Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00208)
Name
Dofetilide
Synonyms    Click to Show/Hide the Synonyms of This API
Dofetilide; 115256-11-6; Tikosyn; Dofetilida; Dofetilidum; Dofetilidum [INN-Latin]; Dofetilida [INN-Spanish]; UK 68798; UK-68,798; UK-68798; Dofetilide (Tikosyn); UNII-R4Z9X1N2ND; C19H27N3O5S2; beta-((p-Methanesulfonamidophenethyl)methylamino)methanesulfono-p-phenetidide; CHEMBL473; R4Z9X1N2ND; CHEBI:4681; NCGC00164549-01; DSSTox_CID_26433; DSSTox_RID_81610; DSSTox_GSID_46433; Xelide; SMR000466333; Tikosyn (TN); CAS-115256-11-6; UK 68,798; HSDB 7927; Dofetilide [USAN:USP:INN:BAN]; UK68798; SCHEMBL16135; Dofetilide (JAN/USP/INN); MLS000759442; MLS001424185; MLS006010154; GTPL2604; Dofetilide, >=98% (HPLC); DTXSID5046433; HMS2051N14; HMS2089F03; HMS2232H19; HMS3261G03; HMS3370B18; HMS3393N14; HMS3655A17; HMS3715H20; ZINC596731; ACT04222; BCP04770; HY-B0232; Tox21_112178; Tox21_500351; AC-385; BDBM50031720; MFCD00869707; NSC786034; AKOS005259921; Tox21_112178_1; BCP9000619; CCG-101037; DB00204; NC00287; NSC-786034; MRF-0000317; NCGC00164549-02; NCGC00261036-01; AK161932; BCP0726000009; AB0004775; DB-041252; FT-0631076; SW197667-2; A10328; C07751; D00647; AB00639976-06; AB00639976-08; AB00639976_09; 256D116; A803396; SR-01000759368; J-003271; Q3712521; SR-01000759368-4; BRD-K86887724-001-05-6; Dofetilide, United States Pharmacopeia (USP) Reference Standard
Clinical Status
Approved
Disease Indication Atrial fibrillation ICD-11: BC81 [1]
PubChem CID
71329
Formula
C19H27N3O5S2
Canonical SMILES
CN(CCC1=CC=C(C=C1)NS(=O)(=O)C)CCOC2=CC=C(C=C2)NS(=O)(=O)C
InChI
1S/C19H27N3O5S2/c1-22(13-12-16-4-6-17(7-5-16)20-28(2,23)24)14-15-27-19-10-8-18(9-11-19)21-29(3,25)26/h4-11,20-21H,12-15H2,1-3H3
InChIKey
IXTMWRCNAAVVAI-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=71329"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 441.6 Topological Polar Surface Area 122
XlogP 1.8 Complexity 672
Heavy Atom Count 29 Rotatable Bond Count 11
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Dofetilide 0.125 mg capsule 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
Butyl alcohol; Isopropyl alcohol; Magnesium stearate; Ammonia; Ferric oxide red; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Alcohol; Gelatin, unspecified; Microcrystalline cellulose; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Mayne Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Magnesium stearate; Silicon dioxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital; Greenstone; Pfizer Laboratories
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Dofetilide 0.25 mg capsule 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
Butyl alcohol; Isopropyl alcohol; Magnesium stearate; Ammonia; Ferric oxide red; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Alcohol; Gelatin, unspecified; Microcrystalline cellulose; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Mayne Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Magnesium stearate; Silicon dioxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital; Greenstone; Pfizer Laboratories
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Dofetilide 0.5 mg capsule 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
Butyl alcohol; Isopropyl alcohol; Magnesium stearate; Ammonia; Ferric oxide red; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Alcohol; Gelatin, unspecified; Microcrystalline cellulose; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Mayne Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [2]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Magnesium stearate; Silicon dioxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital; Greenstone; Pfizer Laboratories
                   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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved dofetilide from the official website of the U.S. Food and Drug Administration.
2 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
4 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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