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

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Showing 911 - 920 of 13311 results

Status:
Investigational
Source:
NCT00048022: Phase 2 Interventional Completed Asthma
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Valategrast (R-411) is a dual-acting α4/β1 - α4/β7 integrin antagonist which underwent clinical development with Roche for the treatment of multiple sclerosis (MS) and asthma. Phase I and II studies have been conducted. It had shown good efficacy in animal disease models. Following oral administration, R-411 was rapidly and completely biotransformed into its active metabolite, RO-0270608, most of which was eliminated by biliary excretion. R-411 had shown acceptable pharmacokinetics and good safety in healthy volunteers. R-411 inhibited eosinophil and T H 2 cell excitation and survival, and inhibited eosinophil migration from blood to pulmonary tissues. The idea of combining R-411 with montelukast (leukotriene antagonist) in the pharmaceutical dosage forms, therefore, provided a therapeutic treatment that had the combined effect of reducing circulating eosinophil counts and reducing eosinophil egress into pulmonary tissues, thereby providing an early onset of bronchodilation as well as sustained anti-inflammatory effects. Valategrast had been in phase II clinical trials by Roche for the treatment of asthma and in phase I clinical trials for the treatment of multiple sclerosis (MS). However, the study had been discontinued. Development of Valategrast was discontinued for the treatment of asthma after clarification of the regulatory framework for that class of compounds.
Status:
Investigational
Source:
INN:talisomycin
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Talisomycin (former trivial name: tallysomycin A), a third generation bleomycin analog that was studied as an antitumor antibiotic. The drug cleaved DNA preferentially at G-C and G-T sequences and produced specific cleavages at G-A sequences. Talisomycin participated in phase II clinical trial for the treatment of cancer; however, the further development of the drug was discontinued.
Status:
Investigational
Source:
INN:pidolacetamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pidolacetamol is an analgesic and antipyretic agent.
Status:
Investigational
Source:
NCT00248404: Phase 1/Phase 2 Interventional Completed Tumors
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:ditekiren
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ditekiren is a relatively large renin inhibitor incorporating the hydroxyethylene isostere as well as both the P4 proline and P2’ isoleucine of angiotensinogen. Methylation of the P2-site histidine backbone nitrogen stabilizes the P2-P3 peptide bond towards degradation by chymotrypsin. Even though oral bioavailability was low, serum ditekiren levels were equivalent to 4–8 times the in vitro IC50 for renin inhibition for this peptide throughout the 2.5 h after oral administration that blood levels were monitored. In Na-depleted cynomolgus monkeys, oral dose elicited a hypotensive response that had not returned to baseline by 5 h. Ditekiren had been in phase II clinical trials for the treatment of heart failure and hypertension. However, these studies were discontinued.
Status:
Investigational
Source:
JAN:LOXIGLUMIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Loxiglumide is a potent, orally active, and selective CCK-A receptor antagonist which stimulates calorie intake and hunger feelings in humans. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying. Intravenous administration of loxiglumide antagonized the CCK-induced reduction of gastric emptying in rats, acceleration of intestinal transport in mice, increase in ileal motility in rabbits, gallbladder contraction in guinea pigs and acceleration of gallbladder emptying in mice.
Status:
Investigational
Source:
INN:lamifiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LAMIFIBAN is a potent and selective nonpeptide glycoprotein IIb/IIIa antagonist. It inhibits platelet aggregation and thrombus formation by preventing the binding of fibrinogen to platelets. It was in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes but showed no significant effects on clinical outcomes.
Status:
Investigational
Source:
INN:fandofloxacin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fandofloxacin is a difluoroquinolone derivative. This compound possesses an antibacterial spectrum comparable to those of rufloxacin and ciprofloxacin in vivo. Fandofloxacin showed a rapid and nearly complete absorption, and a long residence time in the body. Because it has been reported that the in vivo antibacterial activity of Fandofloxacin is comparable or superior to other quinolones, despite the fact that its in vitro activity is significantly lower than that of the other compounds, the pharmacokinetics of this antibiotic may be responsible, at least in part, for the enhanced in vivo antibacterial activity of Fandofloxacin. Fandofloxacin is an inhibitor of bacterial DNA gyrase. The toxicities and adverse effects of Fandofloxacin observed in various toxicology studies and clinical trials were less than those of commercially available drugs. It has been in phase II clinical trial for the treatment of Urinary tract infections. However, this research has been discontinued in 2008.
Status:
Investigational
Source:
NCT00162253: Phase 2 Interventional Terminated Psoriasis, Moderate to Severe
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT02466971: Phase 3 Interventional Active, not recruiting Advanced Vaginal Adenocarcinoma
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Triapine (3-aminopyridine-2-carboxaldehyde thiosemcirbazone, (3-AP; NTO-1151; OCX-0191) is a novel small molecule ribonucleotide reductase inhibitor that acts on the M2 (R2) subunit. Ribonucleotide reductase is an enzyme involved in the de novo synthesis of deoxyribonucleotides, which are critical for DNA replication and DNA repair. Triapine has been used in trials phase II studying the treatment of Lung Cancer, Kidney Cancer, Prostate Cancer Pancreatic Cancer, among others. Recently was published the article describing, that the triple combination triapine-cisplatin-paclitaxel was safe and provided a rational basis for a follow-up phase II trial to evaluate the efficacy and progression-free survival in women with metastatic or recurrent uterine cervix cancer.