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

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Showing 21 - 30 of 78 results

Status:
US Previously Marketed
Source:
Formic Acid N.F.
(1921)
Source URL:
First marketed in 1921
Source:
Formic Acid N.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Formic acid is the simplest carboxylic acid. In nature, formic acid is found in the stings and bites of many insects of the order Hymenoptera, including bees and ants. The principal use of formic acid is as a preservative and antibacterial agent in livestock feed. When sprayed on fresh hay or other silage, it arrests certain decay processes and causes the feed to retain its nutritive value longer. In medicine 85% formic acid application is a safe, economical, and effective alternative in the treatment of common warts with few side-effects and good compliance.
Status:
Possibly Marketed Outside US
Source:
Imepitoin
Source URL:
First approved in 2022

Class (Stereo):
CHEMICAL (ACHIRAL)



Imepitoin (AWD 131–138 or ELB 138; 1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one) is a new anti-epileptic drug recently approved in the European Union for the treatment of canine idiopathic epilepsy. It was developed from a series of imidazolinones due to its pronounced ant seizure activity in a large variety of rodent models of epileptic seizures, combined with a high tolerability in these models. Imepitoin is a centrally acting antiepileptic substance, which crosses the blood brain barrier without involvement of active transport or active clearance, resulting in immediate equilibrium between plasma and brain. Imepitoin acts as low-affinity partial agonists at the benzodiazepine (BZD) site of the GABAA receptor. Hopefully, that the favorable profile of imepitoin for the treatment of epilepsy in dogs will reactivate the interest in partial BZD site agonists as new treatments for human epilepsy.
Afoxolaner (brand name NexGard) is a member of an isoxazoline class of compounds, which is used to kill adult fleas and is indicated for the treatment and prevention of flea infestations, and the treatment and control of Black-legged tick, American Dog tick, Lone Star tick, and Brown dog tick infestations in dogs and puppies. Afoxolaner is a member of the isoxazoline family, shown to bind at a binding site to inhibit insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), thereby blocking pre- and post-synaptic transfer of chloride ions across cell membranes. Afoxolaner blocks native and expressed insect GABA-gated chloride channels with nanomolar potency. Prolonged afoxolaner-induced hyperexcitation results in uncontrolled activity of the central nervous system and death of insects and acarines.
Sarolaner is a member of the isoxazoline class of parasiticides. It is sold under the brand name Simparica, indicated for the treatment of tick infestations (Dermacentor reticulatus, Ixodes hexagonus, Ixodes ricinus and Rhipicephalus sanguineus), as well as of flea infestations (Ctenocephalides felis and Ctenocephalides canis) in dogs. The primary target of action of sarolaner in insects and acarines is functional blockade of ligand-gated chloride channels (GABA-receptors and glutamate-receptors). Sarolaner blocks GABA- and glutamate-gated chloride channels in the central nervous system of insects and acarines. Disruption of these receptors by sarolaner prevents the uptake of chloride ions by GABA and glutamate gated ion channels, thus resulting in increased nerve stimulation and death of the target parasite. Sarolaner exhibits higher functional potency to block insect/acarine receptors compared to mammalian receptors.
Status:
Possibly Marketed Outside US
Source:
Bravecto by Nissan Chemical Industries
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Fluralaner, isoxazoline class compound, is a systemic insecticide and acaricide with antiparasitic activity against cat and dog fleas and ticks. Fluralaner is an inhibitor of the arthropod nervous system. Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and L-glutamate-gated chloride channels (GluCls). Potency of fluralaner is comparable to fipronil (a phenylpyrazole ectoparasiticide). The U.S. Food and Drug Administration (FDA) approved it under the trade name Bravecto for flea and tick treatment and prevention in dogs in May 2014. Bravecto kills adult fleas and is indicated for the treatment and prevention of flea infestations (Ctenocephalides felis) and the treatment and control of tick infestations [Ixodes scapularis (black-legged tick), Dermacentor variabilis (American dog tick), and Rhipicephalus sanguineus (brown dog tick)] in dogs and puppies 6 months of age and older. Bravecto is also indicated for the treatment and control of Amblyomma americanum (lone star tick) infestations in dogs and puppies 6 months of age and older.
