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

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Showing 21 - 30 of 60 results

Quinacrine was initially developed as an anti-malarial drug marketed under the name Atabrine. Also it was approved for the teratment of ascites, however it was wothdrawn for both indication in 1995 and 2003, respectively. The drug is also used for the treatment of giardiasis, lupus, rheumatoid arthritis, refractory pulmonary effusion and pneumothorax, induce female sterilization etc. Proposed mechanisms of action include DNA intercalation interference with RNA transcription and translation, inhibition of succinate oxidation interference with electron transport, inhibition of cholinesterase, and inhibitor of phospholipase.
Status:
Possibly Marketed Outside US
Source:
Hexamor by Aquarium Muenster Pahlsmeier GmbH
(2020)
Source URL:
First approved in 2020
Source:
Hexamor by Aquarium Muenster Pahlsmeier GmbH
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Melarsomine (melarsomine dihydrochloride) is an organic arsenical chemotherapeutic agent and is a trypanocidal antiparasitic drug. As of 2016 DIROBAN, a generic melarsomine dihydrochloride product, is the only FDA-approved treatment for adult heartworm (Dirofilaria immitis) infection in dogs. It is not approved for treatment in cats, or dogs in late-stage infection. It is marketed by Merial under the trade name Immiticide and is not currently available in the U.S. due to a manufacturing shortage. Sponsored by Anzac Animal Health, LLC and distributed by Zoetis, Inc., DIROBAN is a prescription animal drug supplied as a sterile powder that must be reconstituted with an accompanying sterile water diluent. The exact mode of action on D. immitis is unknown. Post-treatment mortality due to thromboembolism and/or progression of the underlying disease may occur in 10 to 20% of the Class 3 patients treated with DIROBAN.
Status:
Possibly Marketed Outside US
Source:
POULTRYSULFA Soluble Powder by Merck
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfaquinoxaline is a veterinary drug, which can be given to animals to treat coccidiosis and Acute Fowl cholera. It has often used in combinations with others drugs. It had its origins in the chemical synthetic program that sprang from the introduction of sulfonamide drugs into human medicine in the 1930s. The program was sustained through the years of World War II despite declining clinical use of that chemical class. Several sulfa drugs were known to be active against the sporozoan parasite (Plasmodium spp.) that causes malaria, but were not satisfactory in clinical practice. A sulfonamide that had a long plasma half-life would ipso facto be considered promising as an antimalarial drug. Sulfaquinoxaline, synthesized during the war, was such a compound. It proved too toxic to be used in human malaria, but was found to be a superior agent against another sporozoan parasite, Eimeria spp., the causative agent of coccidiosis in domestic chickens. In 1948 sulfaquinoxaline was introduced commercially as a poultry coccidiostat. The action mechanism of sulfaquinoxaline is to inhibit the dihydrofolate synthetase to encumber the nucleate synthesis of bacterium and coccidian its active peak to coccidian is at the second schizont stage (the fourth day of coccidial life cycle), so it will not affect the anti-coccidial immunity in chicken.
Ponazuril, sold by the Bayer Corporation under the trade name Marquis, was the first FDA-approved treatment for equine protozoal myeloencephalitis (EPM) in horse, caused by Sarcocystis neurona. Also this drug was used in animals such as cats, dogs against coccidia, an intestinal parasite. Coccidia treatment is far shorter than treatment for EPM.
Status:
Possibly Marketed Outside US
Source:
COBAN by Eli Lilly|Indiana University School of Medicine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Monensin is an antibiotic produced as a byproduct of fermentation by Streptomyces cinnamonensis and belongs to a family of drugs known as polyether antibiotics or ionophores. The drug was approved by FDA for the prevention of coccidiosis in turkeys, chickens, quail, cattle, goats, calves (Coban, Rumensin). The exact mechanism of monesin action is unknown, however there are several hypotesis, which includes the inhibition of K+ transport, the inhibition of the transport of carbohydrates across the host cell membrane, the interruption host cell invasion by sporozoites, etc.
