relamorelin
Relamorelin is a synthetic peptide, centrally penetrant, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) which is under development by Allergan pharmaceuticals for the treatment of diabetic gastroparesis, chronic idiopathic constipation, and anorexia nervosa. It is a pentapeptide and an analogue of ghrelin with improved potency and pharmacokinetics. In humans, relamorelin produces increases in plasma growth hormone, prolactin, and cortisol levels, and, like other GHSR agonists, increases appetite. As of June 2015, relamorelin is in phase II clinical trials for diabetic gastroparesis and constipation. The United States Food and Drug Administration (FDA) has granted Fast Track designation to relamorelin for diabetic gastroparesis. The development of the drug is uncertain as the most recent mention of it was in a 2019 SEC filing from the drug manufacturer lists the drug's expected launch year as 2024, but not in subsequent filings or press releases. — Wikipedia
Clinical trial activity
13 trials · 6 clinical orgs · 0 marketing orgs
Earliest trial started Jul 1, 2011 (NCT01394055)
Timeline
Indications
Mechanism of action
- Ghrelin receptorAGONIST
GHSR agonist
Chemistry & pharmacology
SMILES
NC(=O)C1(NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2csc3ccccc23)NC(=O)C2CCNCC2)CCNCC1- Mol. weight
- 790.99 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaRelamorelin ↗
- ChEMBLCHEMBL4297525 ↗
Also known as
- bim-28131
- relamorelin
- relamorelin
- relamorelin
- relamorelin
- rm-131
- rm-131
- rm-131
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03786380 | Phase 3 | Dec 20, 2018 | Allergan |
| NCT03426345 | Phase 3 | Feb 20, 2018 | Allergan |
| NCT03420781 | Phase 3 | Jan 24, 2018 | Allergan |
| NCT03383146 | Phase 3 | Dec 19, 2017 | Allergan |
| NCT03285308 | Phase 3 | Sep 29, 2017 | Allergan |
| NCT02466711 | Phase 1 | Jun 1, 2015 | Mayo Clinic, Motus Therapeutics, Inc. |
| NCT02357420 | Phase 2 | Jan 1, 2015 | Motus Therapeutics, Inc. |
| NCT02137642 | Phase 1 | Aug 1, 2014 | Mayo Clinic, Motus Therapeutics, Inc. |
| NCT01955616 | Phase 2 | Sep 1, 2013 | Michael J. Fox Foundation for Parkinson's Research, Motus Therapeutics, Inc. |
| NCT01781104 | Phase 2 | Mar 1, 2013 | Motus Therapeutics, Inc., Rhythm Pharmaceuticals, Inc. |
| NCT01642550 | Phase 2 | Nov 1, 2012 | Harvard University, Motus Therapeutics, Inc. |
| NCT01571297 | Phase 2 | Apr 1, 2012 | Motus Therapeutics, Inc., Rhythm Pharmaceuticals, Inc. |
| NCT01394055 | Phase 1 | Jul 1, 2011 | Mayo Clinic, Motus Therapeutics, Inc. |
Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Motus Therapeutics, Inc. | For profit | 8 | 8 | 2 | 2011 |
| Allergan | For profit | 5 | 5 | 1 | 2017 |
| Mayo Clinic | Academic/Hospital | 3 | 0 | 1 | 2011 |
| Rhythm Pharmaceuticals, Inc. | For profit | 2 | 0 | 1 | 2012 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Michael J. Fox Foundation for Parkinson's Research | Academic/Hospital | 1 | 0 | 1 | 2013 |