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

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Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Ethopabate is a veterinary drug used in the prophylaxis and treatment of coccidiosis in chickens. It is an arylamide containing one phenyl ring, belonging to monocyclic aromatics, is a very safe drug. It has anticoccidial activity especially against intestinal forms and lacks activity against E. tenella of caecal worms. This drug is a competitor of PABA for absorption by the parasite and interferes with folate synthesis. It has good activity against E. acervulina and some strains of E. maxima and E. brunette. It has been used only in combination with Amprolium first at 4 ppm and later at 40 ppm. This drug has peak activity on 4th day of cycle. Ethopabate is a component of marketed AMPROL PLUS (amprolium, ethopabate), indicated for use as an aid in the prevention of coccidiosis (1) in broiler chickens and (2) in replacement chickens where immunity to coccidiosis is not desired.
Suramin is an antiprotozoal and anthelmintic compound. It is indicated for the treatment of African trypanosomiasis (African sleeping sickness; trypanosome fever) and Onchocerciasis (river blindness). Additionally, suramin exhibits antineoplastic action. It was discovered that suramin produced dramatic, but transient, improvement of core symptoms of autism spectrum disorder.
Status:
Possibly Marketed Outside US
Source:
Phanquinone by Yick-Vic Chemicals and
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Phanquone is an orthoquinone that is the 5,6-diketo derivative of 4,7-phenanthroline. It derives from a hydride of a 4,7-phenanthroline. Phanquone (Entobex) is an anti-mycotic drug with anti-protozoal activity. Phanquone is active against a wide range of Gram-positive and Gram-negative organisms. Phanquone partically inhibited oxygen consumption by Escherichia coli and Staphylococcus aureus. It was also tried on cases of rheumatoid diseases.
Sulfamethazine is a sulfonamide used to treat a variety of bacterial diseases in animals. It inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase).
Status:
US Previously Marketed
First marketed in 1914

Class (Stereo):
CHEMICAL (ABSOLUTE)



Emetine is a principal alkaloid of ipecac, isolated from the ground roots of Uragoga ipecacuanha. Early use of emetine was in the form of oral administration of the extract of ipecac root, or ipecacuanha. This extract contains several, including cephaeline, and others. The identification of emetine as a more potent agent improved the treatment of amoebiasis. While the use of emetine still caused nausea, it was more effective than the crude extract of ipecac root. Additionally, emetine could be administered hypodermically which still produced nausea, but not to the degree experienced in oral administration. Emetine dihydrochloride hydrate is used in the laboratory to block protein synthesis in eukaryotic cells. It does this by binding to the 40S subunit of the ribosome. Emetine induces hypotension by blocking adrenoreceptors. Also, emetine was identified as a specific inhibitor of HIF-2α protein stability and transcriptional activity. Heavy or over usage of emetine can carry the risk of developing proximal myopathy and/or cardiomyopathy.
Status:
Possibly Marketed Outside US
Source:
Sacox by Kaken Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Salinomycin as a promising anticancer drug candidate exerts anti-angiogenic and anti-tumorigenic activities by inhibiting vascular endothelial growth factor receptor 2-mediated angiogenesis. Its salt, salinomycin sodium, is an ionophore anticoccidial for use in chickens to prevent coccidiosis caused by Eimeria tenella, E.necatrix, E.acervulina, E.maxima, E.brunetti and E.mivati.
Status:
First approved in 1990

Class (Stereo):
CHEMICAL (ACHIRAL)



Amprolium Hydrochloride is a broad spectrum, potent coccidiostat (anti-protozoal) used for the treatment and prevention of Coccidiosis in cattle, goats, sheep, and poultry (chicken and turkey) in veterinary. Amprolium probably acts by inhibiting thiamine uptake by parasites and thus creates disorders in the metabolism of parasites.
Maduramicin is antibiotic isolated from actinobacteria Actinomadura rubra. Maduramicin is used in veterinary as an aid in the prevention of coccidiosis in broiler chickens and turkeys. The compound is reported to be toxic to animals and humans if improperly used or by accident, resulting in heart failure, skeletal muscle degeneration, and even death. Studies have shown that toxicity is due to activation of protein phosphatase 2A, and the manipulation of the ROS-PTEN-Akt-Erk1/2 pathway may be a potential approach to prevent maduramicin -induced cardiotoxicity.
Status:
Possibly Marketed Outside US
Source:
NCT01661296: Phase 4 Interventional Completed Cutaneous Leishmaniasis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Stibogluconic acid (Sodium stibogluconate) is the pentavalent antimonial compound used to treat leishmaniasis and is only available for administration by injection. Sodium stibogluconate is sold in the UK as Pentostam (manufactured by GlaxoSmithKline). Sodium stibogluconate was granted orphan drug designation for the treatment of cutaneous leishmaniasis by the US FDA in January 2007. It is available in the United States only through the Centers for Disease Control. Sodium stibogluconate is indicated for the treatment of various types of a protozoal infection called leishmaniasis, which may result from sandfly bites in tropical and temperate parts of the world. It is also investigated for use/treatment in cancer. The mode of action of sodium stibogluconate is not clearly understood. In vitro exposure of amastigotes to 500 mg pentavalent antimony/ml results in a greater than 50% decrease in parasite DNA, RNA protein and purine nucleoside triphosphate levels. It has been postulated that the reduction in ATP (adenosine triphosphate) and GTP (guanosine triphosphate) synthesis contributes to decreased macromolecular synthesis. Sodium stibogluconate was shown to specifically inhibit type I DNA topoisomerase from Leishmania donovani through the inhibition of the unwinding and cleavage of the supercoiled plasmid pBR322, and to stabilize topoisomerase and DNA covalent complexes but not calf-thymus topoisomerase I and Escherichia coli DNA gyrase. Sodium stibogluconate is also a potent inhibitor of PTPases Src homology PTPase1 (SHP-1), SHP-2, and PTP1B but not the dual-specificity phosphatase mitogen-activated protein kinase phosphatase 1. Sodium stibogluconate combined with IFN-alpha-2b (IFN-α) inhibited solid tumor cell line growth in vitro, in vivo it was well tolerated and augmented cellular immune parameters.
Status:
Possibly Marketed Outside US
Source:
NCT00818818: Phase 4 Interventional Completed Localized Cutaneous Leishmaniasis
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Antimonic acid is an inorganic acid formed by antimony. As an ion-exchange material crystalline antimonic acid may be used for the regeneration of heteropolyacid catalysts. In addition, as a proton conductor, it may be used for gas sensing.