Details of the Drug Formulation (DFM)

General Information of DFM (ID: F19367)
Name
Rizatriptan 5 mg tablet
Company
Breckenridge Pharmaceutical
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
E02WLG DIG Info Aminoethanoic acid Buffering agent ...
E0BI3X DIG Info Aspartame Flavoring agent
E03SQI DIG Info Carmellose sodium Disintegrant
E0PE9M DIG Info Crospovidone Disintegrant
E01UTP DIG Info Magnesium stearate lubricant
E0Q6DQ DIG Info Mannitol Diluent ...
E0V3GR DIG Info Monosodium citrate Acidulant ...
E0T4TW DIG Info Sodium chloride Diluent ...
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 Magnesium stearate
                    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 Carmellose sodium
                    Biological Activity Protein expression upregulation (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 Carmellose sodium
                    Biological Activity Protein expression upregulation (tested by experiment) [1]
                    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 Crospovidone
                    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
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Serine racemase (SRR) 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 Aminoethanoic acid
                    Biological Activity Ki = 366000 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SRR_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Glycine type-1 transporter (GlyT-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 Aminoethanoic acid
                    Biological Activity IC50 = 31600 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A9_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Glutamate receptor NMDA (GRIN) 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 Aminoethanoic acid
                    Biological Activity Ki = 125.89 nM (tested by experiment) [5]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID NMDZ1_RAT ; NMDE1_RAT ; NMDE2_RAT ; NMDE3_RAT ; NMDE4_RAT ; NMD3A_RAT ; NMD3B_RAT
            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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Aminoethanoic acid
                    Biological Activity EC50 = 94000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_HUMAN
               Experiment (2) 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 ) [7]
                    Structural Similarity Tanimoto coefficient = 0.804878049
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_HUMAN
      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
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 In silico and pharmacological screenings identify novel serine racemase inhibitors. Bioorg Med Chem Lett. 2014 Aug 15; 24(16):3732-5.
4 Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead. Bioorg Med Chem Lett. 2014 Feb 15; 24(4):1067-70.
5 Drug design, in vitro pharmacology, and structure-activity relationships of 3-acylamino-2-aminopropionic acid derivatives, a novel class of partial agonists at the glycine site on the N-methyl-D-aspartate (NMDA) receptor complex. J Med Chem. 2009 Aug 27; 52(16):5093-107.
6 Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor. J Med Chem. 2007 Sep 20; 50(19):4616-29.
7 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
8 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.

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