Narasin is a polyether carboxylic ionophore agent that is authorised in Europe according to Commission Regulation No (EC) 1464/2004 as a coccidiostat for use in chickens for fattening with a maximum content of the active substance in feed of 70 mg/kg and a withdrawal period of one day. Narasin is the active ingredient in Monteban, a premix that is incorporated into chicken feed. Narasin is already approved for continuous oral use as Monteban (NADA 118-980) in chicken feed for the prevention of coccidiosis at doses up to 80 mg narasin/kg feed. Narasin is produced by the fermentation of a strain of Streptomyces aureofaciens.The biological activity of narasin is based on its ability to form lipid soluble and dynamically reversible complexes with cations, preferably monovalent cations such as alkaline K+, Na+ and Rb+: Narasin functions as a carrier of these ions, mediating an electrically neutral exchangediffusion type of ion transport across the membranes. The resultant changes in transmembrane ion gradients and electrical potentials produce critical effects on cellular function and metabolism of coccidia. Narasin is effective against sporozoites and early and late asexual stages of coccidia in broilers caused by Eimeria acervulina, E. brunetti, E. maxima, E. mivati, E. necatrix and E. tenella. Narasin also is used for prevention of necrotic enteritis in broiler chicken. Narasin was identified and characterized as a novel agent that inhibits DENV replication in vitro through non-cytotoxic mechanisms, thus indicating its potential to be further developed as a therapeutic anti-DENV agent.
Lasalocid is a polyether ionophore with potent antibacterial activity. Lasalocid was developed as an animal health product for treatment of coccidia. Lasalocid is able to form neutral complexes with monovalent and divalent cations and transport the ions through apolar phase (including lipid bilayer membranes). Interestingly, lasalocid can also transport larger organic cations, e.g. protonated dopamine. Lasalocid is used for the prevention of coccidiosis caused by Eimeria tenella, E. necatrix, E. acervulina, E. brunetti, E. mivati, and E. maxima, and for increased rate of weight gain and improved feed efficiency in broiler chickens. Also used for control of coccidiosis caused by Eimeria bovis and E. zuernii in cattle up to 800 lbs. and for prevention of coccidiosis caused by Eimeria ovina, E. crandallis, E. ovinoidalis (E. ninakohlyakimovae), E. parva and E. intricata in sheep maintained in confinement. Lasalocid has being shown to induce cytotoxic apoptosis and cytoprotective autophagy through reactive oxygen species in human prostate cancer PC-3 cells. Lasalocid should be useful in the search for new potential chemotherapeutic agents for understanding the molecular mechanisms of anticancer in prostate cancer cells.
Status:
Possibly Marketed Outside US
Source:
NCT02140073: Phase 4 Interventional Unknown status GERD
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Domperidone is a peripherally selective D2 receptor antagonist. It acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine. Domperidone was not approved in USA due to risks of cardiac arrhythmias, cardiac arrest, and sudden death, but is available in other countries. However, FDA allows access to Domperidone through an expanded access investigational new drug application (IND) to patients with gastroesophageal reflux disease with upper GI symptoms, gastroparesis, and chronic constipation. As an “off-label” use, domperidone is prescribed to breastfeeding women to enhance their milk production.
Status:
Possibly Marketed Outside US
Source:
Robenz by Kantor, S.|Kennett, R.L.Jr.|Waletzky, E.|Tomcufcik, A.S.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Robenidine (l,3-6ts (p-chlorobenzylidenamino) guanidine hydrochloride) is an effective anticoccidial, first introduced by Kantor, Kennett, Waletzky & Tomcufcik (1970). It does not affect the earliest stages in the coccidial life-cycle and its main activity is against the almost mature first generation schizont. It is used as an aid in the prevention of coccidiosis caused by Eimeria mivati, E. brunetti, E. tenella, E. acervulina, E. maxima and E. necatrix in broiler chickens.

Showing 21 - 30 of 60 results