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

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Showing 4041 - 4050 of 4227 results

Status:
Possibly Marketed Outside US
Source:
Japan:Etifelmine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Gilutensin is a drug that was developed for the treatment of hypotensive circulatory disorders. As there is no information available on the drug since 1970, its development is supposed to be terminated in early phase.
Bucindolol is a third-generation, non-selective β-adrenergic receptor blocker, that acts on both β-1 and β-2 receptors. Bucindolol’s additional α-1 antagonistic activity contributes to its mild vasodilator effect. It was rejected by the FDA for the heart failure, because of the unreviewed submissions deal with comparative effectiveness, clinical pharmacology, some aspects of pharmacogenetic data, and toxicology/metabolism. In addition, bucindolol is in the phase II of clinical trial for the treatment of atrial fibrillation.
Status:
Possibly Marketed Outside US
Source:
Japan:Menopafant
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Minopafant (E5880) is a novel platelet activating factor receptor antagonist. Minopafant had been in phase II clinical trials by Eisai in Japan for the treatment of disseminated intravascular coagulation. However, this research has been discontinued.
Vincamine is the major alkaloid of Vinca minor. Although vincamine has been used therapeutically for almost three decades, the exact mechanisms of action and its effects are still unknown. Vincamine is a peripheral vasodilator that increases blood flow to the brain. Vincamine is beneficial to the nervous system's cells feeding and protecting processes and is utilized as an adjuvant in case of cerebrovascular insufficiency, age-related psycho-behavioral disorders, post concussion syndrome in head trauma, in case of post-stroke sequels. Vincamine may be used as a dietary nootropic supplement.
Status:
Possibly Marketed Outside US
Source:
Japan:Tipepidine Citrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tipepidine (INN) also known as tipepidine hibenzate (JAN), is a synthetic, non-opioid antitussive and expectorant of the thiambutene class. The drug was discovered in the 1950s, and was developed in Japan in 1959. It is used as the hibenzate and citrate salts. The safety of tipepidine in children and adults has already been established. It is reported that tipepidine inhibits G-protein-coupled inwardly rectifying potassium (GIRK)-channel currents. The inhibition of GIRK channels by tipepidine is expected to modulate the level of monoamines in the brain. Tipepidine can improve attention deficit/hyperactivity disorder (ADHD) symptoms by modulating monoaminergic neurotransmission through the inhibition of GIRK channels. Tipepidine also is being investigated in depression, obsessive-compulsive disorder, and attention-deficit hyperactivity disorder (ADHD). As it acts on the central nervous system, overdose can cause altered mental status and other neurological symptoms; however, there have been few reports of tipepidine intoxication, including six cases in children and no cases in adults.
Status:
Possibly Marketed Outside US
Source:
NCT00180102: Phase 4 Interventional Completed Leukemia, Nonlymphocytic, Acute
(2003)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. Although its mechanism of action is incompletely defined, amsacrine inhibits DNA synthesis by binding to and intercalating with DNA. Amsacrine also inhibits topoisomerase II activity and may exert an effect on cell membranes. This agent also possesses immunosuppressive and antiviral properties. While amsacrine is not cell cycle phase-specific, cytotoxicity is maximal during the G2 and S phases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Cridanimod (Virexxa) is a small-molecule immunomodulator and interferon inducer, which, in preliminary studies, has been shown to increase progesterone receptor expression in endometrial tissue. Restoration of progesterone receptor expression may re-sensitize endometrial tumor tissue to progestin therapy in previously unresponsive tumors. Cridanimod was originally developed by Polysan and Pharmsynthez and licensed to Xenetic Biosciences. Virexxa is currently being studied in an ongoing Phase 2 multi-national study in conjunction with progestin therapy for the treatment of endometrial cancer in women with the recurrent or persistent disease who have failed progestin monotherapy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Alniditan is a non-indole migraine-abortive agent. It is a benzopyran derivative The action of sumatriptan is thought to be mediated by 5-hydroxytryptamine (5-HT)1D-type receptors. Alniditan did not attenuate substance P-induced inflammation, suggesting that the mediating receptors are located prejunctionally. In vitro alniditan exhibited less vasoconstrictive effects on the rat basilar artery than did sumatriptan, although at a very high concentration, alniditan caused intensive constriction, most likely through a mechanism independent from 5-HT receptor activation. Alniditan dose dependently attenuated the neurogenic inflammation and was more potent than sumatriptan. Adverse effects are: head pressure, paraesthesia, and hot flushes.
Status:
Possibly Marketed Outside US
Source:
CALSED by Sumitomo Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Amrubicin is a totally synthetic 9-aminoanthracycline anticancer drug, which is approved in Japan for the treatment of small cell and non-small cell lung cancer. Upon administration amrubicin is reduced to its C-13 hydroxy metabolite, amrubicinol. The cytotoxicity of amrubicinol in vitro is 10 to 100 times greater than that of amrubicin. Thus, the anticancer activity of amrubicin is considered to derive from this active metabolite. The mechanism of action of the drug is related to the inhibition of topoisomerase II by stabilizing the cleavable complex.
Status:
Possibly Marketed Outside US
Source:
Japan:Meprylcaine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Meprylcaine (also known as Epirocaine and Oracaine) is a local anesthetic with stimulant properties that is structurally related to dimethocaine. Meprylcaine has a relatively potent inhibitory action on the monoamine transporter and inhibits the reuptake of dopamine, norepinephrine and serotonin. Oracaine is commonly used as the hydrochloride salt and is compatible with the known vasoconstrictors. It has a slightly more rapid onset than procaine with a slight increase in potency. The earliest symptoms of a toxic overdose are stimulation to the central nervous system, thus following the same symptoms as procaine. Not more than 400 mg. (20 ml. of a 2 per cent solution) should be used at any one time for the ambulatory patient. Oracaine, like metycaine, may be used for patients sensitive to the para-aminobenzoic acid derivatives. Oracaine hydrochloride is used at present mainly by the dental profession and in dermatologic surgery.

Showing 4041 - 4050 of 4227 results