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Status:
Possibly Marketed Outside US
Source:
NCT00219388: Phase 4 Interventional Completed Heart Failure
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Levosimendan (Simdax) is a novel intravenous agent that exerts inotropic effects through sensitization of myofilaments to calcium and vasodilator effects by binding to cardiac troponin C in a calcium-dependent manner. It also has a vasodilatory effect, by opening adenosine triphosphate (ATP)-sensitive potassium channels in vascular smooth muscle to cause smooth muscle relaxation. Unlike other calcium sensitizing compounds, the binding of levosimendan is highly dependent on the intracellular concentration of calcium, such that calcium sensitivity is enhanced only when the calcium level is elevated. Levosimendan is licensed for the treatment of decompensated heart failure in many countries but not in North America. This drug also passed phase III clinical trials for the prevention of low cardiac output syndrome in pediatric patients after open heart surgery.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Aspoxicillin is an injectable, amino acid-type penicillin highly active against Gram-positive ad Gram-negative bacteria, including the beta-lactamase producing Bacillus fragilis. It is reportedly effective in the treatment of peritonitis, pneumonia and bronchitis. Adverse reactions are: rash, urticaria, skin itching, vomiting, abdominal pain.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Astromicin is an aminoglycoside antibiotic produced by Micromonospora spp. It is effective against major gram-negative bacterias such as Proteus, Serratia, Citrobacter, Enterobacter spp., Klebsiella, Escherichia coli and Staphylococcus aureus. Astromicin sulfate has been given by intramuscular injection or intravenous infusion. Side effects are: rash, urticaria, itch, erythema, fever, nausea, vomiting, and diarrhea. Combination with strong diuretics can cause nephrotoxicity and ototoxicity.
Status:
Possibly Marketed Outside US
Source:
ARTECEF by Central Drug Research Institute
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Artemotil (also known as beta-arteether) is an antimalarial artemisinin derivative, approved for the treatment of severe cases of P. falciparum malaria. The mixture of artemotil and alpha-arteether is used in patients with cerebral malaria. Most of the artemisinin compounds including artemotil are metabolized into dihydroartemisinin, which is responsible for antimalarial activity. These compounds contain stable endoperoxide bridge. The antimalarial activity of the drug thus is dependent on the cleavage of the endoperoxide by intraparasitic heme. The cleaved endoperoxide ultimately becomes a carbon centered free radical, which then functions as an alkylating agent, reacting with both heme and parasitic proteins (but not DNA). In P. falciparum, one of the principal alkylation target is the translationally controlled tumor protein (DHA-TCTP) homolog. Some intraparasitic TCTP is situated in the membrane surrounding the heme-rich food vacuole, where heme could catalyse the formation of drug-protein (DHA-TCTP) adduct and inhibit the parasite's growth.
Status:
Possibly Marketed Outside US
Source:
Velaresol by Wellcome (GSK)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Velaresol, also known as BW12C or BW12C79, is an oxyhemoglobin stabilizer that has the potential to induce normal tissue and tumor hypoxia preferential binding to the oxy conformation of hemoglobin, increasing its affinity for oxygen and thereby reducing oxygen availability to tissues. Velaresol stabilizes oxyhemoglobin also protect sickle cells against calcium-mediated dehydration. The activity of a number of bioreductive anticancer drugs, such as mitomycin C, maybe enhanced under hypoxic conditions. Velaresol administration caused significant radioprotection of normal tissues and induced tumor necrosis.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Glymidine (Glycodiazine ) is a hypoglycaemic agent which has been introduced as a possible alternative to the sulphonylurea as and biguanides for the oral treatment of diabetes mellitus. It is one of a group of lipid soluble sulphapyrimidine derivatives synthesized by Gutsche et al. and bears some structural resemlance to tolbutamide. Its mode of action is similar to that of the sulphonylureas in that it appears to stimulate insulin release from the pancreas. Glycodiazine likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin. It is used for the concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus. Glycodiazine is used concomitantly with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Zuclomiphene Citrate is the cis isomer of clomiphene which exhibits weak estrogen agonist activity evaluated for antineoplastic activity against breast cancer. The individual isoforms are not available commercially, but Repros Therapeutics (The Woodlands, TX, USA) has separated them and is using enclomiphene citrate (ENC) in clinical trials in men with secondary hypogonadism who wish to preserve their fertility. Zuclomiphene, possessing no oestrogen antagonism at physiological concentrations, appears to have a longer biological half-life than enclomiphene, and thus may persist for long periods in the body. At high concentrations zuclomiphene can act as an oestrogen agonist. Clomiphene citrate (CC) is often used ‘off-label’ in men who have low testosterone to raise levels, it is also useful for the restoration of sperm counts in men. CC is approved by FDA and widely used in women for induction of ovulation for several conditions. CC is a mixture of two diastereoisomers, a cis isomer, zuclomiphene citrate (ZUC, 38%) and a trans isomer, ENC (62%). The two clomiphene isomers have mixed estrogenic and antiestrogenic effects that vary among species.
Status:
Possibly Marketed Outside US
Source:
NCT02022592: Phase 4 Interventional Completed Sedation in Intensive Care Unit Patients
(2014)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Lormetazepam (or methyl-lorazepam), possesses hypnotic, anxiolytic, sedative and skeletal muscle relaxant properties. Lormetazepam is not approved for sale in the United States or Canada, though it is licensed in the Netherlands as 1 and 2 mg tablets, under the brand names Loramet and Noctamid and as generic, available from several different manufacturers. Lormetazepam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or falling asleep. Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its therapeutic effects as well as adverse effects. Lormetazepam appears to be more selective in the type of benzodiazepine receptor it binds to showing a higher affinity for the omega 1 receptor which is responsible for sedation. Changes in electroencephalography can therefore be used to measure the sedative sleep promoting properties of lormetazepam.
Status:
Possibly Marketed Outside US
Source:
Fenint by Montedison [W. Germany]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Indoprofen is one of several NSAIDs that have been withdrawn from the market due to causing severe gastrointestinal bleeding. The UK Licensing Authority suspended the product license on grounds of safety in 1983 and in 1984 the Italian manufacturers decided to withdraw it from the world market. The UK decision was taken because there was a high rate of adverse drug reactions in a voluntary postmarketing surveillance study and the spontaneous adverse reaction reporting system had noted 217 serious adverse effects, mainly gastrointestinal bleeding and perforation.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Fluocortolone is a topical corticosteroid (class of steroid hormones formed in the adrenal gland). Is primary indicated in condition like, Ana fissure, Dermatosis haemorrhoids, proctitis. The signs and symptoms that are produced after the acute overdosage include convulsions, respiratory arrest, allergic skin reactions. Glucocorticoids, such as fluocortolone, act through nuclear hormone receptors Schaaf and Cidlowski (2002). The two members of this family are glucocorticoid receptor (GR) type I and GR type I I. Activation of these sites alters gene expression of endogenous agents that influence immune and inflammatory responses.