Axelopran

Axelopran (INN, USAN) (developmental code name TD-1211) is a drug which is under development by Theravance Biopharma for the treatment of opioid-induced constipation. It acts as a peripherally acting μ-opioid receptor antagonist and also acts on κ-, and δ-opioid receptors, with similar affinity for the μ- and κ-opioid receptors and about an order of magnitude lower affinity for the δ-opioid receptor. Axelopran has potent μ-opioid receptor antagonist activity on the gastrointestinal tract in vivo, and thus it produces a dose-dependent inhibition of opioid-induced delaying in gastric emptying in mice and rats following subcutaneous or oral administration.[1]

Axelopran
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
KEGG
Chemical and physical data
FormulaC26H39N3O4
Molar mass457.60556 g/mol g·mol−1
3D model (JSmol)

See also

References
  1. , Axelopran (td-1211) briefing document anesthetic and analgesic drug products advisory committee June 11 and 12, 2014.



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