tasimelteon
Trade name: hetlioz
Approved
Jan 31, 2014
Tasimelteon, developed by Vanda Pharmaceuticals Inc under license from Bristol-Myers Squibb Co, is a melatonin receptor agonist. Tasimelteon differs structurally from melatonin and drugs with known melatonin agonist activity, in particular by its distinct aromatic group and linker. Tasimelteon bears also no structural relationship to any other approved active substance. Tasimelteon is presumably acts through activation of MT1 and MT2 G-protein coupled receptors, which are involved primarily in inhibition of neuronal firing and phase shift of circadian rhythms. Tasimelteon is approved for the treatment of Non24-Hour Sleep-Wake Disorder. — NCATS
Clinical trial activity
26 trials · 3 clinical orgs · 4 marketing orgs
Earliest trial started Jul 1, 2004 (NCT00490945)
Timeline
2000s
- Jan 1, 2004
Vanda Pharmaceuticals — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2006
Vanda Pharmaceuticals — Earliest Phase 3 Sponsor(trial)
2010s
- Jan 19, 2010
Orphan Drug Designation
- Jan 1, 2011
Vanda Pharmaceuticals — Earliest Phase 1 Sponsor(trial)
- Jan 31, 2014
Vanda Pharmaceuticals — Earliest FDA Approval
- Jan 31, 2014
Vanda Pharmaceuticals — NDA Secondary Org
- Jan 31, 2014
Vanda Pharmaceuticals — NDA Organization
2020s
- May 28, 2020
MSN Laboratories — Marketing Organization
- Dec 1, 2020
Vanda Pharmaceuticals — Marketing Organization
- Sep 27, 2021
Teva — Marketing Organization
- Dec 20, 2022
Apotex — Marketing Organization
Indications
Approved for
Studied for
- Autism Spectrum Disorder · Phase 1
- Chronobiology Disorders · Phase 3
- Healthy Volunteers · Phase 1
- Kidney Failure, Chronic · Phase 1
- Liver Diseases · Phase 1
- Major Depressive Disorder · Phase 2/Phase 3
- Mutation · Phase 3
- Pharmacokinetics · Phase 1
- REM Sleep Behavior Disorder · Early Phase 1
- Sleep Disorders, Circadian Rhythm · Phase 4
- Sleep Disorders, Intrinsic · Phase 3
- Sleep Initiation and Maintenance Disorders · Phase 3
- Sleep Wake Disorders · Phase 3
- Smith-Magenis Syndrome · Phase 2/Phase 3
Mechanism of action
Approval history
- approvedPriority reviewJan 31, 2014
Chemistry & pharmacology
SMILES
CCC(=O)NC[C@@H]1C[C@H]1C2=CC=CC3=C2CCO3- Mol. weight
- 245.3169 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaTasimelteon ↗
- NCATSSHS4PU80D9 ↗
- ChEMBLCHEMBL2103822 ↗
Also known as
- bms214778
- bms 214778
- bms-214778
- bms-214778
- bms-214778
- bms-214778
- hetlioz
- hetlioz
- hetlioz
- n-{[(1r,2r)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanamide
- n-{[(1r,2r)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanamide
- n-((2-(2,3-dihydro-4-benzofuranyl)cyclopropyl)methyl)propanamide
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimelteon
- tasimeltéon
- tasimeltéon
- vec-162
- vec-162
- vec-162
- vec-162
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06953869 | Phase 3 | Apr 21, 2025 | Vanda Pharmaceuticals |
| NCT06701396 | Phase 3 | Oct 8, 2024 | Vanda Pharmaceuticals |
| NCT05922995 | Early Phase 1 (Phase 1) | Sep 30, 2023 | Harvard University, Vanda Pharmaceuticals |
| NCT05572281 | Phase 1 | May 18, 2022 | Vanda Pharmaceuticals |
| NCT04652882 | Phase 3 | Dec 31, 2020 | Vanda Pharmaceuticals |
| NCT06323655 | Phase 1 | Jul 19, 2018 | Vanda Pharmaceuticals |
| NCT03373201 | Phase 3 | Oct 16, 2017 | Vanda Pharmaceuticals |
| NCT03291041 | Phase 2 | Sep 30, 2016 | Vanda Pharmaceuticals |
| NCT02776215 | Phase 1 | Sep 1, 2016 | Sponsor GmbH, Vanda Pharmaceuticals |
| NCT02231008 | Phase 2/Phase 3 (Phase 3) | Sep 1, 2015 | Vanda Pharmaceuticals |
| NCT02130999 | Phase 4 | May 1, 2014 | Vanda Pharmaceuticals |
| NCT01637636 | Phase 1 | Jun 1, 2012 | Vanda Pharmaceuticals |
| NCT01578057 | Phase 1 | Apr 1, 2012 | Vanda Pharmaceuticals |
| NCT01526746 | Phase 1 | Feb 1, 2012 | Vanda Pharmaceuticals |
| NCT01540500 | Phase 1 | Feb 1, 2012 | Vanda Pharmaceuticals |
| NCT01477619 | Phase 1 | Nov 1, 2011 | Vanda Pharmaceuticals |
| NCT01429116 | Phase 3 | Oct 1, 2011 | Vanda Pharmaceuticals |
| NCT01430754 | Phase 3 | Sep 1, 2011 | Vanda Pharmaceuticals |
| NCT01428661 | Phase 2/Phase 3 (Phase 3) | Sep 1, 2011 | Vanda Pharmaceuticals |
| NCT01402076 | Phase 1 | Aug 1, 2011 | Vanda Pharmaceuticals |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Vanda Pharmaceuticals | For profit | 26 | 25 | 4 | 2004 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2023 |
| Sponsor GmbH | Academic/Hospital | 1 | 0 | 1 | 2016 |
Marketing (7)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Apotex | For profit | MKTG | Dec 20, 2022 |
| MSN Laboratories | For profit | MKTG | May 28, 2020 |
| MSN Laboratories | For profit | SYN | Jan 12, 2023 |
| Teva | For profit | MKTG | Sep 27, 2021 |
| Vanda Pharmaceuticals | For profit | NDA2 | Jan 31, 2014 |
| Vanda Pharmaceuticals | For profit | NDA | Jan 31, 2014 |
| Vanda Pharmaceuticals | For profit | MKTG | Dec 1, 2020 |