Casopitant
Trade name: zunrisa
Casopitant (INNTooltip International Nonproprietary Name), former tentative trade names Rezonic (U.S.) and Zunrisa (Europe), is an NK1 receptor antagonist which was undergoing research for the treatment of chemotherapy-induced nausea and vomiting. It was under development by GlaxoSmithKline. In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn and development was discontinued in September 2009 because GlaxoSmithKline decided that further safety assessment was necessary. However, a 2022 review listed casopitant as under development as a potential novel antidepressant for the treatment of major depressive disorder, with a phase 2 clinical trial having been completed. — Wikipedia
Clinical trial activity
29 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Jul 1, 2004 (NCT00650871)
Timeline
Indications
Studied for
- Depression · Phase 2
- Drug-Related Side Effects and Adverse Reactions · Phase 3
- Dyspepsia · Phase 2
- Major Depressive Disorder · Phase 2
- Nausea · Phase 3
- Neoplasms · Phase 3
- Phobia, Social · Phase 1
- Postoperative Nausea and Vomiting · Phase 3
- Sleep Initiation and Maintenance Disorders · Phase 2
- Urinary Bladder, Overactive · Phase 2
- Vomiting · Phase 3
Mechanism of action
- Neurokinin 1 receptorANTAGONIST
TACR1 antagonist
Filing withdrawn, development halted.
Chemistry & pharmacology
SMILES
CC(=O)N1CCN([C@H]2CCN(C(=O)N(C)[C@H](C)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[C@@H](c3ccc(F)cc3C)C2)CC1- Mol. weight
- 616.62 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
- ChEMBLCHEMBL1672054 ↗
- WikipediaCasopitant ↗
- ChEMBLCHEMBL2107320 ↗
Also known as
- casopitant
- casopitant
- casopitant
- casopitant
- casopitant
- casopitant
- casopitant mesilate
- casopitant mesylate
- casopitant mesylate
- gw679769
- gw679769
- gw679769
- gw679769
- gw-679769
- zunrisa
- zunrisa
- zunrisa
- zunrisa
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00891761 | Phase 3 | Sep 1, 2009 | GlaxoSmithKline |
| NCT00601172 | Phase 3 | Mar 1, 2008 | GlaxoSmithKline |
| NCT00511823 | Phase 1 | Jul 1, 2007 | GlaxoSmithKline |
| NCT00440128 | Phase 1 | May 1, 2007 | GlaxoSmithKline |
| NCT00460707 | Phase 1 | Apr 1, 2007 | GlaxoSmithKline |
| NCT00437229 | Phase 1 | Feb 1, 2007 | GlaxoSmithKline |
| NCT00404274 | Phase 1 | Nov 1, 2006 | GlaxoSmithKline |
| NCT00431236 | Phase 3 | Nov 1, 2006 | GlaxoSmithKline |
| NCT00405080 | Phase 1 | Nov 1, 2006 | GlaxoSmithKline |
| NCT00404378 | Phase 1 | Oct 1, 2006 | GlaxoSmithKline |
| NCT00358813 | Phase 1 | Sep 1, 2006 | GlaxoSmithKline |
| NCT00366834 | Phase 3 | Jul 1, 2006 | GlaxoSmithKline |
| NCT00354809 | Phase 2 | May 1, 2006 | GlaxoSmithKline |
| NCT00334152 | Phase 3 | Mar 1, 2006 | GlaxoSmithKline |
| NCT00326248 | Phase 3 | Mar 1, 2006 | GlaxoSmithKline |
| NCT00332046 | Phase 1 | Jan 1, 2006 | GlaxoSmithKline |
| NCT00280436 | Phase 2 | Jan 1, 2006 | GlaxoSmithKline |
| NCT00358410 | Phase 2 | Jan 1, 2006 | GlaxoSmithKline |
| NCT00280423 | Phase 2 | Jan 1, 2006 | GlaxoSmithKline |
| NCT00332319 | Phase 2 | Jan 1, 2006 | GlaxoSmithKline |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 29 | 29 | 3 | 2004 |