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

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Showing 11641 - 11650 of 13268 results

Status:
Investigational
Source:
NCT00082368: Phase 2 Interventional Completed Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tariquidar, a non-competitive, specific P-glycoprotein (Pgp) inhibitor, is an anthranilamide derivative with multidrug resistance properties. Tariquidar binds to the ATP-binding cassette (ABC) transport protein Pgp, thereby inhibiting transmembrane transport of anticancer drugs resulting in their increased intracellular concentrations augmenting cytotoxicity of an anticancer drug. Tariquidar was discovered by Xenova Group and was developed for the treatment of multidrug resistance in cancer. In October 2002 the US Food and Drug Administration (FDA) has granted fast track review status to tariquidar for the treatment of multi-drug resistance in first-line treatment of non-small cell lung cancer (NSCLC) patients. Tariquidar is still undergoing research as an adjuvant against multidrug resistance in cancer.
Status:
Investigational
Source:
INN:trecetilide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trecetilide is a class III antiarrhythmic agent developed for the treatment of atrial flutter and fibrillation. Trecetilide probably has effects on the cardiac myocyte membrane that are similar to ibutilide. It is being developed for both oral and intravenous administration. Unlike ibutilide, trecetilide has good oral bioavailability. Trecetilide has a good metabolic stability. As with ibutilide, its mechanism of class III action may involve both rectifier K+ current blockade and other mechanisms of prolonging repolarization.
Status:
Investigational
Source:
INN:clamikalant
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



The novel compounds clamikalant (HMR 1883) or its sodium salt HMR 1098) have been shown to block selectively Kir6.2/SUR1-composed K(ATP) channels. Clamikalant is under development by Aventis Pharma (formerly Hoechst Marion Roussel) for the potential treatment of heart arrest and ventricular arrhythmias. Nevertheless, clamikalant and its sodium salt did not pass the clinical trials
Status:
Investigational
Source:
NCT00782535: Phase 2 Interventional Completed Chronic Obstructive Pulmonary Disease
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Carmoterol is a long-acting β2-adrenoceptor agonist with a rapid onset of action and potent bronchodilating activity. Carmoterol has a similar onset of action compared to salbutamol and formoterol, and a faster onset of action compared to salmeterol. Furthermore, the duration of tracheal smooth muscle relaxation is longer for carmoterol compared to both formoterol and salmeterol. In asthmatic patients, the PK of carmoterol is proportional to the dose, and nonlinear accumulation of the drug after repeated dosing treatments is negligible. In patients with persistent asthma carmoterol 2 µg administered once daily is as effective as formoterol 12 µg twice daily. Safety and tolerability results are similar between carmoterol and formoterol. There were no significant changes in ECG results, blood pressure or serum potassium or glucose levels
Status:
Investigational
Source:
NCT00479505: Phase 2 Interventional Completed Urinary Bladder, Overactive
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gisadenafil is a phosphodiesterase V inhibitor in clinical development at Pfizer. It had been in phase II clinical trials for the treatment of Benign prostatic hyperplasia; Chronic obstructive pulmonary disease; Erectile dysfunction; Overactive bladder. Treatment-emergent adverse events were: headache, myalgia, dyspepsia, back pain.
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:dotefonium bromide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dotefonium is the anticholinergic, spasmolytic agent.
Status:
Investigational
Source:
NCT00102973: Phase 3 Interventional Completed Ovarian Neoplasms
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Canfosfamide is a modified glutathione analogue and nitrogen mustard prodrug, with potential antineoplastic activity. Canfosfamide is selectively activated by glutathione S-transferase P1-1 an enzyme that is over-expressed in many human cancers including ovarian cancer. GST P1-1-mediated cleavage leads to an active cytotoxic phosphorodiamidate alkylating metabolite that forms covalent linkages with nucleophilic centers in tumor cell DNA, which may induce a cellular stress response and cytotoxicity, and decrease tumor cell proliferation. Preclinical studies showed that canfosfamide inhibited the growth and was cytotoxic to a wide range of established cancer cell lines including those derived from ovarian cancer (OVCAR3, HEY, SK-OV-3). Canfosfamide treatment inhibited cancer cell proliferation and induced apoptosis through the activation of the cellular stress response kinase pathway. The cytotoxic activity of canfosfamide correlated with the expression of GST P1-1. Cancer cells in which GST expression levels were increased by transfection with the GST P1-1 gene, were more sensitive to the cytotoxic effects of canfosfamide than the parental cell lines Canfosfamide in combination with pegylated liposomal doxorubicin is well tolerated and active in platinum and paclitaxel refractory or resistant ovarian cancer.
Status:
Investigational
Source:
NCT04020224: Not Applicable Interventional Withdrawn Safety Issues
(2024)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Amustaline (S-303) is a quinacrine mustard compound with potential antineoplastic activity. Amustaline binds to, intercalates and crosslinks DNA and RNA. This agent is mainly used for ex vivo purposes, specifically for the inactivation of pathogens such as viruses, protozoa and bacteria in red blood cells (RBCs). When S-303 is added to red blood cells, the compound rapidly passes through membranes, including those of cells and viral envelopes, due to its amphipathic character, and intercalates into helical regions of the nucleic acids of pathogens and white blood cells. TERCEPTTMBlood System usingamustaline (S-303) and glutathione (GSH) was able to inactivate high levels of DENV and ZIKV in RBCs. S-303 system has been shown to effectively inactivate a broad spectrum of pathogens, while maintaining RBC quality.
Status:
Investigational
Source:
INN:sepazonium chloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Sepazonium was studied as a topical anti-infective drug. However, information about the current use of this agent is not available.

Showing 11641 - 11650 of 13268 results