Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23540)
Name
Rolapitant Hydrochloride eq 166.5mg base/92.5ml Emulsion
Company
Tersera
Active Pharmaceutical Ingredient (API) Rolapitant API Info click to show the detail info of this API
Functional nausea/vomiting ICD-11: DD90 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E06YUO DIG Info Disodium hydrogenorthophosphate Buffering agent ...
E05SDN DIG Info Glyceryl monolinoleate Other agent
E0X2OX DIG Info Medium-chain triglyceride Emollient ...
E0DB7F DIG Info Polyoxyl 15 hydroxystearate Emulsifying agent ...
E0T4TW DIG Info Sodium chloride Diluent ...
E0H2SC DIG Info Water Solvent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            DBT Name: Cytochrome P450 3A (CYP3A) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity Inhibition (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
            DBT Name: Albendazole monooxygenase (CYP3A4) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity EC50 = 88.3 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
            DBT Name: Cytochrome P450 2E1 (CYP2E1) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 338.6 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Cytochrome P450 2C9 (CYP2C9) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity EC50 = 123.2 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
            DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity EC50 = 839.3 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2CJ_HUMAN
            DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 147 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2D6_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Cholesterol 25-hydroxylase (CYP1A2) 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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 328.1 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.021 %(w/v) (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.29 %(w/v) (tested by experiment) [3]
                    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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.011 %(w/v) (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.00095 %(w/v) (tested by experiment) [3]
                    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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.0074 %(w/v) (tested by experiment) [3]
                    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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.0041 %(w/v) (tested by experiment) [3]
                    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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.0019 %(w/v) (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B3_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.0087 %(w/v) (tested by experiment) [3]
                    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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 1.5 %(w/v) (tested by experiment) [3]
                    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 Polyoxyl 15 hydroxystearate
                    Biological Activity IC50 = 0.0058 %(w/v) (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NTCP_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 Medium-chain triglyceride
                    Biological Activity Inhibition ratio > 36 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
References
1 In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. iopharm Drug Dispos. 2004 Jan;25(1):37-49.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.
4 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.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.