macimorelin
Trade name: Macrilen
Approved
Dec 20, 2017
Macimorelin (AEZS 130) is an orally active, small-molecule, peptidomimetic growth hormone secretagogue receptor (GHSR1A) agonist (ghrelin analogue), being developed by AEterna Zentaris for the diagnosis of adult growth hormone deficiency (AGHD; somatotropin deficiency), and for the treatment of cachexia associated with chronic disease such as AIDS and cancer. Macimorelin was approved by the FDA in December 2017 under the market name Macrilen for oral solution. Macimorelin stimulates GH release by activating growth hormone secretagogue receptors present in the pituitary and hypothalamus. Macimorelin has been granted orphan drug designation by the FDA for diagnosis of AGHD. — NCATS
Clinical trial activity
6 trials · 8 clinical orgs · 3 marketing orgs
Earliest trial started Nov 1, 2005 (NCT00377377)
Timeline
2000s
- Jan 1, 2005
Earliest Phase 1 Sponsor(trial)
- Jan 1, 2007
AEterna Zentaris — Earliest Phase 3 Sponsor(trial)
- May 14, 2007
Orphan Drug Designation
2010s
- Jan 1, 2012
Earliest Phase 2 Sponsor(trial)
- Dec 20, 2017
AEterna Zentaris — Earliest FDA Approval
- Dec 20, 2017
Novo — NDA Secondary Org
- Dec 20, 2017
AEterna Zentaris — NDA Organization
- Dec 20, 2017
Novo Nordisk — NDA Secondary Org
- Dec 20, 2017
AEterna Zentaris — Marketing Organization
Indications
Approved for
Mechanism of action
- Ghrelin receptorAGONIST
GHSR agonist
Approval history
- approvedDec 20, 2017
Chemistry & pharmacology
SMILES
CC(=O)O.CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O- Mol. weight
- 534.62 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2364617 ↗
- WikipediaMacimorelin ↗
- NCATS8680B21W73 ↗
- ChEMBLCHEMBL278623 ↗
Also known as
- aezs-130
- aezs-130
- aezs-130
- aib-dtrp-dgtrp-cho
- aib-trp-gtrp-cho
- aminoisobutyryl-tryptophyl-tryptophanamine-formyl
- ard-07
- ard-07
- ard-07
- ep-01572
- ep-01572
- ep1572
- ep1572
- ep1572
- ep 1572
- ep-1572
- jmv1843
- jmv 1843
- jmv-1843
- jmv-1843
- jmv-1843
- macimorelin
- macimorelin
- macimorelin
- macimorelin
- macimorelin
- macimorelin acetate
- macimorelin acetate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04786873 | Phase 3 | Sep 30, 2021 | AEterna Zentaris, Novo Nordisk |
| NCT03844217 | N/A | Jan 2, 2019 | University of Basel |
| NCT02558829 | Phase 3 | Sep 1, 2015 | AEterna Zentaris, Baylor University |
| NCT01614990 | Phase 2 | May 1, 2012 | AEterna Zentaris, Baylor University, Department of Veteran Affairs, University of Washington |
| NCT00448747 | Phase 3 | Jun 30, 2007 | AEterna Zentaris, Harvard University |
| NCT00377377 | Phase 1 | Nov 1, 2005 | University of Bern |
Organizations
Research & Development (8)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| AEterna Zentaris | For profit | 4 | 3 | 2 | 2007 |
| Baylor University | Academic/Hospital | 2 | 0 | 2 | 2012 |
| Department of Veteran Affairs | Government | 1 | 0 | 1 | 2012 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Novo Nordisk | For profit | 1 | 0 | 1 | 2021 |
| University of Basel | Academic/Hospital | 1 | 1 | 1 | 2019 |
| University of Bern | Academic/Hospital | 1 | 1 | 1 | 2005 |
| University of Washington | Academic/Hospital | 1 | 1 | 1 | 2012 |
Marketing (4)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| AEterna Zentaris | For profit | NDA | Dec 20, 2017 |
| AEterna Zentaris | For profit | MKTG | Dec 20, 2017 |
| Novo | For profit | NDA2 | Dec 20, 2017 |
| Novo Nordisk | For profit | NDA2 | Dec 20, 2017 |