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Restrict the search for
icosapent ethyl
to a specific field?
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Piprocurarium is a curarimimetic. It is antagonized by neostigmine. Piprocurarium is strongly vagolytic, producing tachicardia. Its duration of action is shorter than that of d-tubocurare and longer than that of succinylcholine. Piprocurarium is not hypotensive, is only slightly histaminogenic, is nonirritating to the veins, and can be mixed with all the anesthetic drugs. Piprocurarium has been offered for clinical trial as a brief-acting, nondepolarizing neuromuscular blocking drug. The drug appears to be anything but short acting. A persistent tachycardia and elevation in systolic and diastolic pressure invariably follows its intravenous injection. Alarming electrocardiographic changes occur, characterized by AV dissociation, depression of the ST segment, supraventricular tachycardia and, at times, inversion of the T waves. In view of these circulatory effects, it is doubtful that the drug will be useful clinically.
Class (Stereo):
CHEMICAL (RACEMIC)
Dexpemedolac is long-acting non-narcotic analgesic. Dexpemedolac exhibited potent analgesic effects against chemically induced pain in rats and mice and against inflammatory pain in rats. Dexpemedolac differed from standard nonsteroidal anti-inflammatory drugs (NSAIDs) in that the doses, which produced analgesia were much lower than those required for either anti-inflammatory or gastric irritant effects. The common to the NCAIDs class actions are antipyresis and inhibitory effects on platelet aggregation. In yeast-induced hyperthermic rats, dexpemedolac exhibited antipyretic actions, whereas the drug did not affect body temperature in normothermic animals. Aggregation of human platelets was inhibited by high concentrations of dexpemedolac.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sibrafiban (G-7453) is the orally administered, nonpeptide, double-prodrug of Ro 44-3888 which is a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban is a double prodrug that undergoes bioconversion to the inactive prodrug Ro 48-3656 and to the active IIb/IIIa antagonist, Ro 44-3888, after oral administration. Sibrafiban was undergoing clinical trials for secondary prevention of cardiac events in patients stabilised after acute coronary syndromes. Sibrafiban has been shown to have comparable efficacy to aspirin in preventing recurrent ischemic events in patients suffering from acute coronary syndromes. Sibrafiban was under development by Genentech and Hoffmann-La Roche, and in phase III trials as an antithrombotic. The development of sibrafiban was discontinued in 1999 following unfavorable Phase III efficacy data.
Class (Stereo):
CHEMICAL (RACEMIC)
Soterenol [(+)-1-(3-methanesulphonamido, 4-hydroxyphenyl)-2-isopropylaminoethanol, MJ 1992] is a directly acting sympathomimetic amine which has been shown to display Beta2-adrenoceptor selectivity. Soterenol, a methanesulfonamido-phenethanolamine related structurally to isoproterenol, was a highly effective bronchodilator agent in several animal species by various routes of administration. The bronchodilator potency of soterenol was equivalent to, or greater than, that of isoproterenol. Soterenol also had potent stimulant action on the alpha-receptor of the smooth muscle.
Status:
Investigational
Class (Stereo):
CHEMICAL (MIXED)
Mesuprine is a β-adrenergic-receptor mimetic agent. It is a smooth muscle relaxant that prevents uterine contractility and premature labor.
Class (Stereo):
CHEMICAL (RACEMIC)
Rocastine (AHR-11325) is a potent, nonsedating antihistamine with a rapid onset of action. This H1-antagonist effectively protected guinea pigs challenged with a lethal dose of histamine. It has also been mentioned in patents as a candidate to treat eye conditions and cough/cold mixtures (in which the lack of sedative effects from a non-sedating antihistamine would be especially useful in children, because daytime sedation is especially undesirable in this group). However, information on current use is not available and other second-generation, non-sedative antihistamines are available.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Letimide is a new analgesic. It is a cyclic derivative of a salicylamide. The analgesic effect of this drug as determined in rats showed a higher potency than aspirin, but was without anti-inflammatory and antipyretic activity. Letimide is not a genotoxic agent according to the cytogenetic damage observed in vivo and in vitro, and would seem to justify other preclinical and clinical studies to confirm its lack of toxicity. Known adverse effects are headache and dizziness.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levdobutamine is a beta-adrenoceptor agonist selective for the beta1-subtype. Levdobutamine was derived from dopamine. It is the active (S)-isomer of dobutamine. It is the cardiotonic agent.
Status:
Investigational
Source:
NCT03594058: Phase 2 Interventional Completed Overactive Bladder
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Solabegron (GW427353), a beta-3 adrenoceptor agonist, is in development with AltheRx (now Velicept Therapeutics) for the treatment of irritable bowel syndrome (IBS) and overactive bladder (OAB). Solabegron was discovered and first developed by GlaxoSmithKline. It was acquired by AltheRx, which merged with Velicept in 2015 to continue development of the program. Solabegron has been tested in over 800 study subjects in a twice-a-day formulation and demonstrated efficacy in the treatment of OAB as well as IBS. A once daily formulation designed to optimize patient convenience as well as efficacy has been developed and is currently being evaluated in a phase 2b dose ranging clinical trial. A Phase 2b dose ranging study with the twice daily formulation also began enrollment in Q1 2018.
Status:
Investigational
Source:
Cancer Treat Rep. Aug 1978;62(8):1173-6.: Phase 2 Human clinical trial Completed Neoplasms
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Hycanthone is a thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. It was clinically available for the treatment of human schistosomiasis. Anti-helmintic action relies on its ability to inhibit worm monoamine oxidase and cholinesterases. Hycanthone produced immediate side effects such as hepatotoxicity and gastrointestinal disturbances, and was consequently withdrawn. Hycanthone inhibits apurinic endonuclease-1 (APE1) by direct protein binding. Hycanthone was used in the 1980s as antitumor agents, it was pulled out of Phase II trials.
