Methylnaltrexone
- Generic Name
- Methylnaltrexone
- Brand Names
- Relistor
- Drug Type
- Small Molecule
- Chemical Formula
- C21H26NO4
- CAS Number
- 916055-93-1
- Unique Ingredient Identifier
- 0RK7M7IABE
- Background
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.
- Indication
Treatment of opioids induced constipation in palliative patients that are inadequately responding to laxative therapy.
- Associated Conditions
- Opioid Induced Constipation (OIC)
ANI Pharmaceuticals Launches Prucalopride Tablets for Chronic Idiopathic Constipation with 180-Day Exclusivity
• ANI Pharmaceuticals has launched Prucalopride Tablets, a generic version of Motegrity, after receiving FDA approval and a Competitive Generic Therapy (CGT) designation.
• Prucalopride, a selective 5-HT4 receptor agonist, enhances colon muscle movement to alleviate infrequent bowel movements in adults with chronic idiopathic constipation.
• Clinical trials have demonstrated prucalopride's efficacy and safety in treating chronic constipation, showing a higher proportion of patients achieving at least 3 spontaneous bowel movements per week compared to placebo.
• Real-world studies suggest prucalopride has higher treatment persistence and adherence compared to other prescription medications for chronic idiopathic constipation.
PAMORAs Enhance Immunotherapy Efficacy by Blocking Opioid-Induced Immunosuppression in Cancer
• New research indicates that opioids can suppress the immune system, reducing the effectiveness of immunotherapy in cancer treatment.
• Peripherally restricted OPRM1 antagonists (PAMORAs) can block opioid-induced immunosuppression, improving response rates to immune checkpoint inhibitors.
• The study found that morphine suppresses CD8 T cell activity by binding to OPRM1, counteracting the effects of anti-PD1 therapy.
• PAMORAs like methylnaltrexone and axelopran, when combined with morphine, effectively blocked immunosuppression, allowing anti-PD1 therapy to work in mice.
Drug Development Updates
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