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

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Showing 411 - 420 of 13408 results

Status:
Investigational
Source:
INN:zaurategrast [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zaurategrast (CDP323) is an ethyl ester prodrug of CT7758, a potent carboxylic acid antagonist of integrin alpha4-beta1 (α4β1) or very late antigen 4 (VLA4). CDP323 was under development with UCB and Biogen Idec for the treatment of multiple sclerosis. Its development was discontinued in 2009 based on inadequate interim efficacy data in a phase II clinical trial.
Status:
Investigational
Source:
INN:tolamolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tolamolol is a phenoxypropranolamine derivative that preferentially inhibits myocardial beta adrenoreceptors, possesses beta blocking potency equivalent to propranolol, has little or no direct cell membrane effect and lacks beta adrenergic stimulating action. Cardioselective beta adrenergic blockade with tolamolol was highly effective in controlling ventricular rate in supraventricular arrhythmias and reduced the frequency of ventricular ectopic beats in half of the small group of patients with this arrhythmia. It is particularly applicable in patients with obstructive pulmonary disease in whom cardiac beta adrenergic blockade is indicated. Hypotension is an important potential side effect. Tolamolol and propranolol are equal in anti-anginal efficacy but tolamolol has the advantage of being cardioselective. It is superior to practolol. Tolamolol had no effect on sperm motility.
Status:
Investigational
Source:
INN:traxoprodil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Traxoprodil (CP-101,606) is a potent, selective N-Methyl-D-aspartate (NMDA) receptor (NR2B subunit) antagonist under development by Pfizer for its potential as a neuroprotectant in head injury and neurodegenerative disease. It is in phase II trials in the US and in phase I in Japan for the potential treatment of head injury, such as, Depressive Disorder, Major and Parkinson's Disease. CP-101,606 does not protect against glutamate-induced neurotoxicity in cultured cerebellar neurons, up to a dose of 10 uM. These results are consistent with CP-101,606 being a potent NMDA antagonist, selective for the type of NMDA receptor associated with the hippocampus. Some further investigation revealed that CP-101,606 was associated with a dose-related dissociation and amnesia. These results support the hypothesis that glutamate antagonists may be useful antidyskinetic agents. However, future studies will have to determine if the benefits of dyskinesia suppression can be achieved without adverse cognitive effects.
Status:
Investigational
Source:
INN:sunepitron [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Sunepitron (CP-93,393) is an anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. Sunepitron hydrochloride had been in Phase III clinical trials by Pfizer for the treatment of anxiety disorder and depression. However, this research has been discontinued.
Status:
Investigational
Source:
INN:sanfetrinem [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sanfetrinem cilexetil (formerly known as GV 118819), a beta-lactam antibiotic, is the oral prodrug of sanfetrinem. Experiments on rodents have revealed that sanfetrinem cilexetil had strong antibacterial activity in vitro and good pharmacokinetic behavior in mice. This drug was suitable for the treatment of infections caused by a variety of bacteria and participated in a phase II clinical trial. However, this study was discontinued.
Clogestone Acetate (AY-11440) is a steroidal progestin that was synthesized in 1964 and was investigated as a progestin-only contraceptive but was never marketed.
Status:
Investigational
Source:
INN:salmefamol
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Salmefamol is a beta2-adrenoceptor agonist that was studied in asthmatic patients. In clinical trials, the drug had shown marked efficacy with low toxicity and was generally well tolerated. However, information about the further development of salmefamol as a bronchodilator drug is not available.
Status:
Investigational
Source:
INN:metrifudil
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Metrifudil (previously known as Y-341) is a synthetic adenosine analog that is acid stable and has a prolonged duration of action. Metrifudil is a selective adenosine A2 receptor agonist and has anticonvulsant activity against seizures. The drug is also studied for the treatment of glomerulonephritis. However, no recent development has been reported.
Lisofylline [1-(5R-hydroxyhexyl)-3,7-dimethylxanthine] is a unique metabolite of pentoxifylline. Lisofylline inhibited the generation of phosphatidic acid and free fatty acids. Lisofylline blocked the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline regulates immune cell function and autoimmune response by inhibition of IL-12 signalling and cytokine production. Lisofylline may have therapeutic value in the prevention of autoimmune disorders, including Type 1 diabetes, autoimmune recurrence following islet transplantation, and in preservation of beta cell functional mass during islet isolation.
Status:
Investigational
Source:
INN:trestolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trestolone is a synthetic androgen that inhibits the release of follicle-stimulating hormone and impairs spermatogenesis. Luteinizing hormone is also suppressed, which cuts production of testosterone. The azoospermia and oligospermia are reversible after discontinuation of trestolone. Trestolone has androgenic and anabolic properties and loss of secondary sex characteristics is not seen. Like testosterone, trestolone undergoes enzymatic aromatization to an estrogen. The use of trestolone instead of testosterone for androgen replacement therapy could have health-promoting effects by reducing the occurrence of prostate disease. Trestolone had been in phase II clinical trial for the andropause control. However, this development was discontinued.