methylnaltrexone

Methylnaltrexone is a peripherally acting mu-opioid receptor antagonist (PAMORA) developed for the treatment of opioid-induced constipation (OIC). It is a quaternary ammonium derivative of naltrexone, which restricts its ability to cross the blood-brain barrier, thereby allowing it to selectively antagonize mu-opioid receptors in the gastrointestinal tract. This mechanism alleviates constipation caused by opioids without compromising their central analgesic effects. Chia Tai Tianqing Pharmaceutical Group developed a subcutaneous formulation of methylnaltrexone bromide, which has been evaluated in clinical trials for patients with advanced illness and received approval from the China National Medical Products Administration (NMPA) in 2021.

Brand names

Jiexin

Other names

methylnaltrexone bromideMNTX