Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00652)
Name
Tapentadol
Synonyms    Click to Show/Hide the Synonyms of This API
Tapentadol; 175591-23-8; Nucynta; Palexia; 3-((2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl)phenol; UNII-H8A007M585; CG5503; phenol, 3-[(1r,2r)-3-(dimethylamino)-1-ethyl-2-methylpropyl]-; BN 200 (BASE); CG5503 (BASE); BN-200; H8A007M585; CG-5503; 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol; (R,R)-Tapentadol; Tapentadol [USAN:INN]; 3-((1R,2R)-3-(Dimethylamino)-1-ethyl-2-methylpropyl)phenol; Phenol, 3-((1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl)-; BN 200; CG 5503; 3-[3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol; Tapentadol (USAN/INN); cc-664; SCHEMBL116924; Phenol,3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]-; GTPL7477; DEA No. 9780; CHEMBL1201776; CG5503 IR; HSDB 8309; ZINC20783; DTXSID30170003; CHEBI:135935; CS-M0020; 4084AH; BDBM50386381; AKOS015951190; ACN-050883; BCP9000118; DB06204; QC-1146; SB17333; FT-0699883; B-1798; D06007; AR-270/43507984; Q414463; 3-[(2R,3R)-1-dimethylamino-2-methylpentan-3-yl]phenol; (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol
Clinical Status
Approved
Disease Indication Neuropathic pain ICD-11: 8E43 [1]
PubChem CID
9838022
Formula
C14H23NO
Canonical SMILES
CC[C@@H](C1=CC(=CC=C1)O)[C@@H](C)CN(C)C
InChI
1S/C14H23NO/c1-5-14(11(2)10-15(3)4)12-7-6-8-13(16)9-12/h6-9,11,14,16H,5,10H2,1-4H3/t11-,14+/m0/s1
InChIKey
KWTWDQCKEHXFFR-SMDDNHRTSA-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=9838022"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 221.34 Topological Polar Surface Area 23.5
XlogP 3.5 Complexity 193
Heavy Atom Count 16 Rotatable Bond Count 5
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Tapentadol 150 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
Alpha.-tocopherol; Fd&c blue no. 2; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Polyvinyl alcohol; Aluminum oxide; Hypromelloses; Polyethylene glycols; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Janssen Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [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
Alpha.-tocopherol; Fd&c blue no. 2; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Aluminum oxide; Hypromellose, unspecified; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Depo NF Sub
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
          Tapentadol 100 mg tablet Click to Show/Hide the Full List of Formulation(s):          6 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
Alpha.-tocopherol; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Polyvinyl alcohol; Aluminum oxide; Hypromelloses; Polyethylene glycols; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Janssen Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [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
Alpha.-tocopherol; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Aluminum oxide; Hypromellose, unspecified; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Depo NF Sub; 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
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [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; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Polyvinyl alcohol; Povidone; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [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
Lactose monohydrate; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Polyvinyl alcohol; Povidone; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycols
                   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
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
             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; Talc; Titanium dioxide; Croscarmellose sodium; Polyvinyl alcohol; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycols; Povidones
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [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
Lactose monohydrate; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Depo NF Sub
                   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) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
          Tapentadol 200 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
Alpha.-tocopherol; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Polyvinyl alcohol; Aluminum oxide; Hypromelloses; Polyethylene glycols; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Janssen Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [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
Alpha.-tocopherol; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Aluminum oxide; Hypromellose, unspecified; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Depo NF Sub
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
          Tapentadol 250 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
Alpha.-tocopherol; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Polyvinyl alcohol; Aluminum oxide; Hypromelloses; Polyethylene glycols; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Janssen Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [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
Alpha.-tocopherol; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Aluminum oxide; Hypromellose, unspecified; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Depo NF Sub
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
          Tapentadol 50 mg tablet Click to Show/Hide the Full List of Formulation(s):          6 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
Alpha.-tocopherol; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Polyvinyl alcohol; Hypromelloses; Polyethylene glycols; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Janssen Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [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
Alpha.-tocopherol; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Hypromellose, unspecified; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Shellac
                   Dosage Form 12 HR Extended Release Oral Tablet
                   Company Depo NF Sub; 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
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [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
Alpha.-tocopherol; Ferrosoferric oxide; Talc; Titanium dioxide; Polyvinyl alcohol; Hypromelloses; Polyethylene glycols; Polyethylene glycols; Shellac
                   Dosage Form 12 HR Extended Release 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
Alpha-tocopherol DIG Info Glutathione S-transferase P (IC50 = 500 nM) [2]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
             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; Croscarmellose sodium; Polyvinyl alcohol; Povidone; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
