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

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Showing 451 - 460 of 13240 results

Status:
Investigational
Source:
INN:daltroban
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Daltroban (also known as BM 13505, SKF 96148), a specific thromboxane A2 receptor antagonist, was studied as an antithrombotic agent. The drug was licensed to Smith Kline Beecham, underwent phase III clinical trials in the UK and Germany as an antithrombotic agent but did not enter clinical trials in the USA. Besides, вaltroban was investigated in patients with an ischemic heart disorder. However, the development of daltroban has been discontinued.
Status:
Investigational
Source:
NCT00664378: Phase 2 Interventional Terminated Relapsed and Refractory Multiple Myeloma
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



CYT997 (Lexibulin) is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. CYT997 (Lexibulin) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. CYT997 (Lexibulin) blocks the cell cycle at the G(2)-M boundary, and Western blot analysis indicates an increase in phosphorylated Bcl-2, along with increased expression of cyclin B1. Caspase-3 activation is also observed in cells treated with CYT997 (Lexibulin) along with the generation of poly(ADP-ribose) polymerase. The compound possesses favorable pharmacokinetic properties, is orally bioavailable, and is efficacious per os in a range of in vivo cancer models, including some refractory to paclitaxel treatment. CYT997 (Lexibulin) exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 (Lexibulin) possesses a useful combination of pharmacologic and pharmacokinetic properties having considerable potential as a novel anticancer agent. Lexibulin was being developed by YM BioSciences as a vascular-disrupting agent (VDA) for the potential treatment of cancer, it was in phase II development on YM BioSciences ' pipeline. It appears that the development of lexibulin has been discontinued.
Status:
Investigational
Source:
NCT02223481: Phase 2 Interventional Completed Hypertension, Pulmonary
(1998)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Terbogrel, an agent having two pharmacodynamic actions, namely inhibition of thromboxane A2 synthase and antagonism of the thromboxane A2 receptor. The antithrombotic effect of terbogrel was dose-dependent and was associated with enhanced prostacyclin production. The drug was studied for the treatment of peripheral vascular disorders, pulmonary hypertension, and thrombosis. Terbogrel participated in phase II clinical trial to investigate its safety and efficacy in patients with primary pulmonary hypertension, however, this study was discontinued due to terbogrel’s induction of leg pain.
Status:
Investigational
Source:
INN:denibulin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Denibulin is a novel antineoplastic agent. Denibulin selectively targets and reversibly binds to the colchicine-binding site on tubulin and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells, ultimately leading to cell cycle arrest, blockage of cell division and apoptosis. This causes inadequate blood flow to the tumor and eventually leads to a decrease in tumor cell proliferation. Denibulin hydrochloride had been in phase I clinical trials for the treatment of solid tumours. It was generally well tolerated and showed decrease in tumor vascular parameters. However, no recent development has been reported.
Status:
Investigational
Source:
INN:mespiperone (¹¹C) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mespiperone C-11 (3-N-[11C] methylspiperone) is a radiolabeled 3-N-methylspiperone. 3-N-methylspiperone is high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. It has been studied as a positron emission tomography (PET) tracer for imaging D2/3 and 5HT2A receptor densities.
Status:
Investigational
Source:
NCT00358488: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Milveterol (also known as GSK159797) was developed as a longer-acting beta2 adrenoceptor agonist for the treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). Milveterol completed phase II clinical trials for asthmatic subjects. However further development of the drug was discontinued.
Status:
Investigational
Source:
INN:fluazuron [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Fluazuron (N-[[4-chloro-3-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]oxyphenyl]carbamoyl]-2,6-difluorobenzamide, trade name Acatak) is an insect growth regulator belonging to the class of benzoyl phenyl urea derivatives, a class of chitin synthesis inhibitors. Fluazuron specifically interferes with chitin formation in ticks during engorgement, molt, and hatching. The substance is intended for tick control in beef cattle applied topically as a pour-on for use at single dose levels of 1.5 and 2.5 mg/kg BW with a possible additional treatment after 3 to 6 months.
Status:
Investigational
Source:
INN:fetoxilate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FETOXYLATE, a phenoxyethyl ester of diphenoxylate, is an opioid receptor agonist. It is used as antidiarrheal.
Status:
Investigational
Source:
INN:peliglitazar [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Peliglitazar (also known as BMS 426707-01), a dual α/γ peroxisome proliferator-activated receptor agonist, has been studied in phase I/II clinical trial in patients with type 2 diabetes mellitus. However, this study was discontinued.
Status:
Investigational
Source:
INN:modoflaner [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)