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

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Showing 641 - 650 of 13408 results

Status:
Investigational
Source:
NCT02536781: Phase 2/Phase 3 Interventional Completed Inflammation of Mouth
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

ARN-810 (GDC-0810) is a novel, orally bioavailable, estrogen receptor antagonist that induces proteasomal estrogen receptor degradation in breast cancer cell lines at picomolar concentrations and tumor regression in tamoxifen-sensitive and resistant BC xenograft models. Results from a first-in-human phase I/IIa study of ARN-810 indicate that it is tolerable and may benefit some postmenopausal women with advanced estrogen receptor-positive breast cancer. Development of ARN-810 was discontinued.
Status:
Investigational
Source:
INN:adomeglivant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adomeglivant, also known as LY2409021, is a potent and selective glucagon receptor antagonist. Adomeglivant lowers blood glucose in healthy people and in those with type 2 diabetes. Blockade of glucagon signalling in patients with type 2 diabetes is well tolerated and results in substantial reduction of fasting and postprandial glucose with minimal hypoglycaemia, but with reversible increases in aminotransferases. Adomeglivant had been in phase II clinical trials by Eli Lilly for the treatment of type 2 diabetes mellitus. However, this research has been discontinued.
Status:
Investigational
Source:
NCT03870776: Phase 2 Interventional Recruiting Depression
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mapreg is developing pregnenolone methyl ether (MAP4343), an injectable neurosteroid stimulator of the tubulin polymerisation and neurite growth stimulator. The synthetic pregnenolone-derivative MAP4343 (3β-methoxy-preg-nenolone) binds in vitro to microtubule-associated-protein 2 (MAP2), stimulates the polymerization of tubulin, enhances the extension of neurites and protects neurons against neurotoxic agents. MAP4343 has been selected after screening of a large library ofnatural and synthetic steroids. MAP4343 has similar in vitro activity as pregnenolone; it cannot be converted into metabolites with hormonal activities, and has been shown to have in vivo beneficial effects in rat models of spinal cord injury. MAP4343 has an interesting pharmacological profile because no in vitro affinity for any CNS neurotransmitter receptor was found. MAP4343 has been shown to have antidepressant efficacy in rats. In the rat isolation-rearing model of depression, administration of MAP4343 showed persistent efficacy in recovering recognition memory deficit, stronger and more rapid anxiolytic activity, and more rapid rescue of passive coping behavior compared with FLX. The behavioral effects of MAP4343 correlated with changes in α-tubulin isoforms in the hippocampus, amygdala, and pre-frontal cortex (PFC). Its efficacy was also assessed in vivo with the most commonly used thoracic spinal cord compression/contusion models in rats. In the three models used, the post-traumatic subcutaneous injection of MAP4343 significantly improved the recovery of locomotor function after spinal cord injury, as shown by an earlier and more complete recovery compared to vehicle-treated rats. The results obtained in three different rat models of spinal cord injury demonstrate the beneficial effects of this therapeutic strategy and identify MAP4343 as a potential treatment for acute spinal cord injury. MAP4343 received EU Orphan Drug designation for spinal cord injury. MAP4343 is in phase II clinical trials by Mapreg for the treatment of depression and in phase I clinical trials for the treatment of spinal cord injury and traumatic brain injury.
Status:
Investigational
Source:
INN:sergliflozin etabonate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sergliflozin, a novel oral selective low-affinity sodium glucose cotransporter (SGLT2) inhibitor, improves hyperglycemia by suppressing renal glucose reabsorption, in which SGLT2 participates as a dominant transporter. Its prodrug form, sergliflozin etabonate, is orally available and is converted to sergiflozin upon absorption. Development of sergliflozin has been discontinued in favor of remogliflozin.
Status:
Investigational
Source:
NCT01229800: Phase 3 Interventional Completed Bowel Preparation, Efficacy, Tolerability, Safety
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)


Dapansutrile is an inhibitor of the NLRP3 inflammasome, developed by Olatec Therapeutics LLC. NLRP3 inflammasome is a driver of sterile inflammation in response to myocardial ischemia-reperfusion and other inflammatory conditions. Dapansutrile limits infarct size and prevents left ventricular systolic dysfunction in the mouse model of ischemia-reperfusion injury and suppresses joint inflammation in the mouse model of acute arthritis. Dapansutrile demonstrated a clinical and inflammatory cytokine response in a clinical trial for the treatment of acute gout and is being investigated for the treatment of Systolic Heart Failure and Schnitzler Syndrome.
Status:
Investigational
Source:
NCT00414869: Phase 2 Interventional Terminated Portal Hypertension
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)