Details of the Drug Formulation (DFM)

General Information of DFM (ID: F08470)
Name
Fluoxetine 20 mg capsule
Company
Clinical Solutions Wholesale; MedVantx; NCS HealthCare of KY, Inc dba Vangard Labs; RemedyRepack
Active Pharmaceutical Ingredient (API) Fluoxetine API Info click to show the detail info of this API
Major depressive disorder ICD-11: 6A70 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0A1CS DIG Info Ammonia Alkalizing agent
E0IC9H DIG Info FD&C blue no. 1 Colorant
E01UTP DIG Info Magnesium stearate lubricant
E0PC2L DIG Info Polyethylene glycol 400 Coating agent ...
E0R4JL DIG Info Polysorbate 80 Dispersing agent ...
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E0H6BT DIG Info Quinoline yellow WS Colorant
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: Serotonin receptor 2B (5HT2B) 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 FD&C blue no. 1
                    Biological Activity EC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID 5HT2B_HUMAN
            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 Polysorbate 80
                    Biological Activity IC50 = 9.3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
            DBT Name: Cannabinoid CB2 receptor (CNR2) 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 FD&C blue no. 1
                    Biological Activity EC50 = 608.6 nM (estimated based on the structural similarity with CHEMBL2326294 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.805970149
                    Tested Species Homo sapiens (Human)
                    UniProt ID CNR2_HUMAN
            DBT Name: Muscarinic receptor M1 (ACM1) 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 Polysorbate 80
                    Biological Activity IC50 = 2.6 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM1_HUMAN
            DBT Name: Muscarinic receptor M2 (ACM2) 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 Polysorbate 80
                    Biological Activity IC50 = 1.3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM2_HUMAN
            DBT Name: Alpha-2A adrenoceptor (ADA2A) 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 Quinoline yellow WS
                    Biological Activity IC50 = 28 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA2A_HUMAN
            DBT Name: Dopamine D3 receptor (DRD3) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity IC50 = 26 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD3_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 = 22 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD3_HUMAN
            DBT Name: Histamine H3 receptor (HRH3) 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 Polysorbate 80
                    Biological Activity IC50 = 5.3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID HRH3_HUMAN
            DBT Name: Thromboxane A2 receptor (TBXA2R) 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 Polysorbate 80
                    Biological Activity IC50 = 12 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TA2R_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 Polysorbate 80
                    Biological Activity IC50 = 1 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH1_HUMAN
            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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 1
                    Biological Activity IC50 = 22 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 = 2.9 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
            DBT Name: Cytochrome P450 3A (CYP3A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity Inhibition (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity Protein expression downregulation (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylene glycol
                    Biological Activity Inhibition ratio < 20 % (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity IC50 = 10.77 mg.mL-1 (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 = 201 uM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 = 400 uM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (6) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity Protein expression downregulation (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
            DBT Name: Cytochrome P450 2E1 (CYP2E1) 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 Polysorbate 80
                    Biological Activity IC50 = 225 uM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Cytochrome P450 2C9 (CYP2C9) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity EC50 = 374.2 uM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 = 40 uM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
            DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) 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 Polysorbate 80
                    Biological Activity IC50 = 118.6 uM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2CJ_HUMAN
            DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) 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 Polysorbate 80
                    Biological Activity EC50 = 486.4 uM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2D6_HUMAN
            DBT Name: Cytochrome P450 3A5 (CYP3A5) 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 Polysorbate 80
                    Biological Activity IC50 = 186.4 uM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A5_HUMAN
      Hydrolase (HDase)
            DBT Name: Acetylcholinesterase (ACHE) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 1
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACES_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACES_HUMAN
            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 Polysorbate 80
                    Biological Activity IC50 > 3 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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 1
                    Biological Activity IC50 = 28 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Primary active transporter (PAT)
            DBT Name: Multidrug resistance protein 2 (ABCC2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 67 % (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio > 73 % (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
            DBT Name: Multidrug resistance protein 1 (ABCB1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 28 % (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 64 % (tested by experiment) [12]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 = 0.31 mg.mL-1 (tested by experiment) [13]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity Inhibition ratio = 60 % (tested by experiment) [14]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity Inhibition ratio > 250 % (tested by experiment) [15]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Dopamine transporter (DAT) 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 Quinoline yellow WS
                    Biological Activity IC50 = 29 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A3_HUMAN
            DBT Name: Solute carrier SLCO2B1 (OATPB) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 1
                    Biological Activity Inhibition ratio = 80.5 % (tested by experiment) [16]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 1
                    Biological Activity Ki = 13 uM (tested by experiment) [16]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
            DBT Name: Solute carrier SLCO1A2 (OATP-A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity IC50 = 0.14 %(w/v) (tested by experiment) [17]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity IC50 = 0.05 %(w/v) (tested by experiment) [17]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity EC50 = 13156.33 nM (estimated based on the structural similarity with CHEMBL1417293 ) [18]
                    Structural Similarity Tanimoto coefficient = 0.828729282
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity IC50 = 18 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polysorbate 80
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
            DBT Name: Progesterone receptor (PGR) 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 Polysorbate 80
                    Biological Activity IC50 = 21 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PRGR_HUMAN
      Cell line (CELL)
            DBT Name: Colon cancer Caco-2 cells (Caco-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 Polysorbate 80
                    Biological Activity Chylomicron secretion upregulation (tested by experiment) [19]
                    Tested Species Homo sapiens (Human)
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation. J Med Chem. 2013 Mar 14; 56(5):2045-58.
3 In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. iopharm Drug Dispos. 2004 Jan;25(1):37-49.
4 Scientific perspectives on extending the provision for waivers of in vivo bioavailability and bioequivalence studies for drug products containing high solubility-low permeability drugs (BCS-Class 3). AAPS J. 2008 Jun;10(2):300-5.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
6 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
7 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
8 Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
9 Inhibition of human efflux transporter ABCC2 (MRP2) by self-emulsifying drug delivery system: influences of concentration and combination of excipients. J Pharm Pharm Sci. 2014;17(4):447-60.
10 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.
11 The effect of polyoxyethylene polymers on the transport of ranitidine in Caco-2 cell monolayers. Int J Pharm. 2011 May 16;409(1-2):164-8.
12 Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm. 2006 Apr 26;313(1-2):49-56.
13 Reversal of multidrug resistance by surfactants. Br J Cancer. 1992 Jul;66(1):62-8.
14 A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci. 2002 Sep;91(9):1991-2002.
15 Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release. 2007 Dec 4;124(1-2):1-5.
16 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
17 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.
18 PubChem BioAssay data set.
19 Stimulation of triglyceride-rich lipoprotein secretion by polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model. Pharm Res. 2004 Dec;21(12):2320-6.

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