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

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Showing 791 - 800 of 13259 results

Status:
Investigational
Source:
NCT00747825: Phase 1 Interventional Terminated Metastatic Melanoma
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ioflubenzamide I-131 (also known as 131-I-MIP-1145) is a radiolabeled iodobenzamide derivative developed by Molecular Insight Pharmaceuticals, Inc for metastatic melanoma treatment. The benzamide moiety of Ioflubenzamide I-131 binds to melanin, selectively delivering a cytotoxic dose of gamma and beta radiation to melanin-expressing tumor cells. In human melanoma xenografts, Ioflubenzamide I-131 exhibited diffuse tissue distribution and washout from all tissues except melanin-expressing tumors. The administration of Ioflubenzamide I-131 at 25 MBq in single or multiple doses significantly reduced SK-MEL-3 tumor growth, with multiple doses resulting in tumor regression and durable response for over 125 days. Unfortunately Phase I clinical trial was terminated by unknown reason.
Status:
Investigational
Source:
INN:trefentanil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Trefentanil is a short-acting synthetic opioid of the piperidine class. The drug caused potent analgesia with the peak effect occurring 3 min after injection. There was no significant difference in analgesic potency of trefentanil and alfentanil as measured by tolerance to tibial pressure at 3 min. Trefentanil had a pharmacokinetic and pharmacodynamic profile similar to alfentanil, with a small extent of tissue distribution and a rapid blood/brain equilibration. Trefentanil caused significant respiratory depression at doses of 32 ug/kg and 64 ug/kg. It is a mu-opioid receptor agonist. Trefentanil produced naloxone reversible anti-nociception equi-efficacious to that of fentanyl.
Status:
Investigational
Source:
INN:levofenfluramine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LEVOFENFLURAMINE is a levorotatory enantiomer of fenfluramine, a substituted amphetamine which was formerly used to treat obesity. LEVOFENFLURAMINE has dopamine-antagonistic properties and, at high doses, increases dopamine concentrations in rat striatal dialysates. It is essentially inactive to reduce food intake in human subjects.
Status:
Investigational
Source:
INN:rocastine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Rocastine (AHR-11325) is a potent, nonsedating antihistamine with a rapid onset of action. This H1-antagonist effectively protected guinea pigs challenged with a lethal dose of histamine. It has also been mentioned in patents as a candidate to treat eye conditions and cough/cold mixtures (in which the lack of sedative effects from a non-sedating antihistamine would be especially useful in children, because daytime sedation is especially undesirable in this group). However, information on current use is not available and other second-generation, non-sedative antihistamines are available.
Status:
Investigational
Source:
INN:roflurane
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Roflurane (DA-893) is a fluorinated ether and general inhalation anesthetic. In humans, this compound shows less hypotensive effects than methoxyflurane. Roflurane was never marketed.
Status:
Investigational
Source:
INN:carbenzide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Carbenzide is hydrazine derivative with the high antidepressant activity and low toxicity patented by pharmaceutical company Warner-Lambert Pharmaceutical Co. Carbenzide acts via monoamine oxidase (MAO) inhibition and increase the level of brain serotonin.
Status:
Investigational
Source:
INN:pridefine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pridefine (AHR-1118) is a pyrrolidine derivative with clinically established antidepressant efficacy. Pridefine acted predominantly as a reuptake blocker of norepinephrine, dopamine, and 5-hydroxytryptamine, although some releasing activity was also present. Several clinical studies have demonstrated that pridefine is clinically as efficacious as imipramine and, perhaps more importantly, less toxic than standard antidepressants used.
Status:
Investigational
Source:
NCT04045327: Phase 3 Interventional Completed Hypovolemic Shock
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:bidisomide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Bidisomide (previously known as SC 40230) was developed as a sodium channel antagonist with class I antiarrhythmic properties. Bidisomide participated in clinical trials for patients with arrhythmia. However, the development was discontinued due to a lack of demonstrable efficacy.
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.