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

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Showing 281 - 290 of 8631 results

Status:
Investigational
Source:
INN:myralact [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Myralact is an antiseptic included in multi-ingredient preparations, e.g. vaginal tablets Ginetris, intended for the topical treatment of vaginal infections.
Status:
Investigational
Source:
INN:dioxadrol [INN]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Dioxadrol is the antidepressant agent. It was synthesized in 1966 and pharmacologically evaluated as a local anesthetic and general anesthetic drug. It was shown that dexoxadrol binds with high affinity toward NMDA receptor. Dioxadrol exists in four isomeric forms. alpha-(+)-Dioxadrol (dexoxadrol) showed phencyclidine (PCP)-like activity in rhesus monkeys trained to discriminate subcutaneous administration of ketamine, but neither alpha-(-)-dioxadrol (levoxadrol) nor beta-(+/-)-dioxadrol showed such activity. During clinical evaluation, it became obvious that non-tolerable side effects (retrograde amnesia, psychotomimetic effects) are associated with the application of dexoxadrol. These observations have led to termination of clinical development.
Status:
Investigational
Source:
INN:metkefamide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00081172: Phase 2 Interventional Completed Prostate Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lutetium is a silvery-white, hard, dense metal. Lutetium is little used outside research. One of its few commercial uses is as a catalyst for cracking hydrocarbons in oil refineries. Lutetium-177 radionuclide is used in radiopharmaceutical therapy. FDA approved Lutetium-177 dotatate for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs).
Status:
Investigational
Source:
INN:lupitidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lupitidine (SKF 93479) is a histamine H2 receptor antagonist. Lupitidine is a potent inhibitor of gastric acid secretion with a long duration of action. It lacks an antiandrogenic effect. It enhances pituitary thyroid stimulating hormone drive by increasing thyroid hormone clearance. It exerts an antinociceptive effect in rodents.
Status:
Investigational
Source:
INN:pirogliride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pirogliride is the antidiabetic agent. It has been found to produce a hypoglycemic effect in nondiabetic rats, dogs, mice, and monkeys. To being three to four times more potent than tolbutamide, pirogliride also differs from the sulfonylureas in lowering blood glucose concentrations of streptozotocin-diabetic rats and db/db mice, and, moreover, oral administration to normal fasted dogs did not produce the characteristic rise in insulin concentrations observed with tolbutamide. Pirogliride potentiates glucose-induced insulin secretion from isolated islets. This effect is accompanied by a facilitated glucose metabolism. Pirogliride partially prevents the known inhibitory effects of mannoheptulose on glucose-induced secretion and utilization. Pirogliride was found to produce a concentration-dependent inhibition of gluconeogenesis in rat kidney cortex slices. hepatocytes and perfused liver. Pirogliride was metabolized in man to a small extent by oxidation of the 4-position of the phenyl ring.
Status:
Investigational
Source:
NCT00001018: Phase 1 Interventional Completed Cryptosporidiosis
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Letrazuril is the p-fluoro analogue of diclazuril, a benzeneacetonitrile which is active against Eimeria spp., the causative agent of coccidiosis in poultry. Letrazuril is better absorbed and unlike diclazuril produces detectable plasma drug levels in humans following oral administration. In experimental studies on neonatal mice infected with Cryptosporidium parvum, oral administration of letrazuril for 4 days reduced stool oocyst counts by 95-98%, with complete clearing of oocysts from the stool in 47% of animals receiving the higher dose. Letrazuril has the potential to be an effective agent in the treatment of AIDS-related Cryptosporidiosis, without associated major toxicity. Severely immunocompromised AIDS patients with refractory cryptosporidiosis may show a modest, short-lived response to letrazuril. Letrazuril had been in phase I clinical trials for the treatment of cryptosporidiosis. However, this study was discontinued.
Status:
Investigational
Source:
INN:tesicam
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tesicam is a dioxoisoquinoline derivative patented by Pfizer, Chas. and Co., Inc. as an anti-inflammatory agent. In preclinical models, Tesicam shows potent anti-inflammatory activity against carrageenin-induced edema in rats.
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: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.