Repositioning Candidate Details
| Candidate ID: | R1475 |
| Source ID: | DB13145 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Nedaplatin |
| Synonyms: | (glycolato-O,O')diammineplatinum(II); CDGP; cis-Diammine (glycolato)platinum; cis-diammine(glycolato)platinum; cis-Diammine(glycolato)platinum(II); Nedaplatin |
| Molecular Formula: | C2H8N2O3Pt |
| SMILES: | [H][N]([H])([H])[Pt]1(OCC(=O)O1)[N]([H])([H])[H] |
| DrugBank Description: | Nedaplatin is a second generation platinum analog . It is less nephrotoxic than but has proven equally effective. It was approved for use in Japan in 1995. |
| CAS Number: | 95734-82-0 |
| Molecular Weight: | 303.181 |
| DrugBank Indication: | Used in the treatment of non-small cell lung cancer, small cell lung cancer, oesophygeal cancer, and head and neck cancers . |
| DrugBank Pharmacology: | Nedaplatin damages DNA and induces cell death in cancer cells . It also functions as a radiosensitizer, increasing the susceptibility of the affected cells to radiation therapy . |
| DrugBank MoA: | As a platinum analog, nedaplatin likely works similarly to on which the following mechanistic description is based. Once it has entered the cell it is hydrolyzed to its active form which complexes with water molecules . This form binds to to nucleophiles in the cytoplasm such as glutathione and other cyteine rich proteins resulting in an overall increase in oxidative stress as the cell loses antioxidant proteins. It also binds to purine nucleotides in the DNA. The active form allows for two binding interactions to form cross-links between these nucleotides. High mobility group proteins-1 and -2 induce apoptosis in response to guanine cross-links and their binding serves to shield the cross-linked DNA from repair mechanisms. The mismatch repair (MMR) protein complex also recognizes the distortion caused by platinum complexes and attempts to repair the DNA. This results in single strand breaks when the MMR complex attempts to remove the platinum cross-link. The MMR complex induces apoptosis after the repair attempt has failed. The single strand break in DNA makes it easier to form lethal double strand breaks with radiation treatment thus creating the radiosensitizing effect of nedaplatin . |
| Targets: | Glutathione ligand; DNA ligand |
| Inclusion Criteria: | Therapeutic strategy associated |
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