axelopran

Axelopran (TD-1211) is a peripherally acting mu-opioid receptor antagonist (PAMORA) originally developed by Theravance Biopharma. It was primarily investigated for the treatment of opioid-induced constipation (OIC), a common side effect of chronic opioid therapy. By selectively targeting mu-opioid receptors in the gastrointestinal tract, axelopran aims to alleviate constipating effects without crossing the blood-brain barrier, thereby preserving the central analgesic effects of opioids. Clinical development reached Phase 2 for OIC. More recently, the compound has been explored (potentially under the name azelirpon by Glycyx Therapeutics) for its potential to reverse opioid-induced immunodeficiency in cancer patients. This novel application aims to restore immune function and enhance the efficacy of immune checkpoint inhibitors (such as anti-PD1/PD-L1 therapies) in patients receiving opioid pain management.

Other names

azelirpon