Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D01345)
Name
Pitolisant
Synonyms    Click to Show/Hide the Synonyms of This API
Pitolisant; 362665-56-3; TIPROLISANT; wakix; Pitolisant (BF2.649); 1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine; BF2.649; UNII-4BC83L4PIY; 1-(3-(3-(4-Chlorophenyl)propoxy)propyl)piperidine; Piperidine, 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-; 4BC83L4PIY; CHEMBL462605; HBS-101; 1-{3-[3-(4-chlorophenyl)propoxy]propyl}piperidine; Wakix (TN); 1-[3-[3-(4-Chlorophenyl)propoxy]propyl]-piperidinehydrochloride; Tirolisant; tiprolisant [USAN]; Pitolisant (USAN/INN); Pitolisant [USAN:INN]; SCHEMBL117648; GTPL8924; DTXSID30957654; CHEBI:134709; HMS3743C05; BCP13114; EX-A3601; 3973AH; BDBM50247053; MFCD18782650; ZINC34045468; AKOS028108820; BF-2649; CS-0666; DB11642; SB17037; NCGC00370823-03; AS-57273; BF-2.649; HY-12199; DB-115766; D10749; W-5790; BF2649; BF-2649; BF 2649; Pitolisant; 3-(4-Chlorophenyl)propyl 3-piperidinopropyl ether; Q426044; 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine
Clinical Status
Approved
PubChem CID
9948102
Formula
C17H26ClNO
Canonical SMILES
C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl
InChI
1S/C17H26ClNO/c18-17-9-7-16(8-10-17)6-4-14-20-15-5-13-19-11-2-1-3-12-19/h7-10H,1-6,11-15H2
InChIKey
NNACHAUCXXVJSP-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=9948102"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 295.8 Topological Polar Surface Area 12.5
XlogP 4.3 Complexity 235
Heavy Atom Count 20 Rotatable Bond Count 8
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Pitolisant 17.8 mg 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
Colloidal Silicon Dioxide; Crospovidone; Magnesium Stearate; Microcrystalline Cellulose; Polyethylene Glycol; Polyvinyl Alcohol; Talc; Titanium Dioxide
                   Dosage Form Tablet
                   Company Harmony Biosciences
                   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) [1]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [3]
          Pitolisant 4.45 mg 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
Colloidal Silicon Dioxide; Crospovidone; Magnesium Stearate; Microcrystalline Cellulose; Polyethylene Glycol; Polyvinyl Alcohol; Talc; Titanium Dioxide
                   Dosage Form Tablet
                   Company Harmony Biosciences
                   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) [1]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [3]
References
1 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
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.

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