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

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Showing 41 - 50 of 1021 results

Status:
Investigational
Source:
INN:sibrafiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sibrafiban (G-7453) is the orally administered, nonpeptide, double-prodrug of Ro 44-3888 which is a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban is a double prodrug that undergoes bioconversion to the inactive prodrug Ro 48-3656 and to the active IIb/IIIa antagonist, Ro 44-3888, after oral administration. Sibrafiban was undergoing clinical trials for secondary prevention of cardiac events in patients stabilised after acute coronary syndromes. Sibrafiban has been shown to have comparable efficacy to aspirin in preventing recurrent ischemic events in patients suffering from acute coronary syndromes. Sibrafiban was under development by Genentech and Hoffmann-La Roche, and in phase III trials as an antithrombotic. The development of sibrafiban was discontinued in 1999 following unfavorable Phase III efficacy data.
Status:
Investigational
Source:
JAN:BROFLANILIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

E-7090 is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity. It is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. E-7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses E-7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E-7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E-7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR. Furthermore, E-7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. It is being investigated in a Phase I clinical trial for treatment of patients with solid tumors.
Status:
Investigational
Source:
INN:yttrium (⁹⁰Y) anditixafortide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
JAN:TOLVAPTAN SODIUM PHOSPHATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:iomorinic acid
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Iomorinic Acid is triiodobenzamide derivative patented by Lentia G.m.b.H. as a radiographic contrast medium for liver imaging.
Status:
Investigational
Source:
INN:ofornine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ofornine is a vasodilator with antihypertensive activity. Experiments on rats have shown that ofornine reduced spontaneously hypertensive (SH) blood pressure through vasodilating and presynaptic adrenolytic activities, and that a dopaminergic mechanism may be involved. Information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:cilofungin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ilofungin is a narrow spectrum antimycotic patented by a pharmaceutical company Eli Lilly and Co in 1981. Cilofungin is particularly active against the opportunistic fungal pathogen Candida albicans. Cilofungin action is exerted through inhibition of the synthesis of (1,3)-beta-glucan, an essential cell wall component, it invades a fungus' ability to synthesize cell walls.
Status:
Investigational
Source:
INN:oxarbazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Oxarbazole was developed as an antiasthmatic agent that inhibited the only bronchoconstriction induced by immune complexes. This drug has never been marketed.