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

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Showing 61 - 70 of 1547 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tafluposide (also known as F 11782) is an epipodophyllotoxin derivative patented by Pierre Fabre Medicament as an antitumor agent. Tafluposide acts as a catalytic inhibitor of topoisomerases I and II, that capable of completely inhibiting the DNA-binding activity of topoisomerase. In preclinical models single or multiple i.p. doses of Tafluposide proves highly active against the s.c. grafted B16 melanoma, significantly increasing survival and inhibiting tumor growth. Tafluposide inhibits the number of pulmonary metastatic foci of the melanoma by 99%. In human tumor xenograft studies, multiple i.p. doses of Tafluposide results in major inhibitory activity against breast) tumors, as well as causing definite tumor regression. Significant activity was also recorded Tafluposide against the refractory lung xenografts.
Status:
Investigational
Source:
INN:flufosal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FLUFOSAL is an antithrombotic agent.
Status:
Investigational
Source:
INN:doxibetasol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Doxybetasol is the corticosteroid. It is an impurity of Betamethasone, which is a glucocorticoid used as an anti-inflammatory agent. Doxybetasol also has anti-inflammatory and anti-allergic properties.
Status:
Investigational
Source:
USAN:OCTICIZER [USAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Octicizer is used as a plasticizer.
Status:
Investigational
Source:
NCT00264914: Phase 3 Interventional Completed Inappropriate ADH Syndrome
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Fosbretabulin (Combretastatin A4 phosphate, CA4P) is the lead compound of a relatively new class of agents termed vascular disrupting agents that target existing tumor blood vessels. Rapid tumor blood flow shutdown has been demonstrated in preclinical models and patients by various techniques such as dynamic contrast-enhanced MRI, perfusion computed tomography and PET scans following CA4P infusion. CA4P typically induces rapid tumor necrosis in the center of the tumor and leaves a rim of viable cells in the periphery. In oncology, CA4P does not appear to be that active by itself, but may be more efficacious when combined with chemotherapy, antiangiogenic therapy and radiation therapy. Combretastatin was initially isolated from the root bark of the South African Bush willow Combretum caffrum in 1982 by Pettit and colleagues at the Arizona State University (AZ, USA). Combretastatin A4 phosphate binds avidly to tubulin at the colchicine-binding site to inhibit microtubule assembly and destabilize the cytoskeleton. CA4P is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 uM), inhibits tubulin assembly with IC50 of 2.4 uM. Fosbretabulin has orphan drug status in the EU and the US for the treatment of ATC (Anaplastic Thyroid Cancer). Later the development of this drug was discontinued.
Status:
Investigational
Source:
INN:bromofenofos
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Bromofenofos is an anthelminthic agent used in veterinary medicine to treat common liver fluke (Fasciola hepatica) infections in cattle and sheep.
Status:
Investigational
Source:
INN:perifosine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Perifosine is an orally active alkyl-phosphocholine compound with potential antineoplastic activity. Perifosine is an Akt inhibitor, which targets the pleckstrin homology domain of Akt, thereby preventing its translocation to the plasma membrane. Perifosine exerts Akt-dependent and Akt-independent effects, and although many preclinical studies have documented Akt inhibition by perifosine, clinical validation of these findings is lacking. Perifosine is in phase II and III clinical trials for the treatment of neuroblastoma, glioblastoma multiforme and other solid tumors.
Status:
Investigational
Source:
INN:fosopamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fosopamine (also known as Sim 2055), is a prodrug of epinine was studied for the treatment of renal failure and of essential hypertension. However, phase II of clinical trials in Italy was discontinued in 1995. Information about the current development of this drug is not available.
Status:
Investigational
Source:
JAN:ERITORAN SODIUM [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Eritoran (E-5564) is a synthetic lipid A analog that has been designed to antagonize the effects of lipopolysaccharide (LPS) and has been found to do this by interacting with Toll-like receptor 4, the cell surface receptor for LPS. Preclinical in vitro and in vivo studies of eritoran tetrasodium indicate it can limit excessive inflammatory mediator release associated with LPS and improve survival in sepsis models. Clinically, eritoran was being investigated for the treatment of severe sepsis, septic shock, and other endotoxin-mediated indications. Eritoran development has been discontinued.