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 7951 - 7960 of 167129 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Taltobulin, also known as HTI-286 and SPA-110, is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-based resistance to taxanes. Taltobulin was a potent inhibitor of proliferation (mean IC50 = 4 nm in 18 human tumor cell lines) and had substantially less interaction with multidrug resistance protein (P-glycoprotein) than currently used antimicrotubule agents, including paclitaxel, docetaxel, vinorelbine, or vinblastine. Taltobulin showed strong antitumor activity both in androgen-dependent and androgen- independent tumors and may be a promising agent in second- line treatment strategies for patients suffering from docetaxel- refractory prostate cancer.
Status:
Investigational
Source:
NCT01413932: Phase 1/Phase 2 Interventional Completed Healthy Volunteers (Part 1)
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT02125786: Phase 2 Interventional Active, not recruiting Ependymoma
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

METHIONINE C-11 is a synthetic amino acid radiolabeled with carbon-11. Acting as a methyl donor, methionine C 11 is incorporated into macromolecules, where it serves as a positron emission tomography (PET) imaging agent for detecting tumors with high rates of protein synthesis. METHIONINE C-11 is produced without any significant radiochemical impurities.
Status:
Investigational
Source:
NCT01269242: Phase 2 Interventional Completed Coronary Restenosis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Bindarit (2-Methyl-2-[[1-(phenylmethyl)-1H-indazol-3yl]methoxy]propanoic acid; AF-2838) is an indazolic derivative that is devoid of any immunosuppressive effects and has no effect on arachidonic acid metabolism. It has been proved to have anti-inflammatory activity in a number of experimental diseases, including pancreatitis, arthritis, and lupus nephritis. This therapeutic effect has been associated with its ability to interfere selectively with monocyte recruitment, although the underlying molecular mechanisms are unknown. Bindarit selectively inhibits the production of the monocyte chemotactic protein subfamily of CC inflammatory chemokines (MCP-1/CCL2, MCP-3/CCL7, MCP-2/CCL8) without affecting the production of the cytokines IL-1, IL-6, or the chemokines IL-8, MIP-1α.
Status:
Investigational
Source:
NCT00005093: Phase 3 Interventional Completed Lung Cancer
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



A second generation of HDACs, synthetic benzamide-containing HDACs such as Tacedinaline (CI-994), have reached phase I and II clinical trials. It has been investigated for its applications to the treatment of cancers such as Breast cancer and Colorectal cancer. Tacedinaline has been in phase III clinical trials by Pfizer for the treatment of advanced non-small cell lung cancer and pancreatic cancer combined with gemcitabine. However, this research has been discontinued. Mechanism of Action: Angiogenesis inhibitors; Histone deacetylase inhibitors. Pharmacokinetics showed that CI-994 absorption and disposition were unaffected by carboplatin and paclitaxel coadministration.
Status:
Investigational
Source:
NCT00124696: Phase 1 Interventional Completed Cocaine-Related Disorders
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cocaethylene is the ethyl ester of benzoylecgonine. Cocaethylene is formed in the liver after concurrent use of cocaine and alcohol. Cocaethylene works by blocking the dopamine transporter on dopaminergic presynaptic nerve terminals in the brain. It increases dopamine synaptic content, provoking enhanced postsynaptic receptor stimulation, resulting in euphoria, reinforcement, and self-administration. Compared to cocaine, which is a methyl ether of benzoylecgonine, cocaethylene has three to five times larger half-life in plasma. Cocaethylene is associated with seizures, liver damage and compromised the functioning of the immune system. It carries an 18-25 fold increase in risk for immediate death compared to cocaine alone.
Status:
Investigational
Source:
INN:oxodipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Oxodipine is a dihydropyridine calcium channel blocker that has been developed by IQB as an antihypertensive agent. Experiments on dogs have shown that oxodipine exerted a relatively specific action on blood vessels without significant intrinsic negative chronotropic properties. in addition, in Europe, the drug was involved in phase III clinical trials in and in phase II for the treatment of Hypertension. Besides, oxodipine was studied for the treatment of ischaemic heart disorders. However, these studied were discontinued.
Status:
Investigational
Source:
INN:hydroxindasate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Hydroxindasate is a 5-hydroxytryptamine receptor antagonist.
Status:
Investigational
Source:
INN:hydracarbazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Hydracarbazine, a diuretic, was used in France under the brand name Normatensyl as an antihypertensive drug.
Dactolisib is a dual inhibitor of phosphatidylinositol 3-kinase (P13K) and the downstream mammalian target of rapamycin (mTOR) by binding to the ATP-binding cleft of these enzymes (inhibitor of PI3K/Akt/mTOR cascade). It is being investigated as a possible anti-cancer cancer agent and drug against Influenza virus infections. Frequently reported adverse events included nausea, vomiting, diarrhoea, fatigue/asthenia, anaemia, and anorexia.

Showing 7951 - 7960 of 167129 results