Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00272)
Name
Fesoterodine
Synonyms    Click to Show/Hide the Synonyms of This API
Fesoterodine; 286930-02-7; Fesoterodine maleate; UNII-621G617227; 250214-44-9; [2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate; 621G617227; (R) Fesoterodine; Fesoterodine [INN:BAN]; [2-[(1R)-3-(di(propan-2-yl)amino)-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate; Fesoterodine (INN); SCHEMBL121127; GTPL7473; CHEMBL1201764; DTXSID80182853; CHEBI:135920; CS-M2392; ZINC1552908; AKOS015841710; DB06702; NCGC00346540-01; NCGC00346540-02; NCGC00346540-03; AC-32493; HY-70053; D07226; AB01274866-01; AB01274866_02; 930F027; Q4482372; 2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate; Propanoic acid, 2-methyl-, 2-((1R)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-(hydroxymethyl)phenyl ester
Clinical Status
Approved
Disease Indication Overactive bladder ICD-11: GC50 [1]
PubChem CID
6918558
Formula
C26H37NO3
Canonical SMILES
CC(C)C(=O)OC1=C(C=C(C=C1)CO)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2
InChI
1S/C26H37NO3/c1-18(2)26(29)30-25-13-12-21(17-28)16-24(25)23(22-10-8-7-9-11-22)14-15-27(19(3)4)20(5)6/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3/t23-/m1/s1
InChIKey
DCCSDBARQIPTGU-HSZRJFAPSA-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=6918558"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 411.6 Topological Polar Surface Area 49.8
XlogP 5.5 Complexity 491
Heavy Atom Count 30 Rotatable Bond Count 11
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 4
Full List of Drug Formulations (DFMs) Containing This API
          Fesoterodine 4 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 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; Glyceryl dibehenate; Indigotindisulfonate sodium; Talc; Titanium dioxide; Xylitol; Lecithin, soybean; Polyvinyl alcohol; Aluminum oxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Avera McKennan Hospital; U.S. Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [3]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [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
Lactose monohydrate; Glyceryl behenate; Indigotindisulfonate sodium; Talc; Titanium dioxide; Xylitol; Lecithin, soybean; Polyvinyl alcohol; Aluminum oxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [3]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [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
Lactose monohydrate; Glyceryl dibehenate; Indigotindisulfonate sodium; Talc; Titanium dioxide; Xylitol; Lecithin, soybean; Aluminum oxide; Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Cardinal Health; Pfizer Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [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
Lactose monohydrate; Magnesium stearate; Ferric oxide yellow; Talc; Titanium dioxide; Lecithin, soybean; Povidone; Cellulose, microcrystalline; Hypromelloses; Polyvinyl alcohol, unspecified; Starch, corn; Xanthan gum
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Cadila Healthcare; Zydus 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) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [4]
          Fesoterodine 8 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 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; Glyceryl dibehenate; Indigotindisulfonate sodium; Talc; Titanium dioxide; Xylitol; Lecithin, soybean; Polyvinyl alcohol; Aluminum oxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company U.S. Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [3]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [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
Lactose monohydrate; Glyceryl behenate; Indigotindisulfonate sodium; Talc; Titanium dioxide; Xylitol; Lecithin, soybean; Polyvinyl alcohol; Aluminum oxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [3]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [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
Lactose monohydrate; Glyceryl dibehenate; Indigotindisulfonate sodium; Talc; Titanium dioxide; Xylitol; Lecithin, soybean; Aluminum oxide; Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Avera McKennan Hospital; Cardinal Health; Pfizer Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [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
Lactose monohydrate; Magnesium stearate; Talc; Titanium dioxide; Lecithin, soybean; Povidone; Cellulose, microcrystalline; Hypromelloses; Polyvinyl alcohol, unspecified; Starch, corn; Xanthan gum
                   Dosage Form 24 HR Extended Release Oral Tablet
                   Company Cadila Healthcare; Zydus 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) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [4]
References
1 FDA label for approved fesoterodine 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 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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