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

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Showing 8341 - 8350 of 8504 results

Dimebon (latrepirdine) is an orally available, small molecule, gamma carboline derivative that was developed and used in Russia as an over-the-counter oral antihistamine for allergy treatment since 1980s. In 1990s it was shown that Dimebon has promising potential in treating neurodegenerative diseases. In 2003, Medivation Inc acquired the rights to Dimebon. Medivation went public in December 2004, with Dimebon as the only drug in its pipeline. The product was being developed by Medivation and Pfizer as a treatment for early-stage Alzheimer's disease and Huntington's disease. However, development was discontinued by Medivation and Pfizer in early 2012. Dimebon inhibits alpha-Adrenergic receptors (alpha1A, alpha1B, alpha1D, and alpha2A), Histamine H1 and H2 receptors and Serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors with high affinity. Dimebon may act by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition.
Status:
Possibly Marketed Outside US
Source:
PARKINSAN by Byk-Gulden Lomberg Chemische Fabrik
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Budipine is an antiparkinsonian drug, which was developed by Byk Gulden (now Takeda) for the treatment of Parkinson's disease. The drug has multiple mechanisms of action: it was found to interfere with dopamine biosynthesis, mainly by inhibiting MAO-B enzyme and stimulating aromatic L-amino acid decarboxylase. Also the drug inhibits the dopamine re-uptake and has weak affinity to NMDA and muscarinic receptors. Budipine passes the blood-brain barrier, is metabolized by hydroxylation, and is excreted by both in urine and feces within 24 h.
Clobetasone is a corticosteroid used in dermatology, for treating such skin inflammation as seen in eczema, psoriasis and other forms of dermatitis, and ophthalmology. Topical clobetasone butyrate has shown minimal suppression of the Hypothalamic-pituitary-adrenal axis. It is available as clobetasone butyrate under the brand names Eumosone or Eumovate both manufactured by GlaxoSmithKline. Trimovate also contains Oxytetracycline, an antibiotic, and nystatin, an antifungal. Clobetasone butyrate is classed as a moderately potent topical corticosteroid. Clobetasone butyrate relieves the symptoms of a flare-up by reducing inflammation, itching and redness. It is not a cure for the condition, but it will help to relieve the symptoms. Although less potent topical steriods are often preferred for use in children, a short course of clobetasone butyrate may be prescribed for a child with severe eczema on the arms or legs. Short courses of clobetasone butyrate may also be prescribed for the treatment of psoriasis for areas such as the face, or the inside of elbows and behind the knees. In ophthalmology, clobetasone butyrate 0.1% eye drops have been shown to be safe and effective in the treatment of dry eyes in Sjögren's Syndrome.
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.
Status:
Possibly Marketed Outside US
Source:
Tanatril by Tanabe Seiyaku
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Imidapril (Tanatril), through its active metabolite imidaprilat, acts as an ACE inhibitor to suppress the conversion of angiotensin I to angiotensin II and thereby reduce total peripheral resistance and systemic blood pressure (BP). In clinical trials, oral imidapril was an effective antihypertensive agent in the treatment of mild to moderate essential hypertension. Some evidence suggests that imidapril also improves exercise capacity in patients with chronic heart failure (CHF) and reduces urinary albumin excretion rate in patients with type 1 diabetes mellitus. Imidapril was well tolerated, with a lower incidence of dry cough than enalapril or benazepril, and is a first choice ACE inhibitor for the treatment of mild to moderate essential hypertension.
Status:
Possibly Marketed Outside US
Source:
NCT01710488: Phase 4 Interventional Completed COPD Exacerbation
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Prulifloxacin is a prodrug of ulifloxacin which has been approved in Italy, Japan, China, India and Greece, for treatment of infections caused by susceptible bacteria, in the following conditions: acute uncomplicated lower urinary tract infections (simple cystitis); complicated lower urinary tract infections; acute exacerbation of chronic bronchitis; gastroenteritis, including infectious diarrheas. Like other fluoroquinolones, prulifloxacin prevents bacterial DNA replication, transcription, repair and recombination through inhibition of bacterial DNA gyrase.
Status:
Possibly Marketed Outside US
Source:
Japan:Exatecan Mesilate Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Exatecan (DX-8951f), a new hexacyclic camptothecin analogue, is a second-generation topoisomerase inhibitor that prevents rapidly dividing cells from replicating by interrupting DNA transcription, ultimately leading to cell death. Preclinical studies showed exatecan to have broad-spectrum antitumor efficacy. Exatecan is in phase III clinical trials for the treatment of pancreas cancer. However, there is no recent report of this research. The compound was co-developed by Daiichi Pharmaceutical (now Daiichi Sankyo) and Yakult Honsha.
Status:
Possibly Marketed Outside US
Source:
BIFEMELANE by Mitsubishi Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Bifemelane is a psychotropic drug, was found to inhibit monoamine oxidase (MAO). It inhibited type A MAO (MAO-A) competitively and type B (MAO-B) noncompetitively and it was a more potent inhibitor of MAO-A than of MAO-B. Bifemelane is an antidepressant and cerebral activator that is used in Japan for the treatment of cerebral infarction patients with depressive symptoms, and in the treatment of senile dementia as well. It also appears to be useful in the treatment of glaucoma.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Cediranib (AZD-2171) is a VEGFR-2 kinase inhibitor which was developed by AstraZeneca for the treatment of cancer. The drug reached the final stage of approval by European Medicines Agency in 2008 under the name Zemfirza (it was recommended to be taken in combination with platinum-based chemotherapy), however on 19 September 2016 AstraZeneca decided to withdraw the Marketing Authorisation Application.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Azimilide is a class III antiarrhythmic agent that prolongs cardiac repolarisation by blocking both the rapidly and slowly activating components of the delayed rectifier potassium channel. The most important consequence of this is apparent rate-independent activity, so that, unlike other class III antiarrhythmics, azimilide does not lose efficacy at high heart rates. Azimilide has very predictable pharmacokinetics, is predominantly hepatically metabolized, and has no significant drug interactions with digoxin or warfarin. The most common adverse effects reported by patients on azimilide were approximately equal in frequency with those on placebo: headache, asthenia, infection, diarrhea and dizziness. Azimilide is in phase III clinical trials for the treatment both supraventricular and ventricular tachyarrhythmias.

Showing 8341 - 8350 of 8504 results