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

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Showing 12801 - 12810 of 13362 results

Status:
Possibly Marketed Outside US
Source:
SOFRAMYCIN by Waksman, S.A. et al.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Framycetin is a component of neomycin that is produced by Streptomyces fradiae. Framycetin is used for the treatment of bacterial eye infections such as conjunctivitis. Framycetin is an antibiotic. It is not active against fungi, viruses and most kinds of anaerobic bacteria. Framycetin works by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Framycetin is useful primarily in infections involving aerobic bacteria bacteria. Framycetin binds to specific 30S-subunit proteins and 16S rRNA, four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Framycetin is a component of SOFRACORT (Framycetin sulphate - Gramicidin-dexamethasone), indicated for the treatment of blepharitis and infected eczema of the eyelid; allergic, infective and rosacea conjunctivitis; rosacea keratitis; scleritis and episcleritis; iridocyclitis, and other inflammatory conditions of the anterior segment of the eye, as well as otitis externa (acute and chronic) and other inflammatory and sebhorrheic conditions of the external ear.
Status:
Possibly Marketed Outside US
Source:
Atrinositol sodium by Perstorp (Sweden)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Atrinositol antagonizes the effect of neuropeptide Y (NPY) in guinea pig basilar arteries. Atrinositol molecule derived from phytic acid. It seems to exert potent protective effects on some of the manifestations associated with diabetes in rats. Atrinositol inhibits glucose-stimulated insulin secretion by a direct effect on the pancreatic islets. Atrinositol appears to modulate fatty acid desaturases and aldose reductase in platelets and delay by a few weeks the development of cataract in this acute model of diabetes. It normalizes platelet aggregation in diabetic animals after long-term administration in vivo.
Status:
Possibly Marketed Outside US
Source:
NCT00756717: Phase 4 Interventional Completed Breast Cancer
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


MK-0752 is a potent, reversible inhibitor of γ-secretase, which inhibits γ-secretase to cleave substrates such as amyloid precursor protein. MK-0752 shows promising effects on inhibiting the growth of several types of cancer cells and was investigated in clinical trials for cancer treatment. For example in ovarian cancer models MK-0752 alone actively induced cell growth inhibition, G2/M phase cell cycle arrest and apoptosis with down-regulation of Notch1 and its downstream effectors in a dose- and time-dependent manner. Moreover, the sequential combination of cisplatin prior to MK-0752 significantly promoted cell apoptosis and inhibited the subcutaneous xenograft growth of ovarian cancer in nude mice. Through its effects on the Notch pathway, MK-0752 reduces the number of breast cancer stem cells in tumorgrafts, enhancing the efficacy of the chemotherapy drug docetaxel in mice with breast cancer tumors. Unfortunately, in phase II clinical trials MK-0752 failed to demonstrate efficacy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Atevirdine (U-87201E) is a nonnucleoside inhibitor of HIV-1 reverse transcriptase, that has been studied for the treatment of HIV infection. Atevirdine mesylate is the first-generation member of the bisheteroarylpiperazine class of nonnucleoside inhibitors, which inhibits reverse transcriptase noncompetitively by binding near the catalytic site. The safety, tolerability, and antiviral activity of atevirdine were studied in phase I/II clinical trial. Rash was the most common adverse event, with a grade 3 or 4 rash. No significant change from baseline in HIV-1 plasma RNA mean copy number was detected.
Status:
Possibly Marketed Outside US
Source:
Serotone by Mitsubishi Pharma
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Azasetron is an antiemetic drug. It acts as serotonin 3 receptor antagonist. It is currently used to prevent nausea and vomiting caused by cancer chemotherapy (including cisplatin chemotherapy). Also it was demonstrated that azasetron has potent antimitogenic and apoptotic effect on cancer cell line. It was preclinically tested to treat cocaine abuse.
Status:
Possibly Marketed Outside US
Source:
NCT01520285: Phase 4 Interventional Completed Hypertension
(2011)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Lercanidipine is antihypertensive drugs which acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. Lercanidipine exists as a racemate, with anti-hypertensive activity residing primarily in S-enantiomer. NDA for lercanidipine was submitted to FDA in 2002 by Forest Laboratories, but FDA refused to approve the drug, and lercanidipine is not marketed in USA. Lercanidipine is also investigated in preclinical models of epilepsy and ischemic stroke.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Stallimycin also known as distamycin A is an antibacterial and antitumor compound. It is able to bind to the minor groove of double-stranded B-DNA in a non intercalative manner, where it forms strong reversible complex preferentially at the nucleotide sequences consisting of 4-5 adjacent AT base pairs. The pyrrole-amide skeleton of distamycin A has been also used as DNA sequence selective vehicles for the delivery of alkylating functions to DNA targets, leading to a sharp increase of its cytotoxicity, in comparison to that, very weak, of distamycin itself.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Fenpiprane is a compound with antiallergic and antispasmodic activities. It is used in the treatment of functional gastrointestinal disorders.
Status:
Possibly Marketed Outside US
Source:
Ulcesium by Inpharzam [W. Germany]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fentonium is an anticholinergic, antispasmodic and anti-ulcerogenic agent. It is quaternary analog of hyoscyamine, is a blocker of muscarinic activity and an allosteric blocker of α12βγε nicotinic receptors. It increases the spontaneous release of acetylcholine at the motor endplate without depolarizing the muscle or inhibiting cholinesterase activity. Fentonium inhibited transmitter release and depressed twitch without changing the responsiveness to noradrenaline or ATP. It is a K(+)-channel opener. Administration of fentonium bromide in rats receiving naloxone after chronic morphine treatment reduced the intensity of withdrawal signs such as increased defecation or micturition, salivation and wet-dog shakes, and elevated the nociceptive threshold values.
Status:
Possibly Marketed Outside US
Source:
Propyromazine bromide by Astra (AstraZeneca)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Propyromazine bromide is a quatemary ammonium with muscarinic cholinoceptor antagonistic activity. This antimuscarinic agent with peripheral effects similar to those of atropine is given in the symptomatic treatment of visceral spasm.

Showing 12801 - 12810 of 13362 results