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Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pilsicainide is marketed in Japan as (Sunrythm). Pilsicainide controls the cardiac conduction abnormalities and improves the symptoms of arrhythmia with the blocking action on Na channel. It is usually used to treat tachycardiac arrhythmia. Pilsicainide did not affect the resting membrane potential. Under the voltage-clamp condition, pilsicainide inhibited the transient outward current (Ito) that is more prominent in the atrium than in the ventricle in a concentration-dependent manner. However, in contrast to other class Ic agents, the inhibition to Ito by pilsicainide was observed only at much higher concentrations (IC50-300 uM) and did not affect the inactivation time-course of Ito. Moreover, the drug (10 uM) did not significantly affect the Ca2+, delayed rectifier K+, inward rectifying K+, acetylcholine-induced K+ or ATP-sensitive K+ currents. From these results pilsicainide could be differentiated as a pure Na+ channel blocker from other class Ic agents with diverse effects on membrane currents and should be recognized accordingly in clinical situations. A single oral dose of pilsicainide effectively restores normal sinus rhythm in patients with recent-onset atrial fibrillation and a healthy left ventricle. Long-term therapy with pilsicainide is successful in treating chronic atrial fibrillation
Status:
Possibly Marketed Outside US
Source:
Tiacob by Sanofi-Synthelabo
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. It is used to treat a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. A derivative of benzamide, tiapride is chemically and functionally similar to other benzamide antipsychotics such as sulpiride and amisulpride known for their dopamine antagonist effects. Tiapride is marketed under various trade names and is widely available outside of the United States. The most common trade name for tiapride is Tiapridal, which is used throughout Europe, Russia, as well as parts of South America, the Middle East, and North Africa. It is also sold under different names in Italy (Italprid, Sereprile), Japan (Tialaread, Tiaryl, Tiaprim, Tiaprizal), Chile (Sereprid), Germany (Tiaprid, Tiapridex), and China (Tiapride).
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Manganese gluconate is a manganese salt of gluconic acid. Manganese gluconate is sometimes used as a food additive for its texture and light pink coloring. As a food additive, manganese gluconate increases satiety, and the texture of processed foods related to mouth feel. However, in recent years, manganese gluconate has been used less and less as a food additive due to its high toxicity. Many food manufacturers have abandoned using manganese gluconate in favor of other chemical compounds that provide similar effects with a lower toxicity. According to the Food and Drug Administration, manganese gluconate is generally recognized as safe, or GRAS. However, high amounts of manganese gluconate intake, upwards of 15 mg per day, may cause potentially serious health risks. Manganese gluconate toxicity may cause a chemical imbalance in the brain, increasing your risk of developing anxiety, depression, nervousness, psychosis, and mania. Manganese gluconate is used for prevention of deficiency and osteoporosis (off-label).
Status:
Possibly Marketed Outside US
Source:
SEVISTA by Central Drug Research Institute
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levormeloxifene (INN) is an experimental selective estrogen receptor modulator (SERM) that was being developed as an alternative to estrogen replacement therapy for the treatment and prevention of postmenopausal bone loss. Levormeloxifene is the levorotatory enantiomer of non-hormonal, non-steroidal oral contraceptive -- ormeloxifene (trade names Novex-DS, Centron, and Sevista). The development of Levormeloxifene was stopped because of a high incidence of gynecologic adverse events during clinical trials.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Tropatepine is an anticholinergic drug. Intramuscular injections of tropatepine are used to counteract the extrapyramidal effects of neuroleptic drugs and for the treatment of Parkinson's disease. The drug is marketed in Europe under tradename Lepticur.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (MIXED)
Targets:
Conditions:
Ifenprodil (marketed under the brands Vadilex; Dilvax; Creocral; Cerocral) is a selective NMDA receptor (glutamate) antagonist. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. Ifenprodil acts as a vasodilator. Ifenprodil is a medicine available in a number of countries worldwide, but not in US.
Status:
Possibly Marketed Outside US
Source:
NCT04446026: Phase 4 Interventional Completed Type 2 Diabetes Mellitus
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Teneligliptin is a DPP IV inhibitor which was developed by Mitsubishi Tanabe Pharma and now is used for the treatment of type 2 diabetes mellitus in Asia under the name Tenelia.
Status:
Possibly Marketed Outside US
Source:
MUCOSOLVAN by Boehringer Ingelheim
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Ambroxol, a substituted benzylamine, is an active
metabolite of bromhexine, which is itself
a synthetic derivative of vasicine, the active principle extracted from the plant species Adhatoda vasica. Ambroxol is an expectorant exerting mucokinetic properties, mucociliary activity, stimulation of surfactant production, anti-inflammatory and antioxidative actions and the local anaesthetic effect. Ambroxol was discovered at and has been manufactured by Dr. Karl Thomae GmbH, a division of Boehringer Ingelheim. The ambroxol patent is expired and the drug is available as a generic product from many different companies. Ambroxol was originally developed by Boehringer Ingelheim as a OTC therapy for respiratory disorders related to excessive mucus. Ambroxol's indication is secretolytic therapy in acute and chronic bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. Boehringer Ingelheim markets the product under various brand names such as Mucosolvan® and Lasolvan®. Ambroxol was identified and found to be a pH-dependent, mixed-type inhibitor of glucocerebrosidase (GCase). Its inhibitory activity was maximal at neutral pH, found in the endoplasmic reticulum, and undetectable at the acidic pH of lysosomes. The pH dependence of Ambroxol to bind and stabilize the enzyme was confirmed. Ambroxol increases both the lysosomal fraction and the enzymatic activity of several mutant GCase variants. This profile of Ambroxol would allow to bind and stabilize GCase in the endoplasmic reticulum (thus preventing its degradation within endoplasmic reticulum), but without affecting GCase in the lysosomes (thus allowing it to degrade glucosylceramide). Indeed, studies showed that Ambroxol treatment significantly increased N370S and F213I mutant GCase activity and protein levels in fibroblasts originally obtained from Gaucher patients. Gaucher's disease is caused by the deficiency of glucocerebrosidase; ambroxol is a chaperone that acts by binding to and stabilising glucocerebrosidase. Zywie (formerly ExSAR Corporation) and Belrose Pharma are developing ambroxol hydrochloride (BEL 0218) for the treatment of type III Gaucher's disease.
.
Status:
Possibly Marketed Outside US
Source:
NCT00892892: Phase 4 Interventional Withdrawn Chronic Kidney Disease
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Rilmenidine (brand names Albarel, Hyperium, Iterium and Tenaxum) is an imidazoline derivative used for the treatment of hypertension. Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists. Rilmenidine is as effective in monotherapy as all other first line classes of drugs, including diuretics, beta-blockers, angiotensin converting enzyme (ACE) inhibitors, and calcium antagonists. It is well tolerated and can be taken in combination for greater efficacy. Sedation and dry mouth are not prominent side effects and withdrawal hypertension is not seen when treatment is stopped abruptly. In addition to a reduction in blood pressure, Rilmenidine has been shown to improve glucose tolerance, lipid risk factors, and insulin sensitivity.