samidorphan
Trade name: Lybalvi
Approved
May 28, 2021
Samidorphan is an opioid antagonist that in the form of olanzapine/samidorphan is used in the treatment of schizophrenia and bipolar disorder. Samidorphan reduces the weight gain associated with olanzapine. Samidorphan is taken by mouth. — Wikipedia
Clinical trial activity
37 trials · 3 clinical orgs · 1 marketing orgs
Earliest trial started Dec 1, 2008 (NCT00800319)
Timeline
Indications
Studied for
- Alcoholism · Phase 2
- Binge-Eating Disorder · Phase 2
- Bipolar Disorder · Phase 3
- Cocaine-Related Disorders · Phase 1
- Depression · Phase 3
- Healthy Volunteers · Phase 1
- Kidney Failure, Chronic · Phase 1
- Liver Diseases · Phase 1
- Major Depressive Disorder · Phase 3
- Pharmacokinetics · Phase 1
- Psychotic Disorders · Phase 3
- Schizophrenia · Phase 3
- Substance-Related Disorders · Phase 1
Mechanism of action
- Mu opioid receptorANTAGONIST
OPRM antagonist
Compound is art of the combination product ALKS-5461, where samidorphan is combined with buprenorphine ALKS-5461 is being developed as an as antidepressant drug.
- Kappa opioid receptorPARTIAL AGONIST
Kappa opioid receptor partial agonist
Increased potency at the mu receptor
- Delta opioid receptorPARTIAL AGONIST
Delta opioid receptor partial agonist
Increased potency at the mu receptor
Combination products
lybalvi
with olanzapine
Also known as olanzapine and samidorphan
Approval history
- approvedMay 28, 2021
Chemistry & pharmacology
SMILES
NC(=O)c1ccc2c(c1O)[C@]13CCN(CC4CC4)[C@H](C2)[C@]1(O)CCC(=O)C3.O=C(O)C[C@H](O)C(=O)O- Mol. weight
- 504.54 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
- WikipediaSamidorphan ↗
- ChEMBLCHEMBL426084 ↗
- ChEMBLCHEMBL2105749 ↗
Also known as
- 3-carboxamido-4-hydroxynaltrexone
- alk3831
- alks33
- alks33
- alks 33
- alks 33
- alks 33
- alks-33
- alks-33
- alks-33
- alks 3831
- rdc-0313
- rdc-0313
- rdc-0313
- rdc-0313-00
- rdc-0313-00
- samidorphan
- samidorphan
- samidorphan
- samidorphan
- samidorphan
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05303064 | Phase 3 | Jun 30, 2022 | Alkermes |
| NCT04987229 | Phase 3 | Oct 31, 2021 | Alkermes |
| NCT04987658 | Phase 1 | Jul 22, 2021 | Alkermes |
| NCT03610048 | Phase 3 | Aug 9, 2018 | Alkermes |
| NCT03188185 | Phase 3 | Jun 12, 2017 | Alkermes |
| NCT03187769 | Phase 3 | Jun 8, 2017 | Alkermes |
| NCT03201757 | Phase 3 | Jun 1, 2017 | Alkermes |
| NCT02922426 | Phase 1 | Sep 1, 2016 | Alkermes |
| NCT02873208 | Phase 3 | Aug 1, 2016 | Alkermes |
| NCT02804568 | Phase 1 | Jun 1, 2016 | Alkermes |
| NCT02694328 | Phase 3 | Feb 1, 2016 | Alkermes |
| NCT02669758 | Phase 3 | Jan 1, 2016 | Alkermes |
| NCT02634346 | Phase 3 | Dec 1, 2015 | Alkermes |
| NCT02521857 | Phase 1 | Jul 1, 2015 | Alkermes |
| NCT02545439 | Phase 1 | Jul 1, 2015 | Alkermes |
| NCT02508506 | Phase 1 | Jul 1, 2015 | Alkermes |
| NCT02504463 | Phase 1 | Jun 1, 2015 | Alkermes |
| NCT02479308 | Phase 1 | Jun 1, 2015 | Alkermes |
| NCT02452801 | Phase 1 | May 1, 2015 | Alkermes |
| NCT02413281 | Phase 1 | Mar 1, 2015 | Alkermes |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Alkermes | For profit | 37 | 36 | 3 | 2008 |
| National Institute on Drug Abuse (NIDA) | Government | 2 | 1 | 1 | 2010 |
| IQVIA | For profit | 1 | 0 | 1 | 2008 |