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

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Showing 221 - 230 of 261 results

Status:
Investigational
Source:
INN:furodazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Furodazole, a benzimidazole derivative was studied as an anthelmintic drug. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:pretamazium iodide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pretamazium is thiazolium derivative patented by UK pharmaceutical company Wellcome Foundation Ltd. as antiphrastic compound, that active against parasitic nematodes.
Pafuramidine or DB289, [2,5-bis-(4-amidinophenyl)furan bis-O-methylamidoxime] is a pro-drug of DB75, [2,5-bis(4-amidinophenyl)furan] also known as furamidine. The biotransformation process of DB289 to DB75 in the human liver consists of three O-demethylation reactions catalyzed by the Cyp4F enzyme subfamily and three N-dehydroxylation reactions catalyzed by cytrochrome b5 and NADH-cytochrome b5 reductase. DB289 was studied for therapeutic treatment against human African trypanosomiasis, Pneumocystis pneumonia and malaria. In November 2006, Immtech Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) had granted orphan drug designation for pafuramidine (DB289) to treat Pneumocystis jiroveci pneumonia (PCP), a common life-threatening opportunistic infection in HIV/AIDS and other immunosuppressed patients. Despite the high efficacy of DB289 in patients, the mechanism of action of DB75 is unknown. The mechanism of antimicrobial activity of diamidine compounds is incompletely understood. They undergo active uptake by purine transporter systems in trypanosomes and their mechanism of action may involve interference with DNA-associated enzymes inhibition of heme crystallization11 or/and collapse of the transmitochondrial membrane potential.
Status:
Investigational
Source:
INN:piperamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Piperamide is substituted piperazine with a tertiary amine group. It was used as an anthelmintic agent. Initially, it was investigated because of its effectiveness against Trypanosoma. Piperamide distorts choroid plexus epithelial ultrastructure by engendering hydropic vacuoles.
Status:
Investigational
Source:
INN:carbantel
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Carbantel is imidoylurea derivative patented by pharmaceutical company Sterling Drug Inc. As anthelmintic agent.
Status:
Investigational
Source:
INN:becantone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Becanthone is an antischistosomal agent possesses the ability to inhibit tumors.
Status:
Investigational
Source:
INN:teroxalene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Teroxalene is a dioxopiperazine derivative with multidrug resistance reversal activity
Status:
Investigational
Source:
INN:stilbazium iodide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Stilbazium is a pyridinium derivative with considerable anthelminthic activity against some animal nematodes, including Syphacia obvelata, Ancylostoma caninum, Uncinaria stenocephala and Toxocara cati.
Levamisole (the trade name Ergamisol), an anthelminthic drug with immunological properties. It also has antitumor activity when administered with 5-fluorouracil in patients with Duke's C colorectal carcinoma; however, this use was discontinued. The mechanism of the antitumor effect is unknown but has been postulated to be related to levamisole's immunomodulatory properties. Levamisole can stimulate antibody formation to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis, chemotaxis and increases motility, adherence, and chemotaxis. Levamisole inhibits alkaline phosphatase and possesses cholinergic activity. The mechanism of action of levamisole as an antiparasitic agent, for example, to treat ascariasis, relates to its agonistic activity to L-subtype nicotinic acetylcholine receptors in nematode muscles. In addition, levamisole was studied for preventing relapses of the steroid-sensitive idiopathic nephrotic syndrome (SSINS). It was shown, that alone or in combination with steroids, the drug can prolong the time to relapse and prevented recurrence during one year of treatment. However, these studies also were also discontinued.
Status:
US Previously Marketed
Source:
Lucantbone HCl by Burroughs Wellcome
(1960)
Source URL:
First approved in 1960
Source:
Lucantbone HCl by Burroughs Wellcome
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Lucanthone is a thioxanthenone DNA intercalator. It inhibits topoisomerases and the dual function base excision repair enzyme apurinic endonuclease 1. Lucanthone has been devised for the treatment of schistosomiasis. It is also an antitumor agent. Lucanthone was being developed by Spectrum Pharmaceuticals for the treatment of malignant brain tumours.

Showing 221 - 230 of 261 results