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

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Showing 11691 - 11700 of 13240 results

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Sulisatin (also known as DAN-603) is an indolinone derivative patented by Andreu, Dr., S. A. as a laxative. In preclinical models, Sulisatin increases selectively the colon motility without modifying the speed of gastric, intestinal (small intestine) and caecal emptying in rats. Sulisatin is unable to inhibit water absorption in rat colon while small amounts of Sulisatin may inhibit it significantly.
Status:
Investigational
Source:
USAN:Asulacrine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Asulacrine, also known as CI-921, an inhibitor of topoisomerase II, participated in clinical trials phase II for the treatment of cancer. In spite of the positive and promising results, this drug showed the toxicity, phlebitis that blocks its implementation in the future.
Status:
Investigational
Source:
NCT00156156: Phase 3 Interventional Completed Fibroid Uterus
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Asoprisnil (J867) is a novel selective steroid receptor modulator that shows unique pharmacodynamic effects in animal models and humans. Asoprisnil, its major metabolite J912, and other structurally related compounds represent a new class of progesterone receptor (PR) ligands that exhibit partial agonist and antagonist activities in vivo. Asoprisnil demonstrates a high degree of receptor and tissue selectivity, with a high-binding affinity for PR, moderate affinity for glucocorticoid receptor (GR), low affinity for androgen receptor (AR), and no binding affinity for estrogen or mineralocorticoid receptors. This compound was recently in clinical trials for the treatment of uterine fibroids and endometriosis, but those studies were discontinued.
Status:
Investigational
Source:
INN:flavodic acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Flavodic acid is a synthetic hydrosoluble derivative of natural flavonoids. It has been shown to reduce capiliary fragility and permeability. Sodium flavodate was marketed by the Italian pharmaceutical company Farmaceutici under tradename Pericel.
Status:
Investigational
Source:
INN:roxifiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Roxifiban (also known as DMP754), a potent antiplatelet agent in inhibiting platelet aggregation, and has a high specificity and affinity for human platelet glycoprotein IIb/IIIa complex (GPIIb/IIIa) receptors. Roxifiban participated in clinical trials phase III for the treatment of peripheral arterial disorders. This drug was also well tolerated in patients with chronic stable angina pectoris and was studied in the treatment of heparin-induced thrombocytopenia, and thrombosis. However, the development of this drug appears to have been discontinued.
Status:
Investigational
Source:
INN:butinoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Butinoline (also known as azulone) was used as an antispasmodic drug to treat gastritis.
Status:
Investigational
Source:
NCT00619931: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Temanogrel (also known as APD791) is an oral small molecule inverse agonist of the serotonin 2A (5-HT2A) receptor with potent activity on platelets and vascular smooth muscle. Temanogrel has been studied in phase I clinical trials in healthy subjects to assess its pharmacokinetics, pharmacodynamics, and safety. However, these studies were terminated because of the sponsor’s decision.
Status:
Investigational
Source:
USAN:METALOL HYDROCHLORIDE [USAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Metalol is an antagonist at beta-adrenergic receptors.
Status:
Investigational
Source:
NCT00852839: Phase 2 Interventional Completed Dry Mouth Associated With Sjogren's Syndrome
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Compound 552-02 is a potent, selective inhibitor of epithelial sodium channels that is effective in enhancing mucociliary clearance and is well tolerated when administered as a single dose by inhalation aerosol in normal healthy adult volunteers. Parion Sciences was developing 552 02 for the treatment of xerostomia, cystic fibrosis, chronic bronchitis, chronic obstructive pulmonary disease, radiation injuries. Compound 552-02 was specifically designed for aerosol delivery to the pulmonary system as a more selective, potent, long-acting ENaC blocker to promote an expansion in ASL volume, with or without hypertonic saline. Compound 552-02 was selected from a series of novel ENaC blockers to produce a selective block on airway epithelial sodium channels, with a potency up to 2 orders of magnitude greater than amiloride. 552-02 blocked the majority (95%) of Isc, with a calculated IC50 value of 7 nM. Drug development was discontinued.
Status:
Investigational
Source:
NCT04593940: Phase 3 Interventional Completed Covid19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cenicriviroc (also referred to as TBR-652 and TAK-652) is an orally active, potent inhibitor of ligand binding to C-C chemokine receptor type 2 (CCR2) and C-C chemokine receptor type 5 (CCR5). Cenicriviroc does not inhibit ligand binding to CCR1 (an alternative target of CCR5 ligands). The mean half-life in healthy volunteers is 35 to 40 hours, which allows daily dosing of the drug. Due to its CCR5 blocking activity, Cenicriviroc has initially been tested as a drug against CCR5-tropic HIV infection. In a double-blind placebo-controlled trial involving 54 HIV infected participants, Cenicriviroc monotherapy at different doses (25, 50, 75, 100, or 150 mg) led to a dose-dependent reduction in HIV-1 RNA levels and concomitant increases in circulating levels of the CCR2 ligand monocyte chemoattractant protein 1 (MCP-1, or CCL2), suggesting potent CCR2 and CCR5 inhibition in vivo. According to clinical trials, Cenicriviroc is a very safe drug with a wide therapeutic range and fairly low pharmacokinetic variability. In animal models of liver diseases, Cenicriviroc potently inhibits macrophage accumulation in the liver and ameliorates fibrosis. In a phase 2b clinical trial on 289 patients with NASH and fibrosis, Cenicriviroc consistently demonstrated liver fibrosis improvement after 1 year of therapy and had an excellent safety profile.

Showing 11691 - 11700 of 13240 results