Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00710)
Name
Trospium
Synonyms    Click to Show/Hide the Synonyms of This API
Trospium; 47608-32-2; UNII-T4Y8ORK057; T4Y8ORK057; CHEMBL1888176; Trospium cation; [(1S,5R)-spiro[8-azoniabicyclo[3.2.1]octane-8,1'-azolidin-1-ium]-3-yl] 2-hydroxy-2,2-diphenylacetate; NCGC00167438-01; NCGC00167438-02; tropsium cation; tropsium ion; SCHEMBL119810; SCHEMBL2447242; DTXSID6048337; CHEBI:145791; ZINC12503068; 3alpha-Hydroxyspiro(1alphah,5alphah-nortropane-8,1'-pyrrolidinium) benzilate; ZINC100016084; ZINC100371992; AM84314; DB00209; AB01274814-01; AB01274814_02; (1alpha,3beta,5alpha)-3-[(2-hydroxy-2,2-diphenylacetyl)oxy]-spiro[8-azoniabicyclo[3.2.1]octane-8,1'-pyrrolidinium]; (1alpha,5alpha)-3beta-[(Hydroxydiphenylacetyl)oxy]spiro[8-azoniabicyclo[3.2.1]octane-8,1'-pyrrolidinium]; (1S,3R,5R)-3-[(2-hydroxy-2,2-diphenylacetyl)oxy]-8lambda(5)-azaspiro[bicyclo[3.2.1]octane-8,1'-pyrrolidin]-8-ylium
Clinical Status
Approved
Disease Indication Overactive bladder ICD-11: GC50 [1]
PubChem CID
5284632
Formula
C25H30NO3+
Canonical SMILES
C1CC[N+]2(C1)[C@@H]3CC[C@H]2CC(C3)OC(=O)C(C4=CC=CC=C4)(C5=CC=CC=C5)O
InChI
1S/C25H30NO3/c27-24(25(28,19-9-3-1-4-10-19)20-11-5-2-6-12-20)29-23-17-21-13-14-22(18-23)26(21)15-7-8-16-26/h1-6,9-12,21-23,28H,7-8,13-18H2/q+1/t21-,22+,23?
InChIKey
OYYDSUSKLWTMMQ-AIZNXBIQSA-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=5284632"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 392.5 Topological Polar Surface Area 46.5
XlogP 4.4 Complexity 553
Heavy Atom Count 29 Rotatable Bond Count 5
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Trospium 60 mg capsule 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
D&c red no. 28; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Triethyl citrate; Polyethylene glycol 400; Polyethylene glycol 4000; Polysorbate 80; Polyvinyl alcohol; Ethylcellulose (10 mpa.s); Gelatin; Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s); Poly(methyl acrylate-co-methyl methacrylate-co-methacrylic acid 7:3:1 280000 mw); Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Actavis Pharma; BluePoint Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
D&C red no. 28 DIG Info Organic anion transporter 1 (Ki = 0.064 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [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
D&c red no. 28; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Sucrose; Talc; Titanium dioxide; Triethyl citrate; Polyethylene glycol 400; Polyethylene glycol 4000; Polysorbate 80; Ethylcellulose (10 mpa.s); Gelatin, unspecified; Hypromellose 2910 (3 mpa.s); Hypromellose 2910 (6 mpa.s); Poly(methyl acrylate-co-methyl methacrylate-co-methacrylic acid 7:3:1 280000 mw); Polyvinyl alcohol, unspecified; Shellac; Starch, corn
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
D&C red no. 28 DIG Info Organic anion transporter 1 (Ki = 0.064 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [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; Sodium lauryl sulfate; Fd&c yellow no. 6; Magnesium stearate; Ferrosoferric oxide; Magnesium aluminum silicate; Potassium hydroxide; Propylene glycol; Sodium chloride; Talc; Titanium dioxide; Polyethylene glycol 400; Silicon dioxide; Gelatin; Methacrylic acid - ethyl acrylate copolymer (1:1) type a; Povidones; Shellac
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Paddock Laboratories,
                   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) [2]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Talc; Triethyl citrate
                   Dosage Form 24 HR Extended Release Capsule
                   Company Physicians Total Care
             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
Talc; Triethyl citrate
                   Dosage Form 24 HR Extended Release Oral Capsule
                   Company Allergan
          Trospium 20 mg tablet 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
Stearic acid; Lactose monohydrate; Calcium carbonate; Magnesium stearate; Ferric oxide red; Sucrose; Talc; Titanium dioxide; Carboxymethylcellulose sodium; Croscarmellose sodium; Povidone; Silicon dioxide; Carnauba wax; Cellulose, microcrystalline; Polyethylene glycol 8000; Starch, wheat; White wax
                   Dosage Form Oral Tablet
                   Company Allergan
                   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) [2]
Calcium carbonate DIG Info Carbonic anhydrase IX (Ki = 8600 nM) [7]
Carboxymethylcellulose sodium DIG Info Albendazole monooxygenase (EC50 = 12.6 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Sucralose; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Xylitol; Croscarmellose sodium; Polyethylene glycol 400; Polysorbate 80; Silicon dioxide; Hypromelloses; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Cipla; Exelan Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sucralose DIG Info Carbonic anhydrase II (Ki = 300 nM) [8]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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 monohydrate; Calcium carbonate; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 3350; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company Paddock Laboratories,
                   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) [2]
Calcium carbonate DIG Info Carbonic anhydrase IX (Ki = 8600 nM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Polyethylene glycol 3350 DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Butyl alcohol; Magnesium stearate; Ferric oxide red; Propylene glycol; Sucrose; Talc; Titanium dioxide; Croscarmellose sodium; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols; Shellac
                   Dosage Form Oral Tablet
                   Company Heritage Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Ferric oxide red; Ferric oxide yellow; Sucrose; Talc; Titanium dioxide; Polyethylene glycol 400; Polyethylene glycol 6000; Povidone; Silicon dioxide; Cellulose, microcrystalline; Copovidone k25-31; Croscarmellose; Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Biomes Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Ferric oxide red; Ferric oxide yellow; Sucrose; Talc; Titanium dioxide; Croscarmellose sodium; Polyethylene glycol 400; Polyethylene glycol 6000; Silicon dioxide; Cellulose, microcrystalline; Copovidone k25-31; Hypromelloses; Povidones; Starch, corn
                   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) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Ferric oxide yellow; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (1200000 mw); Hypromellose 2906 (4000 mpa.s); Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company AvKARE
                   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) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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; Ferric oxide yellow; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromellose 2906 (4000 mpa.s); Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   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) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             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
Lactose monohydrate; Magnesium stearate; Ferric oxide yellow; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromellose 2906 (4000 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) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
References
1 FDA label for approved trospium 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 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.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
6 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
7 Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V, and IX with anions isosteric and isoelectronic with sulfate, nitrate, and carbonate. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):567-71.
8 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.

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