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

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Showing 5731 - 5740 of 6013 results

Alatrofloxacin is a fluoroquinolone antibiotic developed as a mesylate salt and was sold under brand name Trovan, but was withdrawn from the U.S. market in 2001. Trovan was indicated for the treatment of patients initiating therapy in in-patient health care facilities (i.e., hospitals and long term nursing care facilities) with serious, life- or limb-threatening infections caused by susceptible strains of the designated microorganisms in the conditions listed below. Nosocomial pneumonia caused by Escherichia coli, Pseudomonas aeruginosa, Haemophilus influenzae, or Staphylococcus aureus. Community acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Klebsiella pneumoniae, Staphylococcus aureus. Complicated intra-abdominal infections, including post-surgical infections caused by Escherichia coli. Gynecologic and pelvic infections including endomyometritis, parametritis, septic abortion and post-partum infections caused by Escherichia coli, Bacteroides fragilis, viridans group streptococci, Enterococcus faecalis. Complicated skin and skin structure infections, including diabetic foot infections, caused by Staphylococcus aureus, Streptococcus agalactiae, Pseudomonas aeruginosa, Enterococcus faecalis, Escherichia coli, or Proteus mirabilis. After intravenous administration, alatrofloxacin is rapidly converted to trovafloxacin, which is responsible for therapeutic effect. Plasma concentrations of alatrofloxacin are below quantifiable levels within 5 to 10 minutes of completion of a 1 hour infusion.
Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.
Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.
Cefotiam is a third generation beta-lactam cephalosporin antibiotic. It has broad spectrum activity against Gram positive and Gram negative bacteria. It does not have activity against Pseudomonas aeruginosa. The bactericidal activity of cefotiam results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).
Niclosamide is an antihelminth used against tapeworm infections. It may act by the uncoupling of the electron transport chain to ATP synthase. The disturbance of this crucial metabolic pathway prevents creation of adenosine tri-phosphate (ATP), an essential molecule that supplies energy for metabolism. Niclosamide works by killing tapeworms on contact. Adult worms (but not ova) are rapidly killed, presumably due to uncoupling of oxidative phosphorylation or stimulation of ATPase activity. The killed worms are then passed in the stool or sometimes destroyed in the intestine. Niclosamide may work as a molluscicide by binding to and damaging DNA. Niclosamide is used for the treatment of tapeworm and intestinal fluke infections: Taenia saginata (Beef Tapeworm), Taenia solium (Pork Tapeworm), Diphyllobothrium latum (Fish Tapeworm), Fasciolopsis buski (large intestinal fluke). Niclosamide is also used as a molluscicide in the control of schistosomiasis. Niclosamide was marketed under the trade name Niclocide, now discontinued.
Status:
US Previously Marketed
First approved in 1981

Class (Stereo):
CHEMICAL (ABSOLUTE)


Iodoxamic acid (previously sold under the brand name Cholovue) is an organoiodine compound that was used as a contrast medium. It is intravenous cholecystocholangiographic agent. It features both a high iodine content as well as several hydrophilic groups.
Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage. Also, due to the drugs estrogen component, it can bind more selectively to active estrogen receptors. Used for the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate.
Status:
US Previously Marketed
First approved in 1977

Class (Stereo):
CHEMICAL (ACHIRAL)



Etidronate is a salt of etidronic acid (brand name Didronel, also known as EHDP) a diphosphonate, which is indicated for the treatment of symptomatic Paget’s disease of bone and in the prevention and treatment of heterotopic ossification following total hip replacement or due to spinal cord injury. Didronel is not approved for the treatment of osteoporosis. This drugs acts primarily on bone. It can inhibit the formation, growth, and dissolution of hydroxyapatite crystals and their amorphous precursors by chemisorption to calcium phosphate surfaces. Inhibition of crystal resorption occurs at lower doses than are required to inhibit crystal growth. Both effects increase as the dose increases. Preclinical studies indicate etidronate disodium does not cross the blood-brain barrier. Didronel is not metabolized. The amount of drug absorbed after an oral dose is approximately 3 percent. Bisphosphonates, when attached to bone tissue, are absorbed by osteoclasts, the bone cells that breaks down bone tissue. Although the mechanism of action of non-nitrogenous bisphosphonates has not been fully elucidated, available data suggest that they bind strongly to hydroxyapatite crystals in the bone matrix, preferentially at the sites of increased bone turnover and inhibit the formation and dissolution of the crystals. Other actions may include direct inhibition of mature osteoclast function, promotion of osteoclast apoptosis, and interference with osteoblast-mediated osteoclast activation. Etidronic acid may promote osteoclast apoptosis by competing with adenosine triphosphate (ATP) in the cellular energy metabolism. The osteoclast initiates apoptosis and dies, leading to an overall decrease in the breakdown of bone.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control isoleucine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Isoleucine is an essential α-amino acid that is used in the biosynthesis of proteins. L-isoleucine is commonly used in parenteral and enteral nutrition. It is used in combination with the other branched chain amino acids to improve the nutritional status of patients with hepatic diseases. BCAAs serve as important fuel sources for skeletal muscle during periods of metabolic stress
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(22)(ii) antifungal:diaper rash benzoxiquine
Source URL:
First approved in 1964
Source:
UDDER BALM by H. W. Naylor Company Inc.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

In cosmetics and personal care products, Benzoxiquine has been reported to be used in the formulation of hair tonics, dressings, and other hair grooming aids. Benzoxiquine is described as a biocide for use in cosmetic products. It is currently reported to be used in only one product. In a separate finding, the Food and Drug Administration determined that Benzoxiquine is not generally recognized as safe and effective in over-the-counter topical antifungal drug products. The only data available on the toxicity of Benzoxiquine indicates that it is mutagenic in the Ames test without metabolic activation. Because of the lack of data, the safety of Benzoxiquine could not be substantiated. The data needed to make a safety assessment include purity/impurities, ultraviolet absorption (if there is absorption, then photosensitization data will be needed), 28-day dermal toxicity, dermal teratogenicity, ocular irritation (if already available only), dermal irritation and sensitization, and two different genotoxicity studies (one using a mammalian system). If the latter data are positive, dermal carcinogenesis data using the methods of the National Toxicology Program will be needed. It cannot be concluded that Benzoxiquine is safe for use in cosmetic products until these safety data have been obtained and evaluated.

Showing 5731 - 5740 of 6013 results