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Restrict the search for
dimethyl fumarate
to a specific field?
Status:
Investigational
Source:
NCT00080132: Phase 2 Interventional Terminated Hypertriglyceridemia
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor with antihyperlipidemic activity. Microsomal triglyceride transfer protein (MTP) is essential for the synthesis of both chylomicron in the intestine and very low-density lipoprotein in the liver. In an animal model, inhibition of MTP by implitapide reduced both total cholesterol and triglyceride levels and suppressed progression of atherosclerotic lesions in apolipoprotein E knockout mice fed a Western-type diet.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Darodipine is a calcium channel blocking drug, developed by Sandoz in the early 1980s. It potently and selectively antagonizes calcium-induced contraction, decreases the rate of spontaneously beating guinea-pig and rabbit atria. In open-chest dogs, darodipine increased coronary flow and cardiac output, lowered blood pressure, and tended to decrease heart rate while the myocardial contractile force was unchanged. Administration of darodipine led to a significant reduction in mortality and in the severity of neurological symptoms in various types of experimental brain ischemia. Clinical trials demonstrated efficacy for the treatment of stable angina pectoris. In the pilot trial, darodipine was found to be safe but not effective in patients with acute ischemic cerebral infarction.
Status:
Investigational
Source:
Am J Clin Oncol. Apr 2001;24(2):150-4.: Phase 2 Human clinical trial Completed Prostatic Neoplasms
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Menogaril is a semisynthetic derivative of the anthracycline antineoplastic antibiotic nogalamycin. Biochemical studies indicated that, in comparison to doxorubicin, menogaril is bound weakly to DNA, inhibits RNA synthesis less, and has different cell cycle phase-specific cytotoxicity. Menogaril acts as a cleavable complex-stabilizing topoisomerase II inhibitor. Menogaril has been studied in the treatment of various cancers.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Mixidine is negative chronotropic agent patented by McNeil Laboratories. Mixidine produced a dose-related decrease in heart rate elevated reflexly by aminophylline, by beta-adrenergic stimulation induced by isoproterenol, by sympathetic nerve stimulation and by intravenous infusion of glucagon. Mixidineattenuated the increase in contractile force produced by sympathetic nerve stimulation but not that induced by isoproterenol. The compound antagonized the increase in the rate of isolated guinea-pig atria induced by both isoproterenol and histamine. In the conscious dog, Mixidine caused no decrease in resting heart rate, mean arterial pressure and cardiac output. It reduced atropine-induced sinus tachycardia as well as that induced by treadmill exercise.
Class (Stereo):
CHEMICAL (ACHIRAL)
Metipirox was developed as a bactericide agent. Information about the current use of this compound is not available
Class (Stereo):
CHEMICAL (MIXED)
Myfadol is a phenacylpiperidine derivative patented by Tanabe Seiyaku Co., Ltd as low molecular weight non-peptide analgesic. Myfadol produces hot-plate analgesia in rodents with minimal side-effects, and when given parenterally in humans produces analgesia to experimentally-produced and postoperative pain.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Brobactam is a synthetic inhibitor of beta-lactamases produced by both gram-positive and gram-negative bacteria. Brobactam potentiates the antibacterial activity of ampicillin against a wide range of clinically important bacterial strains which produce beta-lactamase. No resistant sub-population was observed amongst the strain s of staphylococci studied, and the development of resistance in vitro was not recorded in individual strains of Staphylococcus aureus and Escherichia coli exposed to subinhibitory concentrations of ampicillin/brobactam. Reduced sensitivity was observed in the case of one strain of M. morganii, which was known to produce an inducible chromosomal cephalosporinase.
Status:
Investigational
Source:
NCT00564226: Phase 2 Interventional Completed Overactive Bladder
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Burapitant (SSR-240,600) is a drug developed by Sanofi-Aventis which was one of the first compounds developed that acts as a potent and selective antagonist for the NK1 receptor. Burapitant inhibited the binding of radioactive substance P to tachykinin NK1 receptors in human lymphoblastic IM9 cells, human astrocytoma U373MG cells, and human brain cortex. It also showed a subnanomolar affinity for guinea pig NK1 receptors but was less potent on rat and gerbil NK1 receptors. Burapitant inhibited [Sar(9),Met(O2)(11)]substance P-induced inositol monophosphate formation in human astrocytoma U373MG cells. Burapitant (0.1-10 mg/kg i.p. or p.o.) antagonized the excitatory effect of i.c.v. infusion of [Sar(9),Met(O2)(11)]substance P (SP) on the release of acetylcholine in the striatum of anesthetized and awake guinea pigs. This antagonistic action was still observed after repeated administration of Burapitant (5 days, 10 mg/kg p.o., once a day). Burapitant (10 mg/kg i.p.) inhibited the phosphorylation of the cAMP response element-binding protein in various brain regions induced by i.c.v. administration of [Sar9,Met(O2)(11)]SP. While burapitant itself did not proceed beyond early clinical trials and was never developed for clinical use in humans, promising animal results from this and related compounds have led to a number of novel drugs from this class that has now been introduced into medical use.
Status:
Investigational
Source:
NCT01490736: Phase 1/Phase 2 Interventional Completed Acne
(2011)
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Lemuteporfin is a newly introduced, light-sensitive drug for use in combination photodynamic therapy (PDT). It acts on mitochrondria to initiate the apoptotic cascade resulting in cell death (apoptosis). The photosensitizer was highly potent, killing cells at low nanomolar concentrations upon exposure to activating light. The cellular uptake of lemuteporfin was rapid with maximum levels reached within 20 min. Mitogen-activated lymphoid cells accumulated more of the lemuteporfin than their quiescent equivalents, supporting selectivity. Lemuteporfin had been in phase II clinical trials for the treatment of benign prostatic hypertrophy. It is in phase I clinical trials for the treatment of acne rosacea.
