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

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Showing 101 - 110 of 261 results

Status:
US Previously Marketed
Source:
Alcopara by Burroughs Wellcome
(1967)
Source URL:
First approved in 1967
Source:
Alcopara by Burroughs Wellcome
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


BEPHENIUM HYDROXYNAPHTHOATE is an anthelmintic agent used in the treatment of hookworm and roundworm infections (Ancylostoma duodenale, Ascaris lumbricoides, and Necatore americanus). It targets the AChRs of nematodes producing spastic paralysis of the worms.
Thiabendazole (TBZ, trade names Mintezol, Tresaderm, and Arbotect) was first introduced in 1962. This drug is a fungicide and parasiticide and is indicated for the treatment of: strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, trichinosis: relief of symptoms and fever and a reduction of eosinophilia have followed the use of this drug during the invasion stage of the disease. But usage of this drug was discontinued. The precise mode of action of thiabendazole on the parasite is unknown, but it may inhibit the helminthspecific enzyme fumarate reductase. It was shown, also that thiabendazole reversibly disassembles newly established blood vessels, marking it as vascular disrupting agent (VDA) and thus as a potential complementary therapeutic for use in combination with current anti-angiogenic therapies. Was shown, that vascular disruption by TBZ results from reduced tubulin levels and hyper-active Rho signaling. In addition, was confirmed, that thiabendazole slowed tumor growth and decreased vascular density in preclinical fibrosarcoma xenografts and thus, it could lead directly to the identification of a potential new therapeutic application for an inexpensive drug that is already approved for clinical use in humans.
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.
Status:
US Previously Marketed
First approved in 1958
Source:
Delvex by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dithiazanine, 3-ethyl-2-[5-(3-ethyl-2-benzothiazolinylidene)-l, 3- pentadienyl] benzothiazolium iodide, is an old effective broad-spectrum human anthelmintic. In proper dosage, this polyvermicide is therapeutic for trichuriasis, strongyloidiasis, ascariasis, and enterobiasis. The drug also has significant anthelmintic activity against human hookworm, Necator americanus. It fulfills a need for an effective therapeutic for trichuriasis and strongyloidiasis. Dithiazanine is useful for the treatment of patients with either single or multiple intestinal helminth infections. It is effective for mass therapy for trichuriasis. Nowdays Dithiazanine is used only as a veterinary anthelmintic for dogs. It has being proved to be a highly toxic chemical, with a lethal dose for humans of about 4–16 mg/kg by oral ingestion.
Status:
US Previously Marketed
Source:
Mantomide by Winthrop
(1955)
Source URL:
First approved in 1955
Source:
Mantomide by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Chlorbetamide is dichlorobenzene derivative with antimicrobial and amebicidal activity.
Status:
US Previously Marketed
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)


Diethylcarbamazine is used in humans, dogs and cats for the treatment of parasitic infections, including pulmonary eosinophilia, loiasis, and lymphatic filariasis. The exact mechanism of its action is unknown, however some studies showed the involvment of inducible nitric-oxide synthase and the cyclooxygenase pathway. Although there is no information on whether the drug is marketed in the USA and Europe, it is currently used in India.
Status:
US Previously Marketed
Source:
CAMOPRIM CT AMODIAQUINE by PD
(1961)
Source URL:
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Amodiaquine is a medication used to treat malaria, including Plasmodium falciparum malaria when uncomplicated. The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function. The side effects of amodiaquine are generally minor to moderate and are similar to those of chloroquine. Rarely liver problems or low blood cell levels may occur. When taken in excess headaches, trouble seeing, seizures, and cardiac arrest may occur. After oral administration amodiaquine hydrochloride is rapidly absorbed,and undergoes rapid and extensive metabolism to desethylamodiaquine which concentrates in red blood cells. It is likely that desethylamodiaquine, not amodiaquine, is responsible for most of the observed antimalarial activity, and that the toxic effects of amodiaquine after oral administration may in part be due to desethylamodiaquine.
Status:
US Previously Marketed
Source:
Carbarsone by Lilly
(1944)
Source URL:
First approved in 1944
Source:
Carbarsone by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Carbarsone is an antiambeic, antihistomonal drug effective in controlling and preventing blackhead disease in turkeys (a disease caused by a protozoan parasite Histomonas meleagridis). Carbarsone was approved by FDA, however, it has not been marketed in the USA scince 1996.
Status:
US Previously Marketed
Source:
Plasmoquine
(1926)
Source URL:
First marketed in 1926
Source:
Plasmoquine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

The discovery of pamaquine, developed by replacing one of the methyl groups of methylene blue by a dialkylaminoalkyl chain, was a landmark in the design of drugs for malaria. It is closely related to primaquine. The administration of pamaquine during the incubation period delayed but did not prevent primary attacks of a New Guinea strain of Plasmodium vivax malaria. Hemolytic anemia after administration of the antimalarial drug pamaquine was reported in patients with Glucose-6-phosphate dehydrogenase (G6PD) deficiency. Pamaquine itself could not be used clinically due to high toxicity.
Status:
US Previously Marketed
Source:
Cinchonine Sulphate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Cinchonine Sulphate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cinchonine is cinchona bark alkaloid, which was used to treat malaria. Cinchonine is more efficient than quinine in increasing the intracellular accumulation and restoring the cytotoxicity of doxorubicin, mitoxantrone and vincristine on well-characterized multidrug resistance (MDR) cell lines. In the phase I of clinical trial was investigated the properties of cinchonine combined with the CHVP (cyclophosphamide, doxorubicin, vinblastine, methylprednisolone) regimen in relapsed and refractory lymphoproliferative syndromes.

Showing 101 - 110 of 261 results