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

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Showing 271 - 280 of 4873 results

Elocalcitol (also known as BXL-628), a vitamin D3 analog. This compound regulates cell proliferation and apoptosis via its binding to the vitamin D receptor (VDR) having anti-proliferative and anti-inflammatory properties in benign prostatic hyperplasia (BPH) treatment. In a phase, IIb trial in patients with BPH, treatment with elocalcitol resulted in a significantly reduced prostate volume compared with placebo; irritative urinary symptoms (frequency, urgency, and nocturia) and urodynamic parameters were comparable to the alpha1-adrenoceptor antagonist tamsulosin. In a phase IIa trial in patients with prostatitis, elocalcitol significantly reduced levels of IL-8 in semen, suggesting improved quality and forward motility of sperm. However, phase IIb trial data from patients with overactive bladder (OAB) were less promising: elocalcitol failed to meet the primary endpoint despite demonstrating good efficacy in a phase IIa trial. Based largely on these disappointing data, BioXell decided to terminate all further clinical development of elocalcitol, including an uncompleted phase IIa trial in patients with male infertility. Recently was shown, that VDR agonists as elocalcitol could be therapeutic tools for skeletal muscle integrity/function maintenance, an indispensable condition for health homeostasis.
Status:
Investigational
Source:
INN:iometin (¹²⁵I) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Iomethin I-125 is radioiodinated quinoline derivative with potential tumor localizing activity.
Status:
Investigational
Source:
INN:xantifibrate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

AstraZeneca was developing AZD-8055, an orally active mTORC1/mTORC2 inhibitor, for the treatment of advanced solid tumours. AZD-8055 is an ATP-competitive mTORC1/2 inhibitor that exhibits immunosuppressive and anticancer chemotherapeutic activities. AZD-8055 promotes antibody class switching in B cells at low doses and decreases B cell proliferation and differentiation at high doses. In vivo, this compound suppresses CC4 and CD8 T cell proliferation, increasing survival among MHC-mismatched heart transplant recipients. In vitro, AZD-8055 decreases viability of brain tumor cells; in vivo, it inhibits tumor growth. AZD-8055 had been in phase I trials by AstraZeneca for the treatment of malignant gliomas and solid tumours. However, this research has been discontinued.
Status:
Investigational
Source:
NCT02946060: Not Applicable Interventional Completed Physical Activity
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT03465384: Not Applicable Interventional Completed Oppositional Defiant Disorder
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00525213: Phase 2 Interventional Completed Rheumatoid Arthritis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Rabeximod is an indolo[2,3-b]quinoxaline derivative patented by OxyPharma AB as anti-inflammatory agent useful for the treatment of autoimmune disease. Rabeximod impaired monocyte differentiation into monocyte-derived dendritic cells and pro-inflammatory allostimulated macrophages. Monocyte-derived dendritic cells that were treated with Rabeximod resulted in a significant decrease in their ability to pinocytose antigens, while no effect was exerted by the drug on the ability of allostimulated macrophages and anti-inflammatory macrophages to phagocytose. Rabeximod reduces the severity of arthritis in rodent models of rheumatoid arthritis and multiple sclerosis. Rabeximod efficiently prevented arthritis during the time window when TLR2 or TLR4 ligands activate inflammatory macrophages.
Status:
Investigational
Source:
INN:moxilubant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Moxilubant is an orally active leukotriene B4 antagonist patented by Ciba-Geigy A.-G. and studied for psoriasis, rheumatoid arthritis, and chronic obstructive pulmonary disease treatment. Moxilubant inhibits LTB4 signaling with a potency of 2–4 nM. In a phase 1 study in 10 healthy volunteers, Moxilubant was administered orally once or twice daily for 7 days at doses ranging from 100 to 500 mg. At dose levels of 150 mg and above, LTB4 pathway inhibition reached at least 75%. At doses of 300 mg and above, pathway inhibition reached 100%. A Phase 2 study was conducted in 24 patients with COPD treated with 240 mg/day Moxilubant for 4 weeks. In this study, there were no changes in sputum cell counts or biomarkers or in spirometry measures, even though plasma levels of Moxilubant were sufficient to significantly reduce pathway signaling.
Status:
Investigational
Source:
NCT01494441: Not Applicable Interventional Completed Degenerative Disc Disease
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bathocuproine is a promising organic material of a hole blocking layer in organic light-emitting diodes or an electron buffer layer in organic photovoltaic cells. When a thin layer of bathocuproine is inserted between the metal electrode and the organic layer of the organic semiconductor device, the electron injection/collection efficiency at the interface is significantly improved. As an organic electronic material bathocuproine useful as OLED electron transporter and hole blocker. Bathocuproine sulphonate acts as a specific chelator of monovalent copper Cu(I).
Status:
Investigational
Source:
NCT03189394: Phase 1 Interventional Unknown status HIV Infections
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fluridone, an herbicide that used for controlling invasive aquatic plants such as hydrilla in surface water bodies. It inhibits carotenoid synthesis in targeted plant species, preventing photosynthesis and ultimately causing mortality. This compound contains a 4(1H)-pyridone and a trifluoromethyl-benzene moiety, which are also present in molecules with analgesic and anti-inflammatory properties. Experiments on rodents have confirmed that fluridone could represent a new prototype of an anti-inflammatory drug.