ulimorelin
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
Earliest trial started Aug 1, 2006 (NCT00639808)
Timeline
Indications
Mechanism of action
- Ghrelin receptorAGONIST
GHSR agonist
Chemistry & pharmacology
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
- ChEMBLCHEMBL1963249 ↗
- WikipediaUlimorelin ↗
- NCATSK2X1EE8C73 ↗
- ChEMBLCHEMBL1923502 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02784392 | Phase 2 | Jul 1, 2016 | Lyric Pharmaceuticals |
| NCT02993055 | Phase 1 | Jan 1, 2015 | Lyric Pharmaceuticals |
| NCT01668199 | Phase 1 | Feb 1, 2012 | Norgine, Quotient |
| NCT01710982 | Phase 3 | Feb 1, 2012 | Norgine |
| NCT01405599 | Phase 1 | Jun 1, 2011 | Norgine |
| NCT01405612 | Phase 1 | Jun 1, 2011 | Norgine |
| NCT01296620 | Phase 3 | Feb 1, 2011 | Norgine, Tranzyme, Inc. |
| NCT01285570 | Phase 3 | Jan 1, 2011 | Norgine, Tranzyme, Inc. |
| NCT00612014 | Phase 2 | Oct 1, 2007 | Tranzyme, Inc. |
| NCT00617552 | Phase 2 | Jul 1, 2007 | Tranzyme, Inc. |
| NCT00639808 | Phase 1 | Aug 1, 2006 | Tranzyme, Inc. |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Norgine | For profit | 6 | 4 | 2 | 2011 |
| Tranzyme, Inc. | For profit | 5 | 5 | 3 | 2006 |
| Lyric Pharmaceuticals | For profit | 2 | 2 | 2 | 2015 |
| Quotient | For profit | 1 | 0 | 1 | 2012 |