Status:
Possibly Marketed Outside US
Source:
NCT03044652: Phase 4 Interventional Completed Vulvovaginal Atrophy
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Estriol (E3), also spelled oestriol, is a steroid, a weak agonist of the estrogen receptors ERα and ERβ., and a minor female sex hormone. According to in vitro study, the relative binding affinity (RBA) of estriol for the human ERα and ERβ was 11.3% and 17.6% of that estradiol, respectively, and the relative transactivational capacity of estrone at the ERα and ERβ was 10.6% and 16.6% of that of estradiol, respectively. Estriol is marketed widely in Europe and elsewhere throughout the world under the brand names Ovestin, Ortho-Gynest, and a variety of others. It is available in oral tablet, vaginal cream, and vaginal suppository form, and is used in menopausal hormone therapy for the treatment of menopausal symptoms. Estriol is also available in some countries as estriol succinate (brand name Synapause), a dosage-equivalent ester prodrug of estriol. Estriol and estriol succinate are not approved for use in the United States and Canada, although they have been produced and sold by compounding pharmacies in North America for use as a component of bioidentical hormone therapy. Estriol can be measured in maternal blood or urine and can be used as a marker of fetal health and well-being. If levels of unconjugated estriol (uE3 or free estriol) are abnormally low in a pregnant woman, this may indicate chromosomal or congenital anomalies like Down syndrome or Edward's syndrome. It is included as part of the triple test and quadruple test for antenatal screening for fetal anomalies.
Status:
Possibly Marketed Outside US
Source:
Veraflox by Bayer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pradofloxacin (trade name Veraflox) is a 3rd generation enhanced spectrum veterinary antibiotic of the fluoroquinolone class. It was developed by Bayer HealthCare AG, Animal Health GmbH, and received approval from the European Commission in April 2011 for prescription-only use in veterinary medicine for the treatment of bacterial infections in dogs and cats. The primary mode of action of fluoroquinolones involves interaction with enzymes essential for major DNA functions such as replication, transcription, and recombination. The primary targets for Pradofloxacin are the bacterial DNA gyrase and topoisomerase IV enzymes. Reversible association between Pradofloxacin and DNA gyrase or DNA topoisomerase IV in the target bacteria results in inhibition of these enzymes and rapid death of the bacterial cell. The rapidity and extent of bacterial killing are directly proportional to the drug concentration.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tildipirosin is a semisynthetic derivative of the naturally occurring 16-membered macrolide tylosin. Tildipirosin is intended for parenteral treatment of respiratory disease in cattle and swine. Tildipirosin will be administered as a single-dose injection: subcutaneously in cattle and intramuscularly in swine. The anticipated optimal clinical dose is 4 mg/kg bw. Tildipirosin is not used in human medicine. It is marketed under the brand name Zuprevo. As for other macrolides, the antimicrobial activity of tildipirosin is due to its binding to the ribosomal 50S subunit of bacterial cells thereby inhibiting bacterial protein synthesis. The in vitro antimicrobial activity against Gram-negative and Gram-positive pathogens indicates that tildipirosin is effective against a range of bacterial pathogens frequently associated with bovine and swine respiratory disease. Comparison of minimum inhibitory versus bactericidal concentrations shows that generally the antimicrobial action of tildipirosin is bacteriostatic.
Status:
Possibly Marketed Outside US
Source:
AIVLOSIN by Japan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tylvalosin tartrate is a third-generation macrolide antibiotic that has antibacterial activity against Gram-positive, some Gram-negative organisms and mycoplasma. Tylvalosin interferes with protein synthesis by reversibly binding to the 50S ribosome subunit. Tylvalosin binds to the donor site and prevents the translocation necessary for keeping the peptide chain growing. Its effect is essentially confined to rapidly dividing organisms. Tylvalosin tartrate is the active ingredient of Aivlosin -- a modern macrolide that has shown its effectiveness in the control of porcine proliferative enteropathy, EP and swine dysentery.