Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23278)
Name
Risdiplam 0.75 mg/ml powder
Company
Genentech
Active Pharmaceutical Ingredient (API) Risdiplam API Info click to show the detail info of this API
Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0S7FK DIG Info Ascorbic acid Acidulant ...
E0FY2S DIG Info Edetate disodium Complexing agent
E0DW0Y DIG Info Isomalt Binding agent ...
E0Q6DQ DIG Info Mannitol Diluent ...
E09BYS DIG Info Polyethylene glycol 6000 Coating agent ...
E0Y7PW DIG Info Sodium benzoate Antimicrobial preservative ...
E04KTP DIG Info Sucralose Flavoring agent
E06RNC DIG Info Tartaric acid Acidulant ...
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 Ascorbic acid
                    Biological Activity IC50 = 4.1 mg.mL-1 (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 Polyethylene glycol 6000
                    Biological Activity Inhibition ratio < 70 % (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase II (CA2) 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 Sucralose
                    Biological Activity Ki = 300 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sodium benzoate
                    Biological Activity Ki = 30000 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
            DBT Name: Carbonic anhydrase IV (CA4) 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 benzoate
                    Biological Activity Ki = 74700 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH4_HUMAN
            DBT Name: Carbonic anhydrase IX (CA9) 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 Sucralose
                    Biological Activity Ki = 2200 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH9_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 ) [4]
                    Structural Similarity Tanimoto coefficient = 0.804878049
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_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 Isomalt
                    Biological Activity EC50 = 99390 nM (estimated based on the structural similarity with CHEMBL4539030 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.979166667
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0025
References
1 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
2 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.
3 Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):573-8.
4 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
5 Novel natural compounds from endophytic fungi with anticancer activity. Eur J Med Chem. 2018 Aug 5; 156:316-343.

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