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

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Showing 5541 - 5550 of 167129 results

Status:
Investigational
Source:
INN:mocimycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Mocimycin (also known as kyrromycin) was isolated from Streptomyces ramocissimus and tested in vitro against wide range of bacterias. Although having showed good results, drug did not enter clinical trials. Mocimycin acts by binding tightly and specifically to bacterial EF-Tu. Upon administration the antibiotic prevents EF-Tu-GDP from leaving the ribosome and thus inhibits bacterial protein synthesis. Nowadays, the antibiotic is mainly used to study bacterial protein synthesis at the level of elongation factor EF-Tu-GDP release.
Status:
Investigational
Source:
NCT01285414: Phase 2 Interventional Completed Glioblastoma Multiforme
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Veribulin is a novel microtubule destabilizer that both functions as a potent cytotoxin and acts as a vascular disrupting agent (VDA). It binds to the same (or nearby) sites on β-tubulin as colchicine. It is capable of evading multidrug resistance pumps and, thus, achieves high CNS concentrations. It is efficacious in multiple xenograft models without CNS toxicity. Veribulin had previously demonstrated pre-clinical and clinical activity in multiple tumor types. Veribulin is in phase II clinical trial for the treatment of Glioblastoma and Malignant melanoma.
Status:
Investigational
Source:
NCT00004937: Phase 2 Interventional Completed Brain and Central Nervous System Tumors
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Acridine carboxamide (XR5000) is a tricyclic acridine-based (or carboxamide-based) drug with dual topoisomerase inhibitor and potential antineoplastic activities. Acridine carboxamide inhibits both topoisomerases I and II and intercalates into DNA, resulting in DNA damage, the disruption of DNA repair and replication, the inhibition of RNA and protein synthesis, and cell death. Acridine carboxamide has been used in trials studying the treatment of lung cancer and brain and central nervous system tumors. In clinical trials acridine carboxamide did not show efficacy when tested against various types of cancers.
Status:
Investigational
Source:
NCT01951235: Phase 2 Interventional Completed Type 2 Diabetes Mellitus
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Imeglimin is the first in class tetrahydrotriazine‐containing oral glucose-lowering agent that has been studied in clinical trials as a possible monotherapy or add-on therapy to lower fasting plasma glucose. It is being developed as an alternative and a complement to drugs that act on insulin‐resistant organs or drugs acting on insulin secretion and β‐cell protection. When investigated in preclinical studies, Imeglimin showed that it can target insulin‐resistant organs by decreasing excessive hepatic glucose production and increasing muscle glucose uptake. It also showed a potential to restore appropriate glucose‐stimulated insulin secretion and protect β‐cells from cell death under high glucose conditions. Imeglimin acts on the liver, muscle, and the pancreas (6), three key organs involved in the pathophysiology of type 2 diabetes through suspected mechanisms targeting the mitochondria and reduced oxidative stress. Imeglimin decreases hepatic glucose production and increases muscle glucose uptake. Recently, Imeglimin demonstrated increased insulin secretion in response to glucose in diabetic patients during a hyperglycemic clamp study. In clinical trials, Imeglimin treatment for 7 days raised the insulin secretory response to glucose, improved β-cell glucose sensitivity and tended to decrease hepatic insulin extraction. Imeglimin did not affect glucagon secretion.
Status:
Investigational
Source:
INN:dimepranol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dimepranol is an immunomodulator and antiviral agent. As a mixture ingredient dimepranol was used for the treatment of recurrent local herpes simplex virus infections but results have been disappointing. As a component of inosine pranobex, dimepranol was licensed for the treatment of cell-mediated immune deficiencies associated with viral infections. In particular, for the management of: Mucocutaneous infections due to herpes simplex virus (type 1 and/or type 2); Genital warts as adjunctive therapy to podophyllin or carbon dioxide laser; Subacute sclerosing panencephalitis. Dimepranol in treatment regimens with antibiotics and inosin didn’t show any effect on PFAPA syndrome management.
Status:
Investigational
Source:
INN:timobesone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Timobesone is a topical corticosteroid and thiol ester derivative with anti-inflammatory activity.
Status:
Investigational
Source:
INN:tioperidone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tioperidone is tranquilizer. This antidepressant agent reverses P-glycoprotein-mediated multidrug resistance.
Status:
Investigational
Source:
NCT00363454: Phase 1 Interventional Completed Cancer
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.
Status:
Investigational
Source:
INN:cethexonium chloride
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Cethexonium is a cyclohexanols derivative with antimicrobial activities.
Status:
Investigational
Source:
INN:triflubazam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Triflubazam is a 1,5-benzodiazepine derivative. The hypnotic activity of the 1,5-benzodiazepines is limited, and that this is particularly so in the case of triflubazam. Subjects reported impaired sleep with triflubazam (40 mg), and a sense of less wakefulness the morning. The effect of triflubazam may have persisted beyond the night of ingestion. No effect of triflubazam was observed on total sleep time, stage shifts in the first 6 h or latency to the first rapid eye movement period of sleep. Triflubazam has psychopharmacological properties in animals suggestive of antianxiety activity of a longer duration than that of diazepam. The metabolism of triflubazam by man is characterized by extensive N-demethylation, aromatic hydroxylation, aromatic O-methylation and dihydrodiol formation.

Showing 5541 - 5550 of 167129 results