Axelopran

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Axelopran
Axelopran structure.png
Systematic (IUPAC) name
3-[(1R,5S)-8-[2-[cyclohexylmethyl-[(2S)-2,3-dihydroxypropanoyl]amino]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]benzamide
Identifiers
CAS Number 949904-48-7
949904-50-1 (sulfate)
ATC code none
PubChem CID 67156338
ChemSpider 31444004
Chemical data
Formula C26H39N3O4
Molar mass 457.60556 g/mol
3D model (Jmol) Interactive image

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 potent, selective, and peripherally-restricted μ-, κ-, and δ-opioid receptor antagonist, 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]

See also[edit]

References[edit]

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