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methylnaltrexone + naloxone
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MNTX + NLX refers to the investigation of methylnaltrexone (MNTX) and naloxone (NLX) in the context of opioid-induced constipation (OIC), specifically within a Phase 1 clinical trial conducted by University Medicine Greifswald. This study compared the effects of extended-release formulations of these two opioid antagonists on gastrointestinal transit times. Methylnaltrexone is a peripherally acting mu-opioid receptor antagonist (PAMORA) that does not cross the blood-brain barrier, thereby reversing opioid-induced bowel dysfunction without interfering with central analgesia. Naloxone is a non-selective opioid antagonist that, when administered orally, targets enteric opioid receptors due to high first-pass metabolism. The research aimed to characterize the pharmacokinetics and pharmacodynamics of these agents using a loperamide-induced constipation model in healthy volunteers.
- Other names
- methylnaltrexone bromide + naloxone hydrochlorideMNTX + NLX
02
Targets
KOR (Kappa opioid receptor)FLNA (Filamin A)DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)
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