ulimorelin

Small moleculeexperimental

Ulimorelin is a drug with a modified cyclic peptide structure which acts as a selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR-1a). Unlike many related drugs, ulimorelin has little or no effect on growth hormone (GH) release in rats. However, like ghrelin and other ghrelin agonists, ulimorelin does stimulate GH release with concomitant increases in insulin-like growth factor 1 (IGF-1) in humans. It has been researched for enhancing gastrointestinal motility, especially in gastroparesis and in aiding recovery of bowel function following gastrointestinal surgery, where opioid analgesic drugs used for post-operative pain relief may worsen existing constipation. While ulimorelin has been shown to increase both upper and lower gastrointestinal motility in rats, and showed promising results initially in humans, it failed in pivotal clinical trials in post operative ileus. — Wikipedia

Clinical trial activity

11 trials · 4 clinical orgs · 0 marketing orgs

Phase 1
5
Phase 2
6
Phase 3
3
Phase 4
0

Earliest trial started Aug 1, 2006 (NCT00639808)

Timeline

2000s

  1. Jan 1, 2006

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2007

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2011

    Earliest Phase 3 Sponsor(trial)

Indications

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1
Mol. weight
538.66 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • tzp-101
  • tzp-101
  • tzp-101
  • tzp-101
  • ulimorelin
  • ulimorelin
  • ulimorelin
  • ulimorelin
  • ulimorelin
  • ulimorelin hcl
  • ulimorelin hcl
  • ulimorelin hydrochloride
  • ulimorelin hydrochloride

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02784392Phase 2Jul 1, 2016Lyric Pharmaceuticals
NCT02993055Phase 1Jan 1, 2015Lyric Pharmaceuticals
NCT01668199Phase 1Feb 1, 2012Norgine, Quotient
NCT01710982Phase 3Feb 1, 2012Norgine
NCT01405599Phase 1Jun 1, 2011Norgine
NCT01405612Phase 1Jun 1, 2011Norgine
NCT01296620Phase 3Feb 1, 2011Norgine, Tranzyme, Inc.
NCT01285570Phase 3Jan 1, 2011Norgine, Tranzyme, Inc.
NCT00612014Phase 2Oct 1, 2007Tranzyme, Inc.
NCT00617552Phase 2Jul 1, 2007Tranzyme, Inc.
NCT00639808Phase 1Aug 1, 2006Tranzyme, Inc.
Showing 11 of 11 trials
Page 1 / 1

Organizations

Research & Development (4)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
NorgineFor profit6422011
Tranzyme, Inc.For profit5532006
Lyric PharmaceuticalsFor profit2222015
QuotientFor profit1012012
4 organizations
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