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

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Showing 551 - 560 of 4933 results

Status:
Investigational
Source:
INN:mexrenoate potassium [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mexrenoate potassium is an aldosterone antagonist, which was developed as an antihypertensive agent. However, this drug has never been marketed.
Status:
Investigational
Source:
INN:iocanlidic acid (¹²³I) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Iocanlidic Acid I-123 is a radiolabeled phenylfatty acid derivative studied as a diagnostic agent for myocardial imaging
Abexinostat (PCI-24781) is a novel, second-generation phenyl hydroxamic acid–based, orally bioavailable HDAC inhibitor that has previously been shown to have activity in vitro and in vivo against a broad array of cancers, including hematopoietic malignancies and bone and soft-tissue sarcomas. Abexinostat is a pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Abexinostat exhibits potent antitumor activity against a variety of tumor cell lines with GI50 ranging from 0.15 uM to 3.09 uM. PCI-24781 also has an antiproliferative effect on HUVEC endothelial cells with GI50 of 0.43 uM. Abexinostat treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells, induces expression of p21, and leads to PARP cleavage and accumulation of the γH2AX. It has also shown good tolerability and activity in Phase I and II clinical trials against lymphoma, as well as against solid tumors in Phase-I trials. Additionally, it acts as a potent radiosensitizing agent and is synergistic with cytotoxic chemotherapy, such as doxorubicin in preclinical models.
Status:
Investigational
Source:
USAN:Antimony Sodium Thioglycollate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Antimony sodium thioglycollate is an anthelmintic agent. It is a schistosomicide drug.
Status:
Investigational
Source:
NCT00605787: Phase 2 Interventional Completed Type 2 Diabetes Mellitus
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tetradecylthioacetic acid (TTA) is a hypolipidemic antioxidant with immunomodulating properties involving activation of peroxisome proliferator-activated receptors (PPARs). TTA exerts both hypolipidemic and anti-inflammatory effects in psoriasis patients - TTA can be of therapeutic benefit for a subgroup of psoriatic patients. TTA may improve myocardial function in heart failure, potentially involving its ability to decrease the availability of free fatty acids in plasma and increase the myocardial proportion of n-3 polyunsaturated fatty acids. TTA attenuates dyslipidemia in patients with type 2 diabetes mellitus. These effects may occur through mechanisms involving PPAR-alpha and PPAR-delta activation, resulting in increased mitochondrial fatty acid oxidation.
Status:
Investigational
Source:
NCT04290897: Phase 2 Interventional Recruiting Anatomic Stage 0 Breast Cancer AJCC v8
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxaloacetate (OAA), a salt of oxaloacetic acid, is a metabolic intermediate in many processes, e.g., urea cycle, gluconeogenesis, etc. that occur in animals. Experiments on animal have revealed that OAA was able to protect hepatocytes from hypoxia and liver ischemia/reperfusion injury. OAA also possesses a neuroprotective effect against ischemic injury, which strengthens the likelihood of its future applicability as a novel neuroprotective agent for the treatment of ischemic stroke patients. In addition, experiments on adipose stromal cells have shown that OAA directly protected cerebellar granule neurons from apoptosis induced by serum and potassium deprivation.
Status:
Investigational
Source:
INN:gosogliptin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Gosogliptin (PF-734200) is a compound developed for treatment of type II diabetes and has been approved for use in Russia. It is a selective dipeptidyl peptidase 4 (DPP-4) inhibitor, with hypoglycemic activity. The drug is safe and well tolerated at all doses tested when added to metformin (a diabetes drug), and safely and effectively lowered HbA (1c) in subjects receiving metformin. A phase 3 study to study the safety and efficacy of gosogliptin has been completed. Gosogliptin has also been studied as potential drug for the treatment of renal insufficiency.
Status:
Investigational
Source:
NCT01371604: Phase 2 Interventional Completed Hepatitis C, Chronic
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sipoglitazar (TAK 654) was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARγ, PPARα, and PPARδ. Sipoglitazar was developed to improve peripheral insulin sensitivity, normalize circulating lipid profiles, and reduce body weight in patients with metabolic syndrome and type 2 diabetes mellitus (T2DM). Sipoglitazar was being developed by Takeda for the treatment of diabetes mellitus, however in September 2006, development was discontinued.
Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.