Repositioning Candidate Details
| Candidate ID: | R0937 |
| Source ID: | DB06176 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Romidepsin |
| Synonyms: | Romidepsin |
| Molecular Formula: | C24H36N4O6S2 |
| SMILES: | C\C=C1/NC(=O)[C@H]2CSSCC\C=C\[C@H](CC(=O)N[C@H](C(C)C)C(=O)N2)OC(=O)[C@@H](NC1=O)C(C)C |
| Structure: |
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| DrugBank Description: | Romidepsin is a selective inhibitor of histone deacetylase, approved in the US in 2009 for the treatment of cutaneous T-cell lymphoma (CTCL) or/and peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior systemic therapy. These indications are based on response rate. Clinical benefit such as improvement in overall survival has not been demonstrated. |
| CAS Number: | 128517-07-7 |
| Molecular Weight: | 540.69 |
| DrugBank Indication: | For the treatment of cutaneous T-cell lymphoma (CTCL) or/and peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior systemic therapy. These indications are based on response rate. Clinical benefit such as improvement in overall survival has not been demonstrated. |
| DrugBank Pharmacology: | -- |
| DrugBank MoA: | Romidepsin is a prodrug, where it becomes active once taken up into the cell. The active metabolite has a free thiol group, which interacts with zinc ions in the active site of class 1 and 2 HDAC enzymes, resulting in inhibition of its enzymatic activity. Certain tumors have over expressed HDACs and downregulated/mutated histone acetyltransferases. This imbalance of HDAC relative to histone acetyltransferase can lead to a decrease in regulatory genes, ensuing tumorigenesis. Inhibition of HDAC may restore normal gene expression in cancer cells and result in cell cycle arrest and apoptosis. |
| Targets: | Histone deacetylase 1 antagonist&inhibitor; Histone deacetylase 2 antagonist&inhibitor; Histone deacetylase 4 inhibitor; Histone deacetylase 6 inhibitor; Multidrug resistance-associated protein 1 |
| Inclusion Criteria: | Therapeutic strategy associated |
