U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 11 - 20 of 62 results

Status:
Investigational
Source:
NCT00963053: Phase 2 Interventional Completed Primary Dysmenorrhea
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:invopressin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:cligosiban [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


PF-3274167 (Cligosiban) is a potent, selective, brain penetrant oxytocin receptor antagonist. Cligosiban interrupts the expulsion phase of ejaculation by reducing the normal bulbospongiosum burst pattern and reducing the expulsions that accompany bursts. Cligosiban represents a promising compound to test the clinical hypothesis that antagonism of central oxytocin receptors may be of therapeutic benefit in the treatment of premature ejaculation. [11C]PF-3274167 is not a suitable tracer for imaging of OTR in rat brain, probably because of a too low affinity for this receptor in addition to a poor brain penetration. PF-3274167 had been in phase I clinical trial for the treatment of sexual function disorders and urinary incontinence. However, this research has been discontinued.
Status:
Investigational
Source:
INN:ribuvaptan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ribuvaptan (BAY 868050) is a vasopressin receptor antagonist that has been developed for treatment of heart failure. No information on current use is available.
Status:
Investigational
Source:
INN:balovaptan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lixivaptan is an orally-active, vasopressin 2 receptor antagonist. It is indicated for the treatment of symptomatic hypervolemic and euvolemic hyponatremia, associated with heart failure (HF) and syndrome of inappropriate antidiuretic hormone (SIADH). Adverse events likely to be result of the pharmacologic action of lixivaptan are: constipation, dry mouth, dizziness, insomnia. Grapefruit juice significantly increased the extent of lixivaptan absorption as compared to lixivaptan administered under fasted conditions but not under fed conditions. Lixivaptan Cmax and AUC∞ increased by 2.4-fold and 3.2-fold, respectively, when lixivaptan was administered with ketoconazole (the same in case of Simvastatin).
Status:
Investigational
Source:
INN:selepressin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Selepressin (FE 202158) was designed as a selective and short-acting vasopressin type 1a receptor (V(1a)R) agonist. This drug was developed for the treatment of vasodilatory hypotension in shock. Selepressin successfully completed phase IIa clinical trial, where was found that in septic shock patients, selepressin 2.5 ng/kg/minute was able to rapidly replace norepinephrine, improve fluid balance and shorten the time of mechanical ventilation.
Status:
Investigational
Source:
INN:fedovapagon [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Fedovapagon, also known as VA106483 and VT483, is a potent, nonpeptidic vasopressin V2 receptor agonist. Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. Fedovapagon (VA106483) was discovered by Vantia and currently in Phase II trials for the treatment of nocturia, a common condition that causes sufferers to wake frequently during the night in order to urinate. Fedovapagon has been extensively studied in clinical trials and data, presented at the American Urological Association meeting in 2010, demonstrated a dose-dependent reduction in nocturnal urine volumes and a reliable pharmacodynamic effect on repeated dosing. More recently, data presented in San Diego at the 2012 American Urological Association meeting, showed that fedovapagon was effective from the first night of dosing and that there was no effect following cessation of dosing. Further presentations are planned for the International Continence Society meeting being held in Barcelona in August 2013. These data suggest that fedovapagon has the potential to be an effective and well tolerated antidiuretic for the treatment of nocturia. Fedovapagon is currently being investigated as a new treatment for nocturia in a Phase-II/III clinical trials in USA (PO)(NCT02637960).
Status:
Investigational
Source:
INN:satavaptan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sanofi-Synthélabo has developed satavaptan (previously known as SR121463) as a non-peptidic vasopressin V2 receptor antagonist for the potential treatment for cardiovascular indications such as congestive heart failure (CHF) and hypertension. The drug reached phase II for these indications before the studies were discontinued. Satavaptan was also studied for the potential treatment of glaucoma. In addition, this drug was involved in phase III clinical trials in patients with ascites due to cirrhosis of the liver and in in patients with dilutional hyponatremia. However, the further development of the satavaptan was discontinued in 2009.
Status:
Investigational
Source:
INN:nelivaptan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nelivaptan is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V1B subtype. It showed promise in preclinical animal models and advanced to phase II clinical trials for the treatment of anxiety and depression; however, in 2008, Sanofi-Aventis announced that further development of this drug had been halted.