Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00722)
Name
Varenicline
Synonyms    Click to Show/Hide the Synonyms of This API
Varenicline; 249296-44-4; 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro-; CP-526555; 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)benzazepine; CHEMBL556954; 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene; 7,8,9,10-tetrahydro-6h-6,10-methanoazepino[4,5-g]quinoxaline; NCGC00247735-01; NCGC00247735-02; Varenicline (INN); CP-526,555; CHEMBL1396; SCHEMBL225687; CP 526555; Champix; Chantix; BCP01413; BDBM50166908; 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine,7,8,9,10-tetrahydro-; AKOS005145561; CS-0396; DB01273; MCULE-3341459784; SB17430; NCGC00247735-03; HY-10019; DB-015064; D08669; AB01568242_01; J-501695; Q56433825; 7,8,9,10-tetrahydro- 6,10-methano- 6H-pyrazino (2,3-h)(3) benzazepine; 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino-[2,3-h][3]benzazepine; 2-AMINO-4-(TRIFLUOROMETHYL)THIOPHENOL3-AMINO-4-MERCAPTOBENZOTRIFLUORIDE; 5,8,14-Triazatetracyclo[10.3.1.02, 11.04,9]hexadeca-2(11),3,5,7,9-pentaene; 5,8,14-Triazatetracyclo[10.3.1.02,11,04,9]hexadeca-2(11),3,5,7,9-pentaene; 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene; 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9pentaene; 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2(11),3,5,7,9-pentaene; 6,10-Methano-7,8,9,10-tetrahydro-1,4,8-triaza-6H-cyclohepta[b]naphthalene; 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine(Varenicline); 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2(11),3,5,7,9-pentaene; dihydrochloride
Clinical Status
Approved
Disease Indication Nicotine dependence ICD-11: 6C4A [1]
PubChem CID
170361
Formula
C13H13N3
Canonical SMILES
C1C2CNCC1C3=CC4=NC=CN=C4C=C23
InChI
1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2
InChIKey
JQSHBVHOMNKWFT-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=170361"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 211.26 Topological Polar Surface Area 37.8
XlogP 0.8 Complexity 254
Heavy Atom Count 16 Rotatable Bond Count 0
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Varenicline 0.5 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
Fd&c blue no. 2; Magnesium stearate; Anhydrous dibasic calcium phosphate; Titanium dioxide; Triacetin; Croscarmellose sodium; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company Avera McKennan Hospital; 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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
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
Fd&c blue no. 2; Magnesium stearate; Titanium dioxide; Triacetin; Croscarmellose sodium; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Carilion Materials Management
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
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
Magnesium stearate; Anhydrous dibasic calcium phosphate; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products; Rebel Distributors
                   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) [3]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Varenicline 1 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
Fd&c blue no. 2; Magnesium stearate; Anhydrous dibasic calcium phosphate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Aphena Pharma Solutions-Tennessee; 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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
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
Fd&c blue no. 2; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Silicon dioxide; Calcium phosphate, dibasic, anhydrous; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Carilion Materials Management
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
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
Magnesium stearate; Anhydrous dibasic calcium phosphate; Croscarmellose sodium; Silicon dioxide; Cellulose, microcrystalline
                   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
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved varenicline 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 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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