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

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Showing 421 - 430 of 4342 results

Status:
Investigational
Source:
NCT01794104: Phase 1 Interventional Completed Neoplasm
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Indotecan (LMP400) is a novel indenoisoquinoline derivative with specific topoisomerase I inhibition activity, developed by Division of Cancer Treatment and Diagnosis National Cancer Institute for cancer treatment. In preclinical studied Indotecan inhibited the cell growth of established mouse pheochromocytoma cell lines and primary human tumor tissue cultures. Low doses of Indotecan decreased the protein levels of hypoxia-inducible factor 1 (HIF-1α), one of a family of factors studied as potential metastatic drivers in these tumors. In vitro, Indotecan showed an increase in the growth-inhibitory effects in combination with other chemotherapeutic drugs that are currently used for the treatment of pheochromocytoma. Recently Indotecan has entered Phase I clinical trials for the treatment of cancer patients at the National Cancer Institute, and definite plans are being formulated to commence Phase II clinical trials.
Status:
Investigational
Source:
INN:cloperidone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cloperidone is a quinazolinedione derivative with sedative and antihypertensive properties. Cloperidone was discovered in 1965 by Miles Laboratories. The activity of the compound was demonstrated by behavioral observations in dogs and cats, by rotarod and activity cage experiments in mice and in other models.
Status:
Investigational
Source:
INN:delprostenate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Delprostenate is a synthetic analogue of PGF2-alpha, which is the naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. It is a useful synchronizer for the sheep.
Status:
Investigational
Source:
JAN:OMBRABULIN HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Ombrabulin is an experimental drug candidate discovered by Ajinomoto and further developed by Sanofi-Aventis for cancer treatment. Ombrabulin is a synthetic water-soluble analog of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrate, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis. Ombrabulin has been used in trials studying the treatment of Sarcoma, Neoplasms, Solid Tumor, Neoplasms, Malignant, and Advanced Solid Tumors, among others. In January 2013, Sanofi said it discontinued development of Ombrabulin after disappointing results from phase III clinical trials.
Status:
Investigational
Source:
USAN:LEVALBUTEROL SULFATE [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:misonidazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Targets:


Misonidazole is a nitroimidazole with radiosensitizing and antineoplastic properties. Exhibiting high electron affinity, misonidazole induces the formation of free radicals and depletes radioprotective thiols, thereby sensitizing hypoxic cells to the cytotoxic effects of ionizing radiation. This single-strand breaks in DNA induced by this agent result in the inhibition of DNA synthesis. The drug also possesses a substantial cytotoxic effect, independent of radiation, which is selectively expressed in hypoxic cells. Misonidazole may be cytotoxic to the normal hypoxic tissues in the human body, making this became a major concern in the clinical application of the drug. Misonidazole leads to strand breaks in cellular DNA and those cells which fail to survive also fail to repair these strand breaks. Misonidazole depletes intracellular glutathione and is more toxic in glutathione depleted cells.
Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of common anxiety disorders, posttraumatic stress disorder and major depressive disorder. It’s in phase II clinical trials as an effective inhibitor of itch-associated response.
Status:
Investigational
Source:
INN:ioglucomide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ioglucomide is triiodoanilide derivative patented by Mallinckrodt, Inc. as nonionic x-ray contrast media for myelography. In preclinical studies the efficacy of ioglucomide and metrizamide were comparable. However, acute toxicity after intravenous injection or installation into cerebrospinal fluid was significantly less for ioglucomide. Also, in contrast to metrizamide, ioglucomide produced no evidence of any type of convulsive activity after subarachnoid administration.
Status:
Investigational
Source:
INN:fludorex
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

FLUDOREX is an antiemetic and anorexic agent.
Status:
Investigational
Source:
INN:rifamide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rifamides (NSC-143418) are drugs used in the treatment of tuberculosis. They also have immunosuppressive activity, the exact mechanism of which is still unknown, although the ability of rifamides to inhibit tumor necrosis factor (TNF)-induced NF-kB activation may be associated with it. A variety of rifamide analogues exist, such as rifamycin B, rifapentine, rifamycin SV, rifabutin and rifampicin.