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Development Status

US Previously Marketed

3

Investigational

1

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Primary Target

Fumarate reductase flavoprotein subunit

3

Tubulin

3

glutathione metabolic process

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Highest Phase

Approved

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Approval Year

1967

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Unknown

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Condition

Cutaneous larva migrans

3

Strongyloidiasis

3

Trichinosis

3

Visceral larva migrans

3

Unknown

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Treatment Modality

Curative

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Originator

Albertz, A.

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Chemical

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CAS

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FDA UNII

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PUBCHEM

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ALANWOOD

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CHEBI

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ATC Level 1

ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS

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DERMATOLOGICALS

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ANTHELMINTICS

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ANTIFUNGALS FOR DERMATOLOGICAL USE

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ANTIFUNGALS FOR TOPICAL USE

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ANTINEMATODAL AGENTS

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ATC Level 4

Benzimidazole derivatives

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Imidazole and triazole derivatives

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Principal Form

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Salts, Hydrates, Esters, etc.

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Showing 1 - 4 of 4 results

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CHLOROTHALONIL

J718M71A7A

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

glutathione metabolic process

Conditions:

Chlorothalonil (2,4,5,6-tetrachloroisophthalonitrile) is an organic compound mainly used as a broad spectrum, nonsystemic fungicide, with other uses as a wood protectant, pesticide, acaricide, and to control mold, mildew, bacteria, algae. Chlorothalo...

nil reduces fungal intracellular glutathione molecules to alternate forms which cannot participate in essential enzymatic reactions, ultimately leading to cell death. Chlorothalonil is slightly toxic to mammals, but it can cause severe eye and skin irritation in certain formulations. Very high doses may cause a loss of muscle coordination, rapid breathing, nose bleeding, vomiting, and hyperactivity. Dermatitis, vaginal bleeding, bright yellow and/or bloody urine, and kidney tumors may also occur, followed by death. In a number of tests of varying lengths of time, rats which were fed a range of doses of chlorothalonil generally showed no effects on physical appearance, behavior, or survival. Kidney changes such as kidney enlargement were common. In the US, chlorothalonil is used predominantly on peanuts (about 34% of usage), potatoes (about 12%), and tomatoes (about 7%), though the EPA recognizes its use on many other crops. It is also used on golf courses and lawns (about 10%) and as a preservative additive in some paints (about 13%), resins, emulsions, and coatings. Chlorothalonil is commercially available in many different formulations and delivery methods. It is applied as a dust, dry or water-soluble grains, a wettable powder, a liquid spray, a fog, and a dip. It may be applied by hand, by ground sprayer, or by aircraft

THIABENDAZOLE

N1Q45E87DT

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Status:

US Previously Marketed

First approved in 1967

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Fumarate reductase flavoprotein subunit

Conditions:

Strongyloidiasis

Cutaneous larva migrans

Visceral larva migrans

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 eruptio...

n), 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.

THIABENDAZOLE HYDROCHLORIDE

N3B9AKC0T9

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Status:

US Previously Marketed

First approved in 1967

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Fumarate reductase flavoprotein subunit

Conditions:

Strongyloidiasis

Cutaneous larva migrans

Visceral larva migrans

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 eruptio...

n), 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.

THIABENDAZOLE PAMOATE

S5BM1I2UKT

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Status:

US Previously Marketed

First approved in 1967

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Fumarate reductase flavoprotein subunit

Conditions:

Strongyloidiasis

Cutaneous larva migrans

Visceral larva migrans

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 eruptio...

n), 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.

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