Details of the Drug Formulation (DFM)

General Information of DFM (ID: F13608)
Name
Methylphenidate 36 mg tablet
Company
Mallinckrodt
Active Pharmaceutical Ingredient (API) Methylphenidate API Info click to show the detail info of this API
Attention deficit hyperactivity disorder ICD-11: 6A05 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09YYN DIG Info Eisenoxyd Colorant
E02FBG DIG Info Ferrosoferric oxide Colorant
E01UTP DIG Info Magnesium stearate lubricant
E0X2OX DIG Info Medium-chain triglyceride Emollient ...
E0R0WE DIG Info Oleic acid Emulsifying agent ...
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0QY1F DIG Info Talc Anticaking agent ...
E05BSD DIG Info Titanium dioxide Coating agent ...
E0T2AJ DIG Info Triacetin Humectant ...
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 Oleic acid
                    Biological Activity IC50 = 12 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_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 Oleic acid
                    Biological Activity IC50 = 13 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM1_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 Oleic acid
                    Biological Activity IC50 = 25 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TA2R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Aromatase (ARO1) 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 Oleic acid
                    Biological Activity IC50 = 32700 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP19A_HUMAN
            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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Oleic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [3]
                    Tested Species Bos taurus (Bovine)
                    UniProt ID PGH1_BOVIN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Oleic acid
                    Biological Activity IC50 = 6.7 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 Oleic acid
                    Biological Activity IC50 > 500000 nM (tested by experiment) [3]
                    Tested Species Ovis aries (Sheep)
                    UniProt ID PGH2_SHEEP
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Oleic acid
                    Biological Activity IC50 = 3.5 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_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) [4]
                    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) [5]
                    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 Oleic acid
                    Biological Activity Inhibition ratio < 20 % (tested by experiment) [4]
                    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 Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Transferase (TFase)
            DBT Name: Telomerase reverse transcriptase (TERT) 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 Oleic acid
                    Biological Activity IC50 = 8600 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TERT_HUMAN
      Hydrolase (HDase)
            DBT Name: Proconvertin-TF complex (F7-F3) 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 Oleic acid
                    Biological Activity IC50 = 80000 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FA7_HUMAN ; TF_HUMAN
            DBT Name: Trypsin (PRSS) 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 Oleic acid
                    Biological Activity IC50 > 200000 nM (tested by experiment) [7]
                    Tested Species Sus scrofa (Pig)
                    UniProt ID TRYP_PIG
      Primary active transporter (PAT)
            DBT Name: Urate exporter (BCRP) 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 Oleic acid
                    Biological Activity Inhibition ratio > 60 % (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ABCG2_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Norepinephrine transporter (NET) 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 Oleic acid
                    Biological Activity IC50 = 27 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A2_HUMAN
            DBT Name: Monoamine transporter VAT2 (VMAT2) 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 Oleic acid
                    Biological Activity Ki = 4.7 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID VMAT2_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Vanilloid receptor 2 (TrpV2) 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 Oleic acid
                    Biological Activity IC50 > 10000 nM (tested by experiment) [9]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID TRPV2_RAT
      Nuclear receptor (NR)
            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 Oleic acid
                    Biological Activity IC50 = 600 nM (tested by experiment) [10]
                    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 Oleic acid
                    Biological Activity IC50 = 5300 nM (tested by experiment) [10]
                    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 Oleic acid
                    Biological Activity IC50 = 4100 nM (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PPARG_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 Oleic acid
                    Biological Activity IC50 = 12 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PRGR_HUMAN
      Other protein families (OPF)
            DBT Name: Adipocyte lipid-binding protein (ALBP) 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 Oleic acid
                    Biological Activity Ki = 1500 nM (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID FABP4_HUMAN
            DBT Name: Liver lipid-binding protein (L-FABP) 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 Oleic acid
                    Biological Activity Ki = 180 nM (tested by experiment) [12]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID FABPL_RAT
      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 Medium-chain triglyceride
                    Biological Activity Inhibition ratio > 36 % (tested by experiment) [13]
                    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 Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay. J Nat Prod. 2006 Apr; 69(4):700-3.
3 Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun; 64(6):745-9.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 Natural products targeting telomere maintenance. Med Chem Comm. (2011) 2:229-245.
7 Inhibitory activity of unsaturated fatty acids and anacardic acids toward soluble tissue factor-factor VIIa complex. J Nat Prod. 1998 Nov; 61(11):1352-5.
8 Oleic acid decreases BCRP mediated efflux of mitoxantrone in Caco-2 cell monolayers. Food Chem Toxicol. 2012 Oct;50(10):3635-45.
9 Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists. J Med Chem. 2018 Sep 27; 61(18):8255-8281.
10 Molecular properties of fatty acids related to PPAR binding and metabolic diseases. Med Chem Res (2013) 22:3126-3133.
11 The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation. Bioorg Med Chem. 2016 Sep 15; 24(18):4310-4317.
12 Characterization of the drug binding specificity of rat liver fatty acid binding protein. J Med Chem. 2008 Jul 10; 51(13):3755-64.
13 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.

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