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

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Showing 1 - 10 of 16 results

Status:
Investigational
Source:
Cancer Treat Rep. Aug 1978;62(8):1173-6.: Phase 2 Human clinical trial Completed Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hycanthone is a thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. It was clinically available for the treatment of human schistosomiasis. Anti-helmintic action relies on its ability to inhibit worm monoamine oxidase and cholinesterases. Hycanthone produced immediate side effects such as hepatotoxicity and gastrointestinal disturbances, and was consequently withdrawn. Hycanthone inhibits apurinic endonuclease-1 (APE1) by direct protein binding. Hycanthone was used in the 1980s as antitumor agents, it was pulled out of Phase II trials.
Pravadoline is the anti-nociceptive agent, which has analgesic efficacy against postoperative pain in humans. Pravadoline inhibits the enzyme cyclooxygenase, but in contrast to cyclooxygenase-inhibiting NSAIDs does not produce gastrointestinal irritation. Pravadoline inhibited the synthesis of prostaglandins in mouse brain both in vitro and ex vivo. Pravadoline demonstrated only weak anti-inflammatory activity relative to its anti-nociceptive potency. Single doses of pravadoline were safe and effective in humans, without serious adverse events. Single oral administration of pravadoline maleate induced acute tubular necrosis in male and female beagle dogs.
Status:
Investigational
Source:
USAN:Amotriphene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Amotriphene (Myordil, WIN 5494) is a coronary dilator and cardiac antiarrhythmic properties. It has potential value in the treatment of angina-like conditions and the milder cardiac arrhythmias. Amotriphene binds to α‐adrenergic receptors.
Propylnorapomorphine is a potent and selective D2 receptor agonist. Propylnorapomorphine is used as a tool compound to label dopamine receptors in rodent brain, and elicits dopaminergic behavioural effects. It stimulates motor activity, induces stereotypic behaviour and sexual stimulation. Propylnorapomorphine was investigated in clinical trial against Parkinson's disease and schizophrenia
Status:
US Previously Marketed
Source:
Trancopal by Winthrop
(1958)
Source URL:
First approved in 1958
Source:
Trancopal by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Chlormezanone (TRANCOPAL®) is a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. It binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways. Chlormezanone (TRANCOPAL®) was discontinued worldwide in 1996 by Sanofi due to confirmed serious and rare cutaneous reactions (toxic epidermal necrolysis also known as Stevens-Johnson syndrome).
Status:
Possibly Marketed Outside US
Source:
NCT02385058: Phase 4 Interventional Completed Helminthiasis
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Quinafimide is an investigational compound that has been used in trials for the treatment of Amoebiasis and Helminthiasis. This phase 4 trial combined Quinfamide with the approved compound Mebendazole. The details of the mechanism of action are not known, but the overall effect is intraluminal immobilization of the Entamoeba.
Status:
Possibly Marketed Outside US
Source:
Zylofuramine by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Zylofuramine is a psychomotor stimulant. It intended for use as an appetite suppressant and for the treatment of senile dementia in the elderly, but there is little information about it and it does not appear to have ever been marketed.
Status:
Investigational
Source:
Cancer Treat Rep. Aug 1978;62(8):1173-6.: Phase 2 Human clinical trial Completed Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hycanthone is a thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. It was clinically available for the treatment of human schistosomiasis. Anti-helmintic action relies on its ability to inhibit worm monoamine oxidase and cholinesterases. Hycanthone produced immediate side effects such as hepatotoxicity and gastrointestinal disturbances, and was consequently withdrawn. Hycanthone inhibits apurinic endonuclease-1 (APE1) by direct protein binding. Hycanthone was used in the 1980s as antitumor agents, it was pulled out of Phase II trials.
Status:
Investigational
Source:
Cancer Treat Rep. Aug 1978;62(8):1173-6.: Phase 2 Human clinical trial Completed Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hycanthone is a thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. It was clinically available for the treatment of human schistosomiasis. Anti-helmintic action relies on its ability to inhibit worm monoamine oxidase and cholinesterases. Hycanthone produced immediate side effects such as hepatotoxicity and gastrointestinal disturbances, and was consequently withdrawn. Hycanthone inhibits apurinic endonuclease-1 (APE1) by direct protein binding. Hycanthone was used in the 1980s as antitumor agents, it was pulled out of Phase II trials.
Status:
Investigational
Source:
USAN:Amotriphene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Amotriphene (Myordil, WIN 5494) is a coronary dilator and cardiac antiarrhythmic properties. It has potential value in the treatment of angina-like conditions and the milder cardiac arrhythmias. Amotriphene binds to α‐adrenergic receptors.

Showing 1 - 10 of 16 results