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

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Showing 921 - 930 of 24423 results

Status:
Investigational
Source:
NCT00006363: Phase 3 Interventional Completed Adult Acute Basophilic Leukemia
(2000)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Valspodar (PSC-833) is a derivative of cyclosporin but devoid of the immunosuppressive and nephrotoxic properties seen in cyclosporin A. It exhibited high-affinity binding to Mdr1 P-glycoprotein (P-gp) and demonstrated multidrug resistance-reversing activity superior to cyclosporin A and verapamil both in vitro and in vivo. Preclinical and phase I/II clinical data have indicated that plasma levels of PSC-833 with multidrug resistance-reversing activities are achievable. Potent inhibition of intestinal, hepatobiliary and blood-brain barrier P-gp function has been demonstrated. The toxicity profiles of valspodar are acceptable and dose-limited by transient and reversible cerebellar ataxia. It has shown multidrug resistance-modulating activities towards acute myeloid leukemia, multiple myeloma and ovarian cancer in phase I/II clinical trials. However, the company discontinued development of valspodar in April 2001 following disappointing results reported from several multicentre phase III studies.
Status:
Investigational
Source:
NCT00709865: Phase 3 Interventional Completed Renal Insufficiency
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tonapofylline is a selective oral adenosine A, receptor antagonist, for the potential treatment of congestive heart failure. Oral tonapofylline over the dose range of 3 to 225 mg/day produced significant increases in sodium excretion in patients with stable heart failure without causing kaliuresis or reducing renal function. Tonapofylline may be useful in the clinical setting for the prevention of kidney failure induced by nephrotoxic agents such as cisplatin. Tonapofylline may be renoprotective in the setting of concomitant treatment with a loop-diuretic. Adverse effects were generally mild. Tonapofylline had been in phase III clinical trial for the treatment of acute heart failure. However, this development was discontinued.
Status:
Investigational
Source:
INN:indatraline [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Indatraline (Lu 19-005) is a non-selective monoamine transporter inhibitor that has been shown to block the reuptake of dopamine, norepinephrine, and serotonin with effects similar to those of cocaine. In vivo, indatraline produced behavioral effects suggestive of enhanced dopaminergic, noradrenergic, and serotonergic activity in mice. Indatraline also substituted for a high dose of cocaine in rats trained to discriminate between a low and a high dose of cocaine, which demonstrates that indatraline produces cocaine-like discriminative stimulus effects. Indatraline has been studied to block the action of methamphetamine and MDMA.
Status:
Investigational
Source:
INN:alazanine triclofenate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Alazanine triclofenate is a mixture of one molecule of 3-ethyl-2-(3-(3-ethyl-2-benzothiazolinylidene)propenyl)benzothiazolium 2,4,5-trichlorophenate and two molecules of 2,4,5-trichlorophenol. It is an antiparasitic agent. It is antimalarial drug, highly active against multiple Plasmodium falciparum isolates with IC50 value of 2.36E-07 M.
AE-37 (ANAVEX2-73, Tetrahydro-N, N-dimethyl-2, 2-diphenyl-3-furanemethanamine) is an orally available drug candidate developed to potentially modify Alzheimer’s disease rather than temporarily address its symptoms. It has a clean Phase 1 data profile and shows a reversal of memory loss (anti-amnesic properties) and neuroprotection in several models of Alzheimer’s disease. This drug is in Phase II trials for Alzheimer's disease, phase I trials for epilepsy, and in preclinical trials for amyotrophic lateral sclerosis, Parkinson's disease, Rett syndrome, stroke. AE-37 may function as a pro-drug for ANAVEX19-144 and acts as a muscarinic receptor and a moderate sigma1 receptor agonist.
Status:
Investigational
Source:
INN:ortetamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ortetamine, also known as 2-methylamphetamine, is a monoamine releaser that was studied as a stimulant drug. Information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:racemoramide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Racemoramide (also known as Moramide) is an opioid analgesic with a central structural action. In clinical trials, Racemoramide shows a strong analgesic action and low toxicity.
Status:
Investigational
Source:
INN:camonagrel
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Camonagrel is a novel selective thromboxane synthetase inhibitor patented by Ferrer Internacional S. A. Camonagrel reduced platelet-subendothelium interaction under flow conditions, showing this effect in a range of concentrations lower than in inhibition of platelet aggregation.
Status:
Investigational
Source:
JAN:NUCLOMEDONE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nuclomedone (TEI-3096), a thiazolopyrimidine compound has been shown to suppress adjuvant arthritis in rats without any effect on conventional inflammation. TEI-3096 also enhanced the delayed type hypersensitivity in mice and rats. These results suggests that TEI-3096 restores the abnormal immune response. Nuclomedone was discovered by Teijin and investigated as a potential treatment for rheumatoid arthritis and inflammatory disorders.
Status:
Investigational
Source:
INN:rofleponide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rofleponide is a third generation synthetic glucocorticosteroid. This compound has high affinity for the rat thymus glucocorticoid receptor and showed a very high biotransformation rate in the human liver. Rofleponide was being investigated for its anti-inflammatory, immunosuppressive and anti-anaphylactic activity. It was evaluated in phase II clinical trials for its safety and efficacy in allergic rhinitis and asthma, and in a preclinical study for use in inflammatory bowel disease, but development of this drug was discontinued. Rofleponide was never marketed.