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

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Showing 941 - 950 of 16236 results

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

Class (Stereo):
CHEMICAL (RACEMIC)

Olpimedone was developed as an anti-rheumatic agent and analgesic, however, the drug that has never been marketed. Information about the current use of olpimedone is not available.
Status:
Investigational
Source:
INN:litracen [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Litracen revealed very potent thymoleptic properties with a weak sedative action. Melitracen is gradually metabolized to litracen, and after repeated doses of melitracen, the organs will, for the most part, contain the metabolite. Litracen was developed as an antidepressant agent.
Edelfosine is a synthetic alkyl-lysophospholipid, a potent immunomodulator and an effective inhibitor of tumor cell proliferation. The cytotoxic effect of edelfosine has been evaluated in a large variety of both tumor (leukemic and solid) and normal cell types, showing a high degree of selectivity towards tumor cells. Like all alkyl-lysophospholipids, Edelfosine incorporates into the cell membrane and does not target the DNA. In many tumor cells, Edelfosine causes selective apoptosis, sparing healthy cells. Edelfosine can activate the Fas/CD95cell death receptor, can inhibit the MAPK/ERK mitogenic pathway and the Akt/protein kinase B (PKB) survival pathway. Edelfosine apoptosis-inducing abilities were studied with several types of cancer, among them multiple myeloma and non-small and small cell lung carcinoma cell lines. In vivo activity against human solid tumors in mice was shown against malignant gynecological tumor cells, like ovarian cancer, and against breast cancer. In vivo biodistribution studies demonstrated a “considerably higher” accumulation of Edelfosine in tumor cells than in other analyzed organs. Several clinical trials were conducted. Among them, a phase I trials with solid tumors or leukemias and phase II with non-small-cell lung carcinomas (NSCLC). In Phase II clinical trial for use of Edelfosine in treating leukemia with bone marrow transplants, it was found to be safe and 'possibly effective'. A phase II trial for the treatment of brain cancers was also reported. It showed encouraging results in stopping the growth of the tumor and a considerable improvement in the “quality of life” of the patients. A phase II trial on the effect of Edelfosine on advanced non-small-cell bronchogenic carcinoma had a “remarkable” “high proportion of patients with stationary tumor status” as result, stable disease after initial progression in 50% of the patients.
Status:
Investigational
Source:
INN:propizepine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Propizepine is a benzodiazepinone derivative patented by Laboratoires U.P.S.A. as antidepressive, antihistaminic, antianaphylactic, thymoanaleptic, antiserotonine, antispasmodic, and analgetic compound. Propizepine used in France for the treatment of depression in the 1970s.
Status:
Investigational
Source:
INN:elbanizine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Elbanizine [HWA 214] is an antihistamine which was undergoing preclinical trials with Hoechst Marion Roussel in Germany for the treatment of allergic asthma. Elbanizine does not have such drawbacks as causing drowsiness or being effective only as a prophylactic drug, and could provide advantages over other non-sedative compounds, such as terfenadine and astemizole, in that it is water soluble and thus can be administered through inhalation or through intravenous application.
Status:
Investigational
Source:
INN:triclazate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Triclazate is an anticholinergic agent.
Status:
Investigational
Source:
INN:mobecarb [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Mobecarb is morpholineacetic acid derivative patented by Carlo Erba Societa per Azioni to prevent vascular rupture among persons afflicted with arterial hypertension. In preclinical models Mobecarb shows the capillary protective activity in partially omentectomized rats.
Status:
Investigational
Source:
NCT00090090: Phase 2 Interventional Completed Mantle Cell Lymphoma
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Elsamitrucin is a heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. It demonstrated a broad spectrum of in vitro cytotoxicity against tumor cell lines. According to the results of Phase II trials elsamitrucin is not an active drug in patients with metastatic breast cancer, colorectal cancer, non-small cell lung cancer or ovarian cancer, however, it showed modest activity in patients with relapsed or refractory non-Hodgkin's lymphoma.
Status:
Investigational
Source:
NCT00275197: Phase 2 Interventional Completed Depressive Disorder, Major
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Elzasonan (CP 448187) is a serotonin 1B/1D receptor antagonist. Elzasonan was primarily metabolized via oxidative N‐demethylation, N‐oxidation, and aryl hydroxylation. Pfizer was developing elzasonan for the treatment of anxiety and affective disorders however development has been discontinued.
Status:
Investigational
Source:
INN:scopinast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Scopinast (previously known as KA 398) was studied for the treatment of asthma and allergic seasonal. However, the further development of the drug was discontinued.