Repositioning Candidate Details
| Candidate ID: | R1104 |
| Source ID: | DB06800 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Methylnaltrexone |
| Synonyms: | MNTX |
| Molecular Formula: | C21H26NO4 |
| SMILES: | C[N@+]1(CC2CC2)CC[C@]23[C@H]4OC5=C(O)C=CC(C[C@@H]1[C@]2(O)CCC4=O)=C35 |
| Structure: |
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| DrugBank Description: | Methylnaltrexone is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation without producing analgesic effects or withdrawal symptoms. It is also a weak CYP2D6 inhibitor. FDA approved in 2008. |
| CAS Number: | 916055-93-1 |
| Molecular Weight: | 356.441 |
| DrugBank Indication: | Treatment of opioids induced constipation in palliative patients that are inadequately responding to laxative therapy. |
| DrugBank Pharmacology: | Use of opioids induces slowing of gastrointestinal motility and transit. Following remifentanil administration, the methylnaltrexone and placebo groups showed no change in pupiliary constriction while the naloxone group showed a marked change over the time interval tested. |
| DrugBank MoA: | Methylnaltrexone is a pheriphally-acting μ-opioid antagonists that acts on the gastrointestinal tract inhibit opioid-induced decrease in gastric motility and transit time. Because methylnaltrexone is a quaternary derivative of naltrexone, it produces its gastrointestinal effects without producing analgesic effects or withdrawal symptoms as it does not cross the blood-brain-barrier. |
| Targets: | Mu-type opioid receptor antagonist; Kappa-type opioid receptor antagonist |
| Inclusion Criteria: | Indication associated |

| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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