Details of the Drug Formulation (DFM)

General Information of DFM (ID: F16469)
Name
Paliperidone 6 mg tablet
Company
Janssen Pharmaceutical; Patriot Pharmaceuticals
Active Pharmaceutical Ingredient (API) Paliperidone API Info click to show the detail info of this API
Bipolar disorder ICD-11: 6A60 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0J0LX DIG Info Butylated hydroxytoluene Antioxidant
E02FBG DIG Info Ferrosoferric oxide Colorant
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E0T4TW DIG Info Sodium chloride Diluent ...
E06VNY DIG Info Stearic acid Emulsifying agent ...
E05BSD DIG Info Titanium dioxide Coating agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Adenosine receptor A3 (AA3R) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Prostaglandin G/H synthase 1 (COX-1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [2]
                    Tested Species Bos taurus (Bovine)
                    UniProt ID PGH1_BOVIN
            DBT Name: Prostaglandin G/H synthase 2 (COX-2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [2]
                    Tested Species Ovis aries (Sheep)
                    UniProt ID PGH2_SHEEP
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylene glycol
                    Biological Activity Inhibition ratio < 20 % (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Phosphodiesterase 3A (PDE3A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 3.1 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE3A_HUMAN
            DBT Name: Phosphodiesterase 4D (PDE4D) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 6.7 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase I (CA1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylated hydroxytoluene
                    Biological Activity Ki = 245200 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH1_HUMAN
            DBT Name: Carbonic anhydrase II (CA2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylated hydroxytoluene
                    Biological Activity Ki = 630 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
      Nuclear receptor (NR)
            DBT Name: Estrogen receptor alpha (ESR1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 16 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
            DBT Name: PPAR-alpha (PPARA) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 1100 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARA_HUMAN
            DBT Name: PPAR-delta (PPARD) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 6000 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARD_HUMAN
            DBT Name: PPAR-gamma (PPARG) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 = 30000 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARG_HUMAN
      Cell line (CELL)
            DBT Name: Colon cancer COLO 205 cells (COLO 205) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 200000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0218
            DBT Name: Colon cancer HT-29 cells (HT-29) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Stearic acid
                    Biological Activity IC50 > 200000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0320
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun; 64(6):745-9.
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 Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols. Bioorg Med Chem. 2009 Apr 15; 17(8):3207-11.
5 Molecular properties of fatty acids related to PPAR binding and metabolic diseases. Med Chem Res (2013) 22:3126-3133.
6 Liposomal formulation of retinoids designed for enzyme triggered release. J Med Chem. 2010 May 13; 53(9):3782-92.

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