Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23578)
Name
Topotecan Hydrochloride eq 4mg base/vial injectable
Company
Novartis Pharmaceuticals Corporation
Active Pharmaceutical Ingredient (API) Topotecan API Info click to show the detail info of this API
Ovarian cancer ICD-11: 2C73 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0H0KW DIG Info Hydrochloric acid Acidulant
E0Q6DQ DIG Info Mannitol Diluent ...
E06RNC DIG Info Tartaric acid Acidulant ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Lyase/isomerase/ligase (L/I/G)
            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 Hydrochloric acid
                    Biological Activity Ki = 90000 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH4_HUMAN
            DBT Name: Carbonic anhydrase V (CA5) 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 Hydrochloric acid
                    Biological Activity Ki = 156 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH5A_HUMAN ; CAH5B_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
References
1 Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions. Bioorg Med Chem Lett. 2004 Dec 6; 14(23):5769-73.
2 Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1; 14(21):5435-9.
3 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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