Details of the Drug Formulation (DFM)

General Information of DFM (ID: F19348)
Name
Rizatriptan 10 mg tablet
Company
Bionpharma; Panacea Biotec
Active Pharmaceutical Ingredient (API) Rizatriptan API Info click to show the detail info of this API
Migraine ICD-11: 8A80 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0BI3X DIG Info Aspartame Flavoring agent
E0Q8ZK DIG Info Calcium hydrogenphosphate Diluent
E0PE9M DIG Info Crospovidone Disintegrant
E0N2PK DIG Info Isopropyl alcohol Antimicrobial preservative ...
E00DHW DIG Info Lactose monohydrate Binding agent ...
E0Q6DQ DIG Info Mannitol Diluent ...
E09ZXG DIG Info Menthol Flavoring agent
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0RS6F DIG Info Sodium stearyl fumarate lubricant
E0V5AX DIG Info Xylitol Coating agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            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 Calcium hydrogenphosphate
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    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 Crospovidone
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    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 Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Matrix metalloproteinase-1 (MMP1) 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 Aspartame
                    Biological Activity IC50 = 20000 nM (estimated based on the structural similarity with CHEMBL62186 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.916666667
                    Tested Species Homo sapiens (Human)
                    UniProt ID MMP1_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Glycine receptor alpha-1 (GLRA1) 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 Mannitol
                    Biological Activity EC50 = 12589.25 nM (estimated based on the structural similarity with CHEMBL604608 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.804878049
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_HUMAN
            DBT Name: Wasabi receptor (TRPA1) 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 Menthol
                    Biological Activity EC50 = 30000 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPA1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Menthol
                    Biological Activity EC50 = 56000 nM (tested by experiment) [5]
                    Tested Species Mus musculus (Mouse)
                    UniProt ID TRPA1_MOUSE
            DBT Name: Transient receptor potential p8 (TRPM8) 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 Menthol
                    Biological Activity EC50 = 3000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPM8_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Menthol
                    Biological Activity EC50 = 75000 nM (tested by experiment) [7]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID TRPM8_RAT
      Nuclear receptor (NR)
            DBT Name: Pregnane X receptor (NR1I2) 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 Aspartame
                    Biological Activity Ki = 13 uM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NR1I2_HUMAN
      Cell line (CELL)
            DBT Name: Leukemia K562 cells (K562) 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 Sodium stearyl fumarate
                    Biological Activity IC50 = 20.2 ug.mL-1 (estimated based on the structural similarity with CHEMBL3126829 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.75
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0004
            DBT Name: Breast cancer MCF7 cells (MCF7) 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 Sodium stearyl fumarate
                    Biological Activity IC50 = 60 ug.mL-1 (estimated based on the structural similarity with CHEMBL3126829 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.75
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0031
            DBT Name: Lymphoma P388/ADR cells (P388/ADR) 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 Isopropyl alcohol
                    Biological Activity IC50 = 0.22 uM (estimated based on the structural similarity with CHEMBL545 ) [10]
                    Structural Similarity Tanimoto coefficient = 0.789473684
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_IZ75
References
1 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
2 Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket. Bioorg Med Chem Lett. (1997) 7:193-198.
3 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
4 N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites. Eur J Med Chem. 2019 May 15; 170:141-156.
5 Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents. J Med Chem. 2010 Jul 22; 53(14):5085-107.
6 Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists. Bioorg Med Chem Lett. 2013 Nov 15; 23(22):6118-22.
7 Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators. J Med Chem. 2016 Mar 10; 59(5):2179-91.
8 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
9 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.
10 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.

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