methylsamidorphan

Methylsamidorphan (previously known as ALKS 37) is an orally active, peripherally restricted opioid receptor antagonist developed by Alkermes for the treatment of opioid-induced bowel dysfunction (OBD), including opioid-induced constipation. The drug was designed to improve gastrointestinal motility in patients taking opioid analgesics by blocking peripheral opioid receptors in the gut without affecting central analgesia or causing significant systemic exposure. Clinical studies demonstrated that methylsamidorphan increased bowel movements and improved GI motility while preserving pain relief from opioids. However, development was discontinued after phase 2 trials due to not meeting pre-specified efficacy criteria for advancement[1][2][3][4][5].

Other names

methylsamidorphan