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

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Showing 581 - 590 of 4351 results

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

Class (Stereo):
CHEMICAL (RACEMIC)

Cimoxatone is a fully reversible inhibitor selective for the A form of monoamine oxidase. Oral administration of Cimoxatone increased brain noradrenaline, dopamine, and serotonin and decreased DOPAC , 5-HIAA, and 3-methoxy-4-hydroxyphenylethylene glycol sulfate.
Status:
Investigational
Source:
INN:bucrilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Bucrylate (isobutyl cyanoacrylate) is a liquid tissue adhesive for transcatheter embolization. It is used in radiological and endoscopic interventions to occlude vessels and to stop bleedings. In comparison with sponges, coils and plugs, bucrylate is inexpensive and achieves immediate, irreversible and complete occlusion of the vessel irrespective of coagulation deficiencies.
Status:
Investigational
Source:
NCT03440632: Not Applicable Interventional Completed Cerebral Palsy
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zearalenone (ZEN) is a toxic non-steroidal mycoestrogen produced by fungi that widely contaminate agricultural products, eliciting estrogenic responses by mimicking sex steroid hormones. Zearalenone is biosynthesised through a polyketide pathway by a variety of Fusarium fungi including Fusarium graminearum (Gibberella zeae), Fusarium culmorum, Fusarium equiseti, Fusarium crookwellense, Fusarium cerealis and Fusarium semitectum. Zearalenone and its derivatives share similar molecular mechanisms and activity with estrogens. They interact with the estrogen receptors (ERa and ERb) leading to functional and morphological changes in the reproductive system in both animals and humans. Zearalenone exposure is associated with the estrogenic syndrome and infertility in animals and premature thelarche and precocious puberty in girls. In animal models, it was found that prepubertal exposure to a low dose of Zearalenone, decreased breast cancer risk. When prepubertal rats were treated with 20 lg (1 mg ⁄ kg body weight) of Zearalenone, a significant reduction of both the incidence and multiplicity of DMBA-induced mammary tumours was noted. Zearalenone has been used to treat postmenopausal symptoms in women.
Status:
Investigational
Source:
NCT04464070: Early Phase 1 Interventional Enrolling by invitation Metabolism of Prostaglandin D2
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



PGD2 (Prostaglandin D2) is a major cellular regulator, has been shown to bind different receptors: D prostanoid receptor (DP) and chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). PGD2 reportedly inhibits platelet aggregation, the proliferation of cells, and activation of neutrophils. This compound is also a potent vasodilator that also relaxes smooth muscle but causes contraction of the bronchial airways. PGD2 promotes T cell migration via CRTH2 and aggravates asthma. In contrast, there have been some studies suggesting that PGD2 exerts anti-inflammatory effects via DP, such as inhibiting the migration and activation of neutrophils, basophils, dendritic cells and T cells. Elevated levels of prostaglandin D2 (PGD2) have been shown to be present in the bald scalp of androgenic alopecia (AGA) patients and was suggested the PGD(2)-GPR44 pathway as a potential target for treatment. Also was revealed, that PGD2 might be a new target for asthma therapy, PGD2 in serum and BALF were lower in the treated group than in the untreated group.
Status:
Investigational
Source:
INN:brocresine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Brocresine, an aromatic L-amino acid decarboxylase inhibitor with both a peripheral and central action was shown to potentiate the therapeutic effect of levodopa in Parkinson's disease.
Status:
Investigational
Source:
NCT04227756: Phase 1 Interventional Completed Healthy
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01931241: Phase 1 Interventional Unknown status Hypercholesterolemia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Hyodeoxycholic acid, also known as HDCA, is a secondary bile acid. Natural 6alpha-hydroxylated bile acids are receptor-specific activators of nuclear liver X receptor alpha (LXRalpha), a nuclear receptor regulating the expression of the cholesterol 7alpha-hydroxylase gene. AHRO-001 (Hyodeoxycholic acid) is in phase I clinical trials for the treatment of atherosclerosis. Through a complex signaling processes utilizing LXR receptors, the compound is designed to increase the efficiency of cholesterol efflux using the HDL cells, which act on all cholesterol in the arterial circulation as well as in the lipid core of plaque deposits in the artery walls. Use of AHRO-001 has shown no adverse effects on morbidity, mortality or toxicity and has been well tolerated at high doses.
Status:
Investigational
Source:
INN:triflumidate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Triflumidate is a fluoroalkanesulfonanilide. It had been identified for clinical trials. This non-steroidal compound is an anti-inflammatory agent.
Status:
Investigational
Source:
NCT02664181: Phase 2 Interventional Active, not recruiting Lung Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Tetrahydrouridine is a potent competitive reversible inhibitor of cytidine deaminase. Tetrahydrouridine can inhibit cell proliferation by regulation of the cell cycle independent of cytidine deaminase (CDA) expression levels. Tetrahydrouridine may be useful for researching potential treatments for high CDA-expressing tumors. Tetrahydrouridine use, alone or in combination with the DNA methyltransferase inhibitor 5-fluoro-2’-deoxycytidine, is being evaluated in animal models and clinical trials for diseases, including cancer and mitochondrial DNA depletion syndrome.
Status:
Investigational
Source:
USAN:Amonafide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amonafide is an imide derivative of naphthalic acid. It is a novel topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA. Amonafide retains cytotoxic activity even in the presence of P-glycoprotein (Pgp)-mediated multi-drug resistance (MDR). It is a new investigational anticancer drug. Amonafide has been extensively studied in patients with malignant solid tumors, like prostate cancer, breast cancer and others. When its usefulness in the treatment of various solid malignancies proved limited, focus was shifted to establishing its use as an antileukemic agent, specifically against secondary and treatment-associated acute myeloid leukemia (AML).