Repositioning Candidate Details
| Candidate ID: | R0137 |
| Source ID: | DB00488 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Altretamine |
| Synonyms: | |
| Molecular Formula: | C9H18N6 |
| SMILES: | CN(C)C1=NC(=NC(=N1)N(C)C)N(C)C |
| Structure: |
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| DrugBank Description: | An alkylating agent proposed as an antineoplastic. It also acts as a chemosterilant for male houseflies and other insects. |
| CAS Number: | 645-05-6 |
| Molecular Weight: | 210.2794 |
| DrugBank Indication: | For use as a single agent in the palliative treatment of patients with persistent or recurrent ovarian cancer following first-line therapy with a cisplatin and/or alkylating agent-based combination. |
| DrugBank Pharmacology: | Altretamine is a novel antineoplastic agent. The precise mechanism by which altretamine exerts its cytotoxic effect is unknown, although a number of theoretical possibilities have been studied. Structurally, altretamine resembles the alkylating agent triethylenemelamine, yet <i>in vitro</i> tests for alkylating activity of altretamine and its metabolitics have been negative. Altretamine has been demonstrated to be efficacious for certain ovarian tumors resistant to classical alkylating agents. Metabolism of altretamine is a requirement of cytotoxicity. Synthetic monohydroxymethylmelamines, and products of altretamine metabolism, <i>in vitro</i> and <i>in vivo</i>, can form covalent adducts with tissue macromolecules including DNA, but the relevance of these reactions to antitumor activity is unknown. |
| DrugBank MoA: | The precise mechanism by which altretamine exerts its cytotoxic effect is unknown although it is classified as an alkylating anti-neoplastic agent. Through this mechanism, the drug is metabolized into alkylating agents by N-demethylation. These alkylating species consequently damage tumor cells. |
| Targets: | DNA |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
|---|
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name | |
|---|---|---|---|---|---|---|---|
| T03 | Angiotensin-converting enzyme | ACE | INHIBITOR | Target is a single protein chain | P12821 | ACE_HUMAN | Details |
| T47 | Sialin | SLC17A5 | Target is a single protein chain | Q9NRA2 | SLC17A5_HUMAN | Details | |
| T22 | Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 | ENPP1 | Target is a single protein chain | P22413 | ENPP1_HUMAN | Details | |
| T23 | Polycystin-1 | PKD1 | Target is a single protein chain | P98161 | PKD1_HUMAN | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I02 | 1184 | nephrotic syndrome | "A nephrosis characterized by marked increase in glomerular protein permeability resulting in marked elevation of urine protein levels, hypoalbuminemia, hyperlipidemia, and hypercoagulability." [url:https\://en.wikipedia.org/wiki/Nephrotic_syndrome, url:https\://www.niddk.nih.gov/health-information/kidney-disease/nephrotic-syndrome-adults] | Details |