conivaptan
Trade name: vaprisol
Approved
Dec 29, 2005
Conivaptan is an arginine vasopressin (AVP) receptor antagonist with affinity for AVP receptor subtypes V1A and V2. The antidiuretic action of AVP is mediated through activation of the V2 receptor, which functions to regulate water and electrolyte balance at the level of the collecting ducts in the kidney. Conivaptan was approved in 2004 for hyponatremia caused by syndrome of inappropriate antidiuretic hormone. Conicaptan is being evaluated for reduce intracranial pressure in patients with traumatic brain injury, and as a treatment for heart failure. — NCATS
Clinical trial activity
21 trials · 14 clinical orgs · 2 marketing orgs
Earliest trial started Jan 1, 2000 (NCT00492037)
Timeline
2000s
- Jan 1, 2000
Cumberland Pharmaceuticals — Earliest Phase 3 Sponsor(trial)
- Jan 1, 2002
Cumberland Pharmaceuticals — Earliest Phase 2 Sponsor(trial)
- Dec 29, 2005
Astellas — Earliest FDA Approval
- Dec 29, 2005
Astellas — NDA Organization
- Dec 29, 2005
Cumberland Pharmaceuticals — NDA Secondary Org
- Jan 1, 2009
Cumberland Pharmaceuticals — Earliest Phase 1 Sponsor(trial)
Indications
Approved for
Mechanism of action
- Vasopressin V2 receptorANTAGONIST
AVPR2 antagonist
- Vasopressin V1a receptorANTAGONIST
AVPR1A antagonist
Approval history
- approvedDec 29, 2005
Chemistry & pharmacology
SMILES
Cc1nc2c([nH]1)-c1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC2- Mol. weight
- 498.59 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
Oral
No
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL1755 ↗
- WikipediaConivaptan ↗
- NCATS0NJ98Y462X ↗
- ChEMBLCHEMBL1201108 ↗
Also known as
- (1,1'-biphenyl)-2-carboxamide, n-(4-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1h)-yl)carbonyl)phenyl)-
- (1,1'-biphenyl)-2-carboxamide, n-(4-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1h)-yl)carbonyl)phenyl)-, monohydrochloride
- 4'-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1h)-yl)carbonyl)-2-biphenylcarboxanilide
- 4'-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1h)-yl)carbonyl)-2-biphenylcarboxanilide
- 4''-((4,5-dihydro-2-methylimidazo(4,5-d)(1)benzazepin-6(1h)-yl)carbonyl)-2-biphenylcarboxanilide
- ci-1025
- ci-1025
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan
- conivaptan hcl
- conivaptan hcl
- conivaptan hcl
- conivaptan hydrochloride
- conivaptan hydrochloride
- conivaptan hydrochloride
- conivaptan hydrochloride
- conivaptan hydrochloride
- conivaptan hydrochloride
- vaprisol
- vaprisol
- vaprisol
- vaprisol
- vaprisol
- vaprisol
- ym087
- ym087
- ym087
- ym 087
- ym-087
- ym-087
- ym-087
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03000283 | N/A | Jan 1, 2017 | Allina Health, Allina Health System |
| NCT01954290 | Phase 2 | Sep 1, 2015 | University of Florida |
| NCT01752543 | Phase 4 | Dec 1, 2013 | University of Copenhagen |
| NCT01451411 | Phase 3 | Feb 1, 2012 | Cumberland Pharmaceuticals |
| NCT01370148 | Phase 1 | Apr 1, 2011 | Cumberland Pharmaceuticals |
| NCT00930202 | Phase 1 | Aug 1, 2009 | University of Washington |
| NCT00924014 | N/A | Jul 1, 2009 | Astellas, Hennepin Healthcare |
| NCT00843986 | Phase 3 | Apr 1, 2009 | Cumberland Pharmaceuticals |
| NCT00887627 | Phase 1 | Apr 1, 2009 | Cumberland Pharmaceuticals |
| NCT00851227 | Phase 1 | Feb 1, 2009 | Cumberland Pharmaceuticals |
| NCT00811486 | N/A | Jan 1, 2009 | University of Colorado, University of Colorado, Denver |
| NCT00806910 | Phase 4 | Oct 1, 2008 | Astellas, Yeshiva University |
| NCT00727090 | Phase 4 | Aug 1, 2008 | Astellas, Northwestern University |
| NCT00684164 | Phase 3 | May 1, 2008 | Astellas, Columbia University |
| NCT00592475 | Phase 2 | Dec 1, 2007 | Cumberland Pharmaceuticals |
| NCT00478192 | Phase 3 | Apr 1, 2007 | Cumberland Pharmaceuticals |
| NCT00435591 | Phase 4 | Jan 1, 2007 | Cumberland Pharmaceuticals |
| NCT00379847 | Phase 3 | Feb 1, 2004 | Cumberland Pharmaceuticals |
| NCT00057356 | Phase 2 | Nov 1, 2002 | Cumberland Pharmaceuticals |
| NCT00380575 | Phase 3 | Aug 1, 2000 | Astellas, Cumberland Pharmaceuticals |
Organizations
Research & Development (14)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cumberland Pharmaceuticals | For profit | 12 | 12 | 4 | 2000 |
| Astellas | For profit | 5 | 0 | 3 | 2000 |
| Allina Health | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Allina Health System | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Columbia University | Academic/Hospital | 1 | 1 | 1 | 2008 |
| Hennepin Healthcare | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Northwestern University | Academic/Hospital | 1 | 1 | 1 | 2008 |
| Parke-Davis | For profit | 1 | 0 | 1 | 2000 |
| University of Colorado | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Colorado, Denver | Academic/Hospital | 1 | 1 | 1 | 2009 |
| University of Copenhagen | Academic/Hospital | 1 | 1 | 1 | 2013 |
| University of Florida | Academic/Hospital | 1 | 1 | 1 | 2015 |
| University of Washington | Academic/Hospital | 1 | 1 | 1 | 2009 |
| Yeshiva University | Academic/Hospital | 1 | 1 | 1 | 2008 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Astellas | For profit | NDA | Dec 29, 2005 |
| Cumberland Pharmaceuticals | For profit | NDA2 | Dec 29, 2005 |