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

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Showing 161 - 170 of 2696 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:rosaramicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rosamaricin is a macrolide antibiotic similar to erythromycin. This compound is more effective against Gram-negative bacteria than erythromycin, especially in the prostate where rosamaricin was shown to be more concentrated than erythromycin in dogs. Rosamaricin has antibiotic activity against Neisseria gonorrhoeae, Chlamydia trachomatis, Ureaplasma urealyticum and Mycoplasma hominis. When the drug was compared with penicillin G in the treatment of pneumococcal meningitis in rabbits it was found to be less effective than penicillin G, as measured by bacterial clearance from cerebrospinal fluid and by treatment outcome. No information on the current use of this compound is available.
Status:
Investigational
Source:
NCT01969357: Phase 2 Interventional Completed Type 2 Diabetes
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

SP-2086 H3PO4 (Retagliptin Phosphate), tetrahydro-imidazo[1,5-a] pyrazine derivative, is a competitive DPP-4 inhibitor innovated in China under development by Jiangsu Hengrui Medicine for the treatment of Type 2 diabetes. In completed phase II trials, retagliptin monotherapy or in combination with metformin significantly decreased the HbA1c level in type 2 diabetic patients. Two phase III trials for retagliptin monotherapy aCnd in combination with metformin, respectively, were ongoing in China. Jiangsu Hengrui Medicine withdrew its application from the Chinese FDA in April 2016 but is expected to refile the application.
Status:
Investigational
Source:
INN:butinoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Butinoline (also known as azulone) was used as an antispasmodic drug to treat gastritis.
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:enazadrem [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Enazadrem (CP-70490-09) is an antipsoriatic agent inhibiting arachidonate 5-lipoxygenase.
Status:
Investigational
Source:
INN:octriptyline
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Octriptyline was used as an antidepressant, however, it has never been marketed.