; Gelatin, unspecified; Hypromellose 2910 (5 mpa.s); Microcrystalline cellulose; Shellac
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Oleic acid; Fd&c blue no. 2; Sucrose; Hypromellose; Medium-chain triglycerides; Ethylcellulose; Gelatin
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [8]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Sodium lauryl sulfate; Fd&c blue no. 2; Ferric oxide yellow; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Ethylcelluloses; Gelatin; Hypromelloses; Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Aphena Pharma Solutions-Tennessee; Avera McKennan Hospital; Golden State Medical Supply; Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [10]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             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
Sodium lauryl sulfate; Fd&c blue no. 2; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Ethylcelluloses; Gelatin; Hypromelloses; Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [10]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             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
Oleic acid; Fd&c blue no. 2; Sucrose; Medium-chain triglycerides; Ethylcellulose, unspecified; Gelatin, unspecified; Hypromellose, unspecified
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Greenstone; Pharmacia and Upjohn Company
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Oleic acid; Fd&c blue no. 2; Sucrose; Medium-chain triglycerides; Ethylcellulose, unspecified; Gelatin, unspecified; Hypromellose, unspecified; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Cardinal Health
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             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
Oleic acid; Fd&c blue no. 2; Sucrose; Medium-chain triglycerides; Ethylcelluloses; Gelatin; Hypromelloses
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company PD-Rx Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
             Drug Formulation 9 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
Fd&c blue no. 1; Ferrosoferric oxide; Propylene glycol; Sucrose; Titanium dioxide; Triethyl citrate; Ethylcellulose (7 mpa.s); Gelatin, unspecified; Hydroxypropyl cellulose (200000 mw); Hypromellose 2910 (6 mpa.s); Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Teva 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) [10]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             Drug Formulation 10 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
Oleic acid; Sucrose; Talc; Medium-chain triglycerides; Cellulose, microcrystalline; Ethylcelluloses; Gelatin; Hypromellose 2910 (5 mpa.s)
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Major Pharmaceuticals; Torrent Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [6]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [7]
          Tolterodine 1 mg tablet Click to Show/Hide the Full List of Formulation(s):          7 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; Magnesium stearate; Anhydrous dibasic calcium phosphate; Titanium dioxide; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose; Sodium starch glycolate type b potato
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Sodium stearyl fumarate; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 6000; Cellulose, microcrystalline; Hypromellose 2910 (15 mpa.s); 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
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [11]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [9]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [5]
             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; Magnesium stearate; Titanium dioxide; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Greenstone; Pharmacia and Upjohn Company
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Magnesium stearate; Titanium dioxide; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Sodium starch glycolate type b potato
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Magnesium stearate; Dibasic calcium phosphate dihydrate; Titanium dioxide; Cellulose, microcrystalline; Colloidal silicon dioxide; Hypromelloses; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Macleods 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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Anhydrous dibasic calcium phosphate; Titanium dioxide; Triacetin; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polydextrose; Polyethylene glycols; Sodium starch glycolate type a potato
                   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) [9]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Dibasic calcium phosphate dihydrate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Polyethylene glycol 8000; Sodium starch glycolate type b potato
                   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) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
          Tolterodine 2 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; Magnesium stearate; Anhydrous dibasic calcium phosphate; Titanium dioxide; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose; Sodium starch glycolate type b potato
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Sodium stearyl fumarate; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 6000; Cellulose, microcrystalline; Hypromellose 2910 (15 mpa.s); 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
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [11]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [9]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [5]
             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; Magnesium stearate; Titanium dioxide; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Greenstone; Pharmacia and Upjohn Company
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Magnesium stearate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Stat Rx USA
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Magnesium stearate; Dibasic calcium phosphate dihydrate; Titanium dioxide; Cellulose, microcrystalline; Colloidal silicon dioxide; Hypromelloses; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Macleods 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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Anhydrous dibasic calcium phosphate; Titanium dioxide; Triacetin; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polydextrose; Polyethylene glycols; Sodium starch glycolate type a potato
                   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) [9]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Dibasic calcium phosphate dihydrate; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Polyethylene glycol 8000; Sodium starch glycolate type b potato
                   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) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
             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; Titanium dioxide; Triacetin; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polydextrose; Polyethylene glycols; Sodium starch glycolate type a potato
                   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) [9]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [9]
References
1 FDA label for approved tolterodine from the official website of the U.S. Food and Drug Administration.
2 A novel chalcone derivative as Nrf2 activator attenuates learning and memory impairment in a scopolamine-induced mouse model. Eur J Med Chem. 2020 Jan 1; 185:111777.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.
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 Characterization of the drug binding specificity of rat liver fatty acid binding protein. J Med Chem. 2008 Jul 10; 51(13):3755-64.
7 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.
8 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
9 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
10 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.
11 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.

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