Repositioning Candidate Details
| Candidate ID: | R0852 |
| Source ID: | DB05719 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Elesclomol |
| Synonyms: | 1-N'-Benzenecarbothioyl-3-(2-benzenecarbothioyl-2-methylhydrazinyl)-N'-methyl-oxopropanehydrazidide |
| Molecular Formula: | C19H20N4O2S2 |
| SMILES: | CN(NC(=O)CC(=O)NN(C)C(=S)C1=CC=CC=C1)C(=S)C1=CC=CC=C1 |
| Structure: |
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| DrugBank Description: | Elesclomol is a novel, injectable, drug candidate that kills cancer cells by elevating oxidative stress levels beyond a breaking point, triggering programmed cell death. In preclinical models elesclomol showed potent killing of a broad range of cancer cell types at high doses, and an ability to strongly enhance the efficacy of certain chemotherapy agents, with minimal additional toxicity, at moderate doses. It is being developed by Synta Pharmaceuticals. |
| CAS Number: | 488832-69-5 |
| Molecular Weight: | 400.518 |
| DrugBank Indication: | Investigated for use/treatment in melanoma. |
| DrugBank Pharmacology: | Elesclomol is a first-in-class heat shock protein 70 (Hsp70) inducer that activates natural killer (NK) cell-mediated tumor killing. |
| DrugBank MoA: | Elesclomol acts through a novel mechanism of action. Elesclomol has been shown to rapidly cause a dramatic increase in oxidative stress (ROS) inside cancer cells. The prolonged elevation of ROS inside cancer cells induced by elesclomol causes the cell to exceed a critical breaking point and undergo apoptosis. The triggering of the mitochondrial apoptosis pathway is observed within the first six hours of applying elesclomol. Cancer cells operate at a much higher intrinsic level of ROS than normal cells, and have a greatly reduced anti-oxidant capacity compared to normal cells. This leaves them more vulnerable to an agent such as elesclomol that elevates oxidative stress. In similar experiments at similar doses, elesclomol has been found to have little to no impact on normal cells. |
| Targets: | -- |
| Inclusion Criteria: | Therapeutic strategy associated |
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