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axelopran

Small moleculeexperimental

Axelopran is a drug which is under development by Theravance Biopharma and licensed to Glycyx for all indications. 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. Recent data suggests that μ-opioid antagonists have a direct effect on overall survival in patients with advanced cancer. — Wikipedia

Clinical trial activity

7 trials · 1 clinical orgs · 0 marketing orgs

Phase 1
4
Phase 2
4
Phase 3
0
Phase 4
0

Earliest trial started Jan 1, 2010 (NCT01040637)

Timeline

2010s

  1. Jan 1, 2010

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2011

    Earliest Phase 2 Sponsor(trial)

Indications

Studied for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

NC(=O)c1cccc([C@H]2C[C@H]3CC[C@@H](C2)N3CCN(CC2CCCCC2)C(=O)[C@@H](O)CO)c1
Mol. weight
457.62 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 3-(8-(2-(cyclohexylmethyl(2,3-dihydroxypropionyl)amino)ethyl)-8-azabicyclo(3.2.1)oct-3-yl)benzamide
  • 3-endo-(8-(2-(cyclohexylmethyl-((s)-2,3-dihydroxypropionyl)amino)ethyl)-8-azabicyclo(3.2.1)oct-3-yl)benzamide
  • axelopran
  • axelopran
  • axelopran
  • td-1211
  • td-1211
  • td-1211
  • td-1211

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT01702194Phase 1Nov 1, 2012Theravance
NCT01655771Phase 1Aug 1, 2012Theravance
NCT01568411Phase 1Apr 1, 2012Theravance
NCT01459926Phase 2Nov 1, 2011Theravance
NCT01401985Phase 2Oct 1, 2011Theravance
NCT01333540Phase 2May 1, 2011Theravance
NCT01040637Phase 1/Phase 2 (Phase 2)Jan 1, 2010Theravance
Showing 7 of 7 trials
Page 1 / 1

Organizations

Research & Development (1)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
TheravanceFor profit7722010
1 organizations
Page 1 / 1