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

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Showing 161 - 170 of 462 results

Status:
Possibly Marketed Outside US
Source:
Apravet by Aventis Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Apramycin is a broad-spectrum aminocyclitol antibiotic produced by a strain of Streptomyces tenebrarius. It has a bactericidal action against many gram-negative bacteria. Apramycin is a structurally unique antibiotic that contains a bicyclic sugar moiety and a monosubstituted deoxystreptamine. It is not approved for use in humans. Apramycin is registered for use in more than twenty countries in cattle, pigs and chickens. The drug exerts its antibacterial effect by inhibiting protein synthesis at the level of peptidyl translocation. It is mostly used for treating gastrointestinal infections. Apramycin is available in soluble powder and feed premix formulations.
Status:
Possibly Marketed Outside US
Source:
Japan:Carumonam Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Carumonam is a monobactam antibacterial agent. It was highly active in vitro against members of the family Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae and weakly active against Streptococcus pneumoniae, but it was not active against Staphylococcus aureus. The excellent activity of carumonam against Gram-negative bacteria is related to its high affinity for their penicillin-binding proteins. It is indicated for the treatment of urinary tract infections, chronic respiratory infections, biliary tract infections, peritonitis, sepsis. Another factor that contributes to the excellent activity of carumonam against Gram-negative bacteria is its resistance to beta-lactamases. Adverse effects of the carumonam were limited to phlebitis at the intravenous infusion site; bloody diarrhea.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Clomocycline is the approved name of a methylol derivative of chlortetracycline. Clomocycline is a tetracycline antibiotic that is commonly prescribed by medical doctors for infections and to treat acne. It may also be used to treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia. Clomocycline is also used commonly as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria and is also prescribed for the treatment of Lyme disease. Clomocycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Clomocycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane. This drug has been reported to be noticeably free of side-effects such as nausea, vomiting, and diarrhea.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Moxestrol (11β-methoxy-17-ethynyl-estradiol) is estrogen receptor agonist. It is used in the studies of estrogen receptor activity and distribution. Moxestrol is rapidly metabolized by the liver. Hydroxylation was the main transformation pathway. Moxestrol yielded metabolites hydroxylated (or methoxylated) at C-2, C-15 and C-16, but not at C-6, and also gave rise to D-homo derivatives. It was considered as a potentially effective drug in the treatment of postmenopausal disturbances.
Status:
Possibly Marketed Outside US
Source:
Japan:Cetraxate Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cetraxate is an oral gastrointestinal medication, mucosal protectant. Cetraxate might indirectly stimulate capsaicin-sensitive afferent nerves and increase mucosal blood flow, and that this may be a key mechanism underlying its gastroprotective action. Cetraxate prevents gastric mucosal blood flow decrease in H. pylori-infected patients. It is usually used to improve gastric mucosal lesion in acute gastritis or acute exacerbation of chronic gastritis and to treat gastric ulcer. The most commonly reported adverse reactions include constipation, rash, nausea, vomiting, dry mouth and diarrhea.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Carbuterol is a beta-adrenergic bronchodilator with selectivity for bronchial smooth muscle relative to cardiac and vascular tissues of several species including man. In vitro studies demonstrated that carbuterol was a direct acting beta-adrenergic agonist, not dependent on endogenous catecholamine release, and was devoid of alpha-adrenergic agonist activity. The activity of the racemate was shown to reside primarily in the l-enantiomer. Carbuterol inhibited immunologically induced release of histamine and slow reacting substance of anaphylaxis from passively sensitized fragmented rhesus monkey lung and also inhibited passive cutaneous anaphylaxis in rats. Acute toxicity studies in mice, rats and guinea pigs indicated a wide safety margin for carbuterol. Carbuterol is a safer and more effective bronchodilator than ephedrine.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Cefpirome sulphate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefpirome is a semisynthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity. Cefpirome binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Cefpirome is an injectable extended-spectrum or 'fourth generation' cephalosporin. Its antibacterial activity encompasses many of the pathogens involved in hospital-acquired infections such as Enterobacteriaceae, methicillin-susceptible Staphylococcus aureus, coagulase-negative staphylococci and viridans group streptococci. Cefpirome also has in vitro activity against Streptococcus pneumoniae regardless of penicillin susceptibility. It is stable against most plasmid- and chromosome-mediated beta-lactamases, with the exception of the extended-spectrum plasmid-mediated SHV enzymes. Intravenous cefpirome 2g twice daily has shown clinical efficacy comparable to that of ceftazidime 2g 3 times daily in the treatment of hospitalised patients with moderate to severe infections. Clinical response and bacteriological eradication rates were similar in patients with severe pneumonia or septicaemia treated with either cefpirome or ceftazidime. Cefpirome appeared more effective than ceftazidime in the eradication of bacteria in patients with febrile neutropenia in 1 study; however, clinical response rates were similar in the 2 treatment groups. The tolerability of cefpirome appears similar to that of ceftazidime and other third generation cephalosporins, diarrhoea being the most frequently observed event. Thus, cefpirome is likely to be a valuable extended-spectrum agent for the treatment of severe infections. Cefpirome offers improved coverage against some Gram-positive pathogens and Enterobacteriaceae producing class I beta-lactamases compared with the third generation cephalosporins, although this has yet to be demonstrated in clinical trials.
Status:
Possibly Marketed Outside US
Source:
Japan:Dibekacin Sulfate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Dibekacin is a semisynthetic aminoglycoside antibiotic useful in the treatment of severe gram-negative bacterial infections. The drug is marketed in Japan.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Isoxicam is a nonsteroidal anti-inflammatory drug with long half-life. The major oxidative excretion product of isoxicam is the hydroxymethlyisoxazole metabolite, minor metabolites are open-ring sulfonamide and N-methylsaccharin. Isoxicam Is effective and well tolerated in all the major rheumatic diseases.
Status:
Possibly Marketed Outside US
Source:
Japan:Tosufloxacin Tosilate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tosufloxacin is a fluoroquinolone antibacterial agent. Tosufloxacin is an inhibitor of bacterial DNA gyrase and topoisomerase IV. Tosufloxacin is indicated for the treatment of various infections such as skin, respiratory, urinary, gynecologic, ophthalmologic, otolaryngologic, dental infections. Fluoroquinolones including tosufloxacin have a potential risk of inducing cartilage and joint toxicity in children. It is also associated with severe thrombocytopenia and nephritis, and hepatotoxicity.

Showing 161 - 170 of 462 results