             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; Talc; Titanium dioxide; Croscarmellose sodium; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Depo NF Sub
                   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) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [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
Lactose monohydrate; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Aluminum oxide; Microcrystalline cellulose; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack
                   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) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
          Tapentadol Hydrochloride eq 100mg base extended release tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Alpha-Tocopherol (Vitamin E); Hypromellose; Polyethylene Glycol; Polyethylene Oxide; Polyvinyl Alcohol; Polyethylene Glycol; Talc; Titanium Dioxide; The Colorant Fd&C Blue 2 Aluminum Lake
                   Dosage Form Extended Release Tablet
                   Company Collegium Pharm
                   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) [3]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 150mg base extended release tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Alpha-Tocopherol (Vitamin E); Hypromellose; Polyethylene Glycol; Polyethylene Oxide; Polyvinyl Alcohol; Polyethylene Glycol; Talc; Titanium Dioxide; The Colorant Fd&C Blue 2 Aluminum Lake
                   Dosage Form Extended Release Tablet
                   Company Collegium Pharm
                   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) [3]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 200mg base extended release tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Alpha-Tocopherol (Vitamin E); Hypromellose; Polyethylene Glycol; Polyethylene Oxide; Polyvinyl Alcohol; Polyethylene Glycol; Talc; Titanium Dioxide; The Colorant Fd&C Blue 2 Aluminum Lake
                   Dosage Form Extended Release Tablet
                   Company Collegium Pharm
                   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) [3]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 250mg base extended release tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Alpha-Tocopherol (Vitamin E); Hypromellose; Polyethylene Glycol; Polyethylene Oxide; Polyvinyl Alcohol; Polyethylene Glycol; Talc; Titanium Dioxide; The Colorant Fd&C Blue 2 Aluminum Lake
                   Dosage Form Extended Release Tablet
                   Company Collegium Pharm
                   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) [3]
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 50mg base solution Click to Show/Hide the Full List of Formulation(s):          1 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
Croscarmellose Sodium; Lactose Monohydrate; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Polyvinyl Alcohol; Titanium Dioxide; Polyethylene Glycol; Talc; The Colorant Fd&C Yellow 6 Aluminum Lake; Colorant D&C Yellow 10 Aluminum Lake
                   Dosage Form Solution
                   Company Collegium Pharm
                   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]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 75mg base solution Click to Show/Hide the Full List of Formulation(s):          1 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
Croscarmellose Sodium; Lactose Monohydrate; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Polyvinyl Alcohol; Titanium Dioxide; Polyethylene Glycol; Talc; The Colorant Fd&C Yellow 6 Aluminum Lake; Colorant D&C Yellow 10 Aluminum Lake
                   Dosage Form Solution
                   Company Collegium Pharm
                   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]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 50mg base extended release tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Alpha-Tocopherol (Vitamin E); Hypromellose; Polyethylene Glycol; Polyethylene Oxide; Polyvinyl Alcohol; Polyethylene Glycol; Talc; Titanium Dioxide; Yellow Iron Oxide
                   Dosage Form Extended Release Tablet
                   Company Collegium Pharm
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
DL-alpha-tocopherol DIG Info Presenilin 1 (EC50 > 100000 nM) [6]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol Hydrochloride eq 100mg base solution Click to Show/Hide the Full List of Formulation(s):          1 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
Croscarmellose Sodium; Lactose Monohydrate; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Polyvinyl Alcohol; Titanium Dioxide; Polyethylene Glycol; Talc; The Colorant Fd&C Yellow 6 Aluminum Lake
                   Dosage Form Solution
                   Company Collegium Pharm
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Tapentadol 75 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
Lactose monohydrate; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Polyvinyl alcohol; Povidone; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycol
                   Dosage Form Oral Tablet
                   Company Physicians Total Care; Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [5]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
             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; Magnesium stearate; Talc; Titanium dioxide; Croscarmellose sodium; Aluminum oxide; Cellulose, microcrystalline; Polyethylene glycol, unspecified; Polyvinyl alcohol, unspecified; Povidone, unspecified
                   Dosage Form Oral Tablet
                   Company Depo NF Sub
                   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) [7]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [7]
          Tapentadol Hydrochloride eq 20mg base/ml solution Click to Show/Hide the Full List of Formulation(s):          1 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
Citric Acid Monohydrate; Purified Water; Raspberry Flavor; Sodium Hydroxide; Sucralose
                   Dosage Form Solution
                   Company Collegium Pharm
                   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]
References
1 FDA label for approved tapentadol from the official website of the U.S. Food and Drug Administration.
2 Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example. J Med Chem. 2018 Sep 13; 61(17):7448-7470.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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 Membrane anchoring -secretase modulators with terpene-derived moieties. Bioorg Med Chem Lett. 2013 Jul 1; 23(13):3852-6.
7 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
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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