Details of the Drug Formulation (DFM)

General Information of DFM (ID: F24151)
Name
Telavancin Hydrochloride eq 750mg base/vial powder
Company
Cumberland Pharms
Active Pharmaceutical Ingredient (API) Telavancin hydrochloride 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
E09IKE DIG Info Hydroxyethyl-beta-cyclodextrin Other agent
E0Q6DQ DIG Info Mannitol Diluent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO1B1 (OATP-C) 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 Hydroxyethyl-beta-cyclodextrin
                    Biological Activity IC50 = 0.24 %(w/v) (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B1_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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hydroxyethyl-beta-cyclodextrin
                    Biological Activity IC50 = 0.01 %(w/v) (tested by experiment) [1]
                    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 Hydroxyethyl-beta-cyclodextrin
                    Biological Activity IC50 = 0.027 %(w/v) (tested by experiment) [1]
                    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 Hydroxyethyl-beta-cyclodextrin
                    Biological Activity IC50 = 0.025 %(w/v) (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_HUMAN
            DBT Name: Organic anion transporter 8 (OAT8) 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 Hydroxyethyl-beta-cyclodextrin
                    Biological Activity IC50 = 0.001 %(w/v) (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B3_HUMAN
            DBT Name: Sodium/bile acid cotransporter (SLC10A1) 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 Hydroxyethyl-beta-cyclodextrin
                    Biological Activity EC50 = 0.52 %(w/v) (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NTCP_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hydroxyethyl-beta-cyclodextrin
                    Biological Activity IC50 = 4.6 %(w/v) (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NTCP_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 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.804878049
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_HUMAN
References
1 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.
2 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.

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