Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00218)
Name
Dronedarone
Synonyms    Click to Show/Hide the Synonyms of This API
Dronedarone; 141626-36-0; Multaq; SR 33589; SR 33589B; UNII-JQZ1L091Y2; SR33589; N-(2-Butyl-3-(p-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)methanesulfonamide; N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-1-benzofuran-5-yl]methanesulfonamide; N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)-methanesulfonamide; CHEMBL184412; JQZ1L091Y2; CHEBI:50659; N-[2-butyl-3-{4-[3-(dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide; NCGC00188863-01; DSSTox_CID_28579; DSSTox_RID_82850; Methanesulfonamide, N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)-5-benzofuranyl)-; Methanesulfonamide, N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-benzofuranyl]-; DSSTox_GSID_48653; N-(2-butyl-3-{4-[3-(dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl)methanesulfonamide; Dronedarone (INN); CAS-141626-36-0; Dronedarone [INN:BAN]; C31H44N2O5S; HSDB 7928; DRONEDARONE BASE; cc-334; SCHEMBL110363; GTPL7465; MET037; DTXSID3048653; HMS3749G19; BCP21326; HY-A0016; Tox21_113008; BDBM50151864; MFCD00910331; SR-33598B; STL451011; ZINC49933061; AKOS005145680; Tox21_113008_1; AC-5012; CS-0384; DB04855; MCULE-5052395136; NCGC00188863-02; NCGC00188863-10; AB0022262; FT-0651916; D02537; W-5212; AB01566893_01; 626D360; A807786; L001445; Q408637; J-520428; Multaq; SR-33589; SR33589; SR 33589; SR-33589B; N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)benzofuran-5-yl) methanesulfonamide; N-[2-butyl-3-(p-{3-(dibutylamino)propoxy} benzoyl)-5-benzofuranyl]methanesulfonamide; n-[2-butyl-3-({4-[3-(dibutylamino)propoxy]phenyl}carbonyl)-1-benzofuran-5-yl]methanesulfonamide; N-[2-butyl-3-[[4-[3-(dibutylamino)propoxy]phenyl]-oxomethyl]-5-benzofuranyl]methanesulfonamide; N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]phenyl]carbonyl-1-benzofuran-5-yl]methanesulfonamide
Clinical Status
Approved
Disease Indication Atrial fibrillation ICD-11: BC81 [1]
PubChem CID
208898
Formula
C31H44N2O5S
Canonical SMILES
CCCCC1=C(C2=C(O1)C=CC(=C2)NS(=O)(=O)C)C(=O)C3=CC=C(C=C3)OCCCN(CCCC)CCCC
InChI
1S/C31H44N2O5S/c1-5-8-12-29-30(27-23-25(32-39(4,35)36)15-18-28(27)38-29)31(34)24-13-16-26(17-14-24)37-22-11-21-33(19-9-6-2)20-10-7-3/h13-18,23,32H,5-12,19-22H2,1-4H3
InChIKey
ZQTNQVWKHCQYLQ-UHFFFAOYSA-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=208898"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 556.8 Topological Polar Surface Area 97.2
XlogP 7.2 Complexity 800
Heavy Atom Count 39 Rotatable Bond Count 18
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 7
Full List of Drug Formulations (DFMs) Containing This API
          Dronedarone Hydrochloride eq 400mg base 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
Hypromellose; Starch; Crospovidone; Poloxamer 407; Lactose Monohydrate; Colloidal Silicon Dioxide; Magnesium Stearate; Polyethylene Glycol 6000; Titanium Dioxide; Carnauba Wax
                   Dosage Form Tablet
                   Company Sanofi Aventis Us
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [3]
          Dronedarone 400 mg tablet Click to Show/Hide the Full List of Formulation(s):          3 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Crospovidone; Poloxamer 407; Polyethylene glycol 6000; Silicon dioxide; Carnauba wax; Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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; Titanium dioxide; Poloxamer 407; Polyethylene glycol 6000; Silicon dioxide; Carnauba wax; Crospovidone (15 mpa.s at 5%); Hypromellose, unspecified; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sanofi-Aventis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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; Titanium dioxide; Poloxamer 407; Polyethylene glycol 6000; Silicon dioxide; Carnauba wax; Crospovidone (15 mpa.s at 5%); Hypromelloses; Starch, corn
                   Dosage Form Oral Tablet
                   Company Cardinal Health
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Poloxamer 407 DIG Info Albendazole monooxygenase (EC50 = 32.8 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 6000 DIG Info Albendazole monooxygenase (Inhibition ratio < 70 %) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved dronedarone from the official website of the U.S. Food and Drug Administration.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
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.

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