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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 971 - 980 of 14117 results

Ruboxistaurin is an orally bioavailable, selective, potent inhibitor of protein kinase C β developed for treating diabetic retinopathy. In vitro and in vivo non-clinical models have demonstrated that Ruboxistaurin decreases PKC β activity and ameliorates many of the effects of PKC β on pathologic processes in the retina. Ruboxistaurin prevents the slowing of retinal blood flow that is observed by fluorescein video angiography in the eyes of diabetic rats. It is also reported to cause regression of retinal neovascularization produced by laser-induced major branch vein occlusions in a porcine model. Ruboxistaurin positively affected the diabetes-induced retinal blood flow abnormalities in a Phase Ib study in diabetic patients. Ruboxistaurin is in phase III clinical trials for the treatment of diabetic nephropathy and diabetic macular edema. Eli Lilly had submitted Ruboxistaurin for approval in the US and the EU; however, the company subsequently discontinued development as it was unable to demonstrate sufficient efficacy
Status:
Investigational
Source:
NCT00514501: Phase 2 Interventional Completed Acute Coronary Syndrome
(2007)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Iodofiltic Acid I-123 is a single-photon branching free fatty acid radiopharmaceutical with potential application in single-photon emission computed tomography (SPECT). Assessment of fatty acid metabolism by radionuclide techniques has a potential role for the early detection of myocardial ischaemia and the assessment of the severity of ischaemic heart disease. The Iodofiltic Acid I-123 scan is preferable because it can provide suitable information for risk stratification just after an acute myocardial infarction (AMI) without requiring the patient to exercise; it can also detect previous ischaemic insult even after recovery of myocardial perfusion, the so- called "ischaemic memory".
Status:
Investigational
Source:
INN:isoxaprolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

ISOXAPROLOL is a potent beta-adrenoceptor antagonist with antihypertensive properties. It was effective in lowering blood pressure in acute trials on spontaneously hypertensive rats at a dosage of 15 mg/kg.
Status:
Investigational
Source:
INN:fenbenicillin
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Fenbenicillin (phenoxybenzylpenicillin) is an acid-stable, orally active penicillin. Fenbenicillin demonstrated antibacterial activity in patients suffering from streptococcal, pneumococcal, and penicillin-sensitive staphylococcal infections.
Status:
Investigational
Source:
INN:pentorex
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Pentorex (Modatrop) is phenylisopropylamine derivative. It is a central adrenergic stimulant drug related to phentermine, which is used as an anorectic to assist with weight loss. Pentorex is sympathomimetic agent.
Status:
Investigational
Source:
USAN:Acebrochol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Acebrochol is a neuroactive steroid that may act as a sedative and hypnotic, through the mechanism of altering ligand-gated ion channels and cell surface receptors.
Status:
Investigational
Source:
NCT00844922: Phase 2 Interventional Completed Depressive Disorders
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ORG-34517 (or PT 150), a glucocorticoid receptor antagonist was development by Organon for the treatment of depression. This drug has completed phase II clinical trial for patients with major depression with psychotic features, however, this study was discontinued. In addition, Pop Test Cortisol LLC is developing ORG-34517 for the treatment of alcoholism. Now, this drug is in phase I clinical trial on stage recruiting to evaluate its safety when it is taken concurrently with alcohol.
Status:
Investigational
Source:
NCT00002315: Phase 3 Interventional Completed HIV Infections
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Netivudine [882C, 882C87, BW 882, Py-araU, Zonavir®] is an orally active thymidine analogue which was being investigated as a treatment for herpes zoster virus infections. Netivudine is a nucleoside analog with potent, specific activity against varicella-zoster virus. It is approximately seven times as potent as acyclovir with an in vitro 50% inhibitory concentration of 1 to 2 uM.
Status:
Investigational
Source:
INN:nitromifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nitromiphene (NIT; CI 628) is a triarylethylene antiestrogen shown to be effective in treatment of experimental breast cancer. Nitromiphene is one of the earliest nonsteroidal selective estrogen receptor modulators (SERMs). It is an anti-estrogen capable to translocate the estrogen receptor to the nucleus and to induce the replenishment of the cytosol receptor. Nitromiphene inhibited the uptake of [3H]-estradiol in rat whole homogenates and isolated cell nuclei tissues and the pituitary, and inhibited estradiol-induced female sexual behavior. Nitromiphene has thus been shown to suppress the growth of chemically induced and ransplantedmammary tumors in rodents. Also, Nitromiphene was shown to have potent, prolonged antiuterotropic effects in immature rats. Nitromiphene has been shown to undergo conversion to demethyl Nitromiphene (CI628M), a phenolic metabolite which had greater affinity for estrogen receptors and greater biological potency in vitro than did Nitromiphene. However, the in vivo antiestrogenic effects of Nitromiphene and demethyl Nitromiphene were similar, possibly due to facile O-demethylation of the former compound after administration.
Status:
Investigational
Source:
NCT00346502: Phase 1/Phase 2 Interventional Withdrawn Dysplastic Nevus Syndrome
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Betulinic acid (BA) is a plant-derived pentacyclic triterpenoid that exerts potent anti-cancer effects in vitro and in vivo. It`s anticancer property is linked to its ability to induce apoptotic cell death in cancer cells by triggering the mitochondrial pathway of apoptosis. In contrast to the cytotoxicity of betulinic acid against a variety of cancer types, normal cells and tissue are relatively resistant to betulinic acid, pointing to a therapeutic window. Compounds that exert a direct action on mitochondria present promising experimental cancer therapeutics, since they may trigger cell death under circumstances in which standard chemotherapeutics fail. Thus, mitochondrion-targeted agents such as betulinic acid hold great promise as a novel therapeutic strategy in the treatment of human cancers. Betulinic acid has antiretroviral, antimalarial, and anti-inflammatory properties. Betulinic acid exerts its inhibitory effect by preventing topoisomerase I-DNA interaction as a result of which the 'cleavable complex' is not formed. In consequence, it also acts as an antagonist to camptothecin-mediated cleavage. The antitumor pharmacological effects of BA consist of triggering apoptosis via the mitochondrial pathway, regulating the cell cycle and the angiogenic pathway via factors, including specificity protein transcription factors, cyclin D1 and epidermal growth factor receptor, inhibiting the signal transducer and activator of transcription 3 and nuclear factor‑κB signaling pathways, preventing the invasion and metastasis of tumor cells, and affecting the expression of topoisomerase I, p53 and lamin B1. Betulinic Acid has also been used in trials studying the treatment of Dysplastic Nevus Syndrome. Betulinic acid acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 uM. Betulinic acid is an inhibitor of HIV-1 with EC50 of 1.4 uM.