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

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Showing 6781 - 6790 of 13501 results

Status:
Investigational
Source:
NCT00104364: Phase 1 Interventional Completed Cancer
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT00820560: Phase 1 Interventional Completed Solid Tumors and Hematologic Malignancy
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Aderbasib, also known as INCB007839, is an orally bioavailable low nanomolar hydroxamate-based inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Aderbasib represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation. In preclinical studies, Aderbasib with lapatinib prevented the growth of HER-2/neu–positive BT474-SC1 human breast cancer xenografts in vivo. Aderbasib was being developed by Incyte as a potential adjunctive treatment for metastatic breast cancer. Aderbasib in combination with trastuzumab increased the response rate in HER2 positive metastatic breast cancer patients with advanced disease, relative to historical controls (50% versus 15–35%). INC7839 also improved progression-free survival in a subset of the patients expressing the p95 fragment of HER2. Aderbasib development was halted in 2011 after positive findings from Phase II trials were contradicted by further research. Aderbasib is currently being tested in combination with rituximab for diffuse large B cell non-Hodgkin lymphoma.
Status:
Investigational
Source:
NCT00001933: Phase 2 Interventional Completed Alzheimer's Disease
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nefiracetam is a cyclic derivative of gamma-aminobutyric acid (GABA). It is thought to act by normalising dysfunctional acetylcholine, GABA and possibly monoamine neurotransmitter systems, but it may also facilitate N/L-type calcium channel opening. Nefiracetam has received attention as a treatment for seizures, depression, and dementia. Nefiracetam was found to be extremely testicular toxic in both rats and dogs; it was found to significantly decrease the levels of testicular testosterone leading to atrophy and malformation of sperm.
Status:
Investigational
Source:
INN:lotrifen [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lotrifen is a non-hormonal abortifacient agent. It is used in veterinary. Lotrifen causes the arrest and involution of pregnancy. It acts, after the implantation of the blastocyst, directly on the product of conception, which undergoes a slow and gradual degenerative process and ends with the reabsorption or expulsion of it.
Status:
Investigational
Source:
INN:lozilurea [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Lozilurea (N' -3-chlorobenzyl-N'-ethylurea, ITA 312) has shown marked anti-ulcer activity. It has shown itself to be active against chemically and neurogenically induced gastric and duodenal lesions in various experimental animal models. It has no major anti-secretory action. The experimental data obtained suggest that the mechanism of action of lozilurea consists in increasing the protective function of the mucus barrier. It increased gastric levels of hexosamines and mucoproteins. In the screening trials carried out in order to detect the side effects of lozilurea, it has shown sedative, antipyretic and vasodilatory actions.
Status:
Investigational
Source:
NCT00002218: Phase 1 Interventional Completed HIV Infections
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:tresperimus
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tresperimus is a new stable immunosuppressive analog of 15-deoxyspergualin (DSG) obtained by organic chemical synthesis. It was initially developed as an antitumor agent. Tresperimus has been designed to be chemically stable in aqueous solution. Tresperimus controlled alloreactivity in a fully major histocompatibility complex (MHC) mismatched rat cardiac transplant model and also induced donor-specific long-lasting unresponsiveness. Posttransplant tresperimus therapy effectively protected mice from lethal graft-versus-host disease (GVHD) in a dose-related manner. It has been shown to suppress graft rejection as efficiently as cyclosporine A. Indeed, a short course of tresperimus has similar or better effects compared to the effects of cyclosporine in bone marrow, cardiac, and skin transplant models. Prevention of rejection is related to the induction of donor-specific tolerance without affecting immunity to third-party antigens. In addition, CD4+ T-cells from tresperimus-treated animals can transfer donorspecific tolerance to naive animals, an effect not seen with cyclosporine or other traditional immunosuppressive drugs. The mechanism by which tolerance is induced is not clear. Tresperimus binds to Hsc70, a heat shock protein– chaperoned peptide that, among other effects, inhibits nuclear localization of nuclear factor (NF)-kB, which is required for CD40 and CD28 ligation signaling in antigen-presenting cells, an important early step in T-cell costimulation. Locally administered tresperimus appears to be a potential immunosuppressive agent in the management of intraocular inflammation. Tresperimus had been in phase III clinical trial for the treatment of graft-versus-host disease. However, this development was discontinued.
Status:
Investigational
Source:
INN:suritozole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Suritozole (also known as MDL 26,479) is an aryldialkyltriazolethione derivative patented by Merrell Dow Pharmaceuticals, Inc as an antidepressant. Suritozole acts as negative modulator at the gamma-aminobutyric acid A (GABAA) receptor that enhances cholinergic function. In preclinical models, chronic treatment Suritozole produces a small but significant decrease in the average spontaneous firing rate of Purkinje neurons. Suritozole attenuated a scopolamine-induced acquisition deficit in a T-maze reinforced alternation task, suggesting that the compound may have memory enhancing potential.
Status:
Investigational
Source:
INN:cinalukast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Cinalukast (Ro 24-5913 ) is a selective leukotriene D4 receptor antagonist originated by Roche. Cinalukast inhibits the actions of Leukotriene D4 at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Leukotriene receptor occupation has been correlated with the pathophysiology of asthma, including airway edema and altered cellular activity associated with the inflammatory process, which contributes to the signs and symptoms of asthma. Cinalukast had been investigated for the treatment of asthma, but that study was discontinued.
Status:
Investigational
Source:
NCT01990755: Not Applicable Interventional Completed Anorexia Nervosa
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Delorazepam is a benzodiazepine with anxiolytic effects. It is a metabolite of the designer drug diclazepam that can be detected in either the serum or urine. Delorazepam can also be produced by enzymatic treatment of lorazepam with β-glucuronidase. It is indicated for the treatment of anxiety, tension and other somatic or psychiatric manifestations associated with anxiety syndrome, insomnia. The side effects and precautions for use of delorazepam are the same as for all benzodiazepines, in particular as regards the development of dependence (mental and physical) and tolerance. Prolonged use may lead to difficulties remembering recent names and events (anterograde amnesia). It has been approved for marketing in Italy.

Showing 6781 - 6790 of 13501 results