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

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Showing 51 - 60 of 462 results

Status:
US Approved OTC
Source:
21 CFR 333.120 first aid antibiotic:ointment oxytetracycline hydrochloride (combination only)
Source URL:
First approved in 1950
Source:
Terramycin HCl by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxytetracycline, a tetracycline analog isolated from the actinomycete streptomyces rimosus, was the second of the broad-spectrum tetracycline group of antibiotics to be discovered The drug is used for the prophylaxis and local treatment of superficial ocular infections due to oxytetracycline- and polymyxin-sensitive organisms for animal use only. These infections include the following: Ocular infections due to streptococci, rickettsiae E. coli, and A. aerogenes (such as conjunctivitis, keratitis, pinkeye, corneal ulcer, and blepharitis in dogs); ocular infections due to secondary bacterial complications associated with distemper in dogs; and ocular infections due to bacterial inflammatory conditions which may occur secondary to other diseases in dogs. Allergic reactions may occasionally occur. Treatment should be discontinued if reactions are severe. If new infections due to nonsensitive bacteria or fungi appear during therapy, appropriate measures should be taken. Oxytetracycline 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. Oxytetracycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane.
Status:
Investigational
Source:
INN:etanidazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etanidazole (also known as Radinyl) is a 2-nitroimidazole with radiosensitizing properties. Etanidazole exerts its therapeutic action by depleting glutathione and inhibiting glutathione S-transferase, thus enhancing the anticancer effects of radiation therapy. Etanidazole was tested in Phase III clinical trials in patients with advanced head and neck cancer, however, its development was stopped. A fluorinated etanidazole (EF5) may also be useful as an imaging agent for identification of hypoxic, drug-resistant regions of primary tumors and metastases.
Status:
Investigational
Source:
INN:levomoprolol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levomoprolol (L-moprolol) is a beta-adrenergic blocker which was introduced as an oral medication for treatment of systemic hypertension. It was found to be effective in 2% eyedrops in reducing the intraocular pressure in glaucoma. Observations on glaucoma patients treated with the eyedrop for 1.5 to 2.5 years was without undesirable side effects. L-moprolol and dipivefrin had an equivalent effect in lowering the intraocular pressure. The association of the two drugs caused a further reduction of intraocular pressure.
Status:
Investigational
Source:
JAN:MENOGARIL [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Menogaril is a semisynthetic derivative of the anthracycline antineoplastic antibiotic nogalamycin. Biochemical studies indicated that, in comparison to doxorubicin, menogaril is bound weakly to DNA, inhibits RNA synthesis less, and has different cell cycle phase-specific cytotoxicity. Menogaril acts as a cleavable complex-stabilizing topoisomerase II inhibitor. Menogaril has been studied in the treatment of various cancers.
Status:
Investigational
Source:
INN:guamecycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Guamecycline, a tetracycline derivative was studied in patients with broncho-pulmonary diseases and for the treatment of acute pneumopathies. However, information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:sancycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

There is a little information around sancycline. It is known, that it was synthesized by Conover and co-workers in 1962 and it was antibacterial compound. It was proposed that sancycline binds to the 30S of bacterial ribosomal subunit and inhibiting protein translation by blocking entry of aminoacyl-tRNA into the ribosome A site.
Status:
Investigational
Source:
INN:pepstatin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pepstatin is a pentapeptide of microbial origin. The peptide inhibits the acid proteases pepsin and cathepsin D and the pressor enzyme renin. Pepstatin was shown to provide long-lasting inhibition (3 to 6 days) of cathepsin D in vivo in non-tumor bearers particularly in spleen, liver, kidney, lung, and heart. Pepstatin may prove useful as "anticachexia" agent by decreasing proteolysis in muscle and other tissues. The in vivo pepstatin and IL-2 treatment decreased the T-cells and increased the natural killer-like LAK precursor cells, possibly also with an increase in its activity, which were further induced by in vitro IL-2 culture to generate an augmented LAK cell activity. This suggests the clinical potential of pepstatin in IL-2-related immunotherapy. In rats injected centrally with the specific cathepsin D inhibitor, pepstatin, the protease activity was inhibited up to 90% in most brain regions.
Status:
Investigational
Source:
INN:tigemonam
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.
Status:
Investigational
Source:
INN:soterenol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Soterenol [(+)-1-(3-methanesulphonamido, 4-hydroxyphenyl)-2-isopropylaminoethanol, MJ 1992] is a directly acting sympathomimetic amine which has been shown to display Beta2-adrenoceptor selectivity. Soterenol, a methanesulfonamido-phenethanolamine related structurally to isoproterenol, was a highly effective bronchodilator agent in several animal species by various routes of administration. The bronchodilator potency of soterenol was equivalent to, or greater than, that of isoproterenol. Soterenol also had potent stimulant action on the alpha-receptor of the smooth muscle.
Status:
Investigational
Source:
INN:carubicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Carubicin (also known as Carminomycin) is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. The drug is active against a variety of experimental tumors. Pharmacology studies in animals revealed that the drug bound largely to serum proteins and that it was widely distributed. In clinical trials The main toxic effect was myelosuppression but gastrointestinal intolerance and alopecia were also reported. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.