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Restrict the search for
amphotericin b
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Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Mivotilate is an orally active hepatoprotective agent for the treatment of liver cirrhosis and hepatitis-B infection. Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450 system, particularly to inhibit CYP2E1 expression and to up-regulate the CYP1A1 expression. The low oral bioavailability of Mivotilate in rats could be primarily attributed to poor absorption and considerable hepatic and gastrointestinal first-pass effects. The thermal reversible microemulsion system of YH439 greatly enhances the bioavailability of YH439 after oral administration. Mivotilate prevents mutagenesis caused by agents such as benzopyrene and reduces skin tumours induced by these agents.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rifametane (SPA-S-565) is a semisynthetic derivative of rifamycin (a natural antibiotic produced by Amycolatopsis rifamycinica). It was being evaluated for treatment of bacterial infections. A phase I study showed that administration of rifametane is safe with minor, reversible adverse events such as mild headache, metallic taste and slightly elevated temperature for 3 to 4 hours. Rifametane has anti-tuberculosis activity and was suggested to be a good candidate for phase II clinical trials.
Status:
Investigational
Class (Stereo):
CHEMICAL (MIXED)
Doxaminol is a recently developed beta-sympathomimetic agent, which has shown promising positive inotropic activity in experimental animal models. It is a dibenzoxepine derivative. In normal volunteers, doxaminol exhibits effects on noninvasive cardiological indices similar to those observed after cardiac glycosides. After single-dose application of doxaminol in cases of congestive heart failure, cardiac output and stroke volume increased, heart rate increased slightly, pulmonary and systemic arterial pressure remained constant, and peripheral vascular resistance decreased. No arrhythmias appeared, but one patient suffered an attack of angina.
Status:
Investigational
Source:
NCT00560716: Phase 1 Interventional Terminated Solid Tumors
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
CYC-116 is a novel, ATP-competitive, pyrimidine drug that is taken by mouth as a capsule. The drug is a selective agent that potently inhibits the enzymes Aurora kinases and VEGFR-2 kinase at comparable levels with a range of 19 to 69 nanomolar. Median potency of CYC-116 in cancer cells is approximately 300 nanomolar. CYC-116 has demonstrated a broad spectrum of potent cytotoxic activity against human tumor cell types. Non-clinical efficacy of CYC-116 has been demonstrated by the oral route using mouse leukemia models, in which increased survival was observed, and human solid tumor xenograft models, in which reductions in tumor growth were observed. Cancer cell types that appear to be particularly sensitive to CYC-116 are leukemia, non-small cell lung cancer and pancreatic cancer. CYC-116 works by affecting the cell cycle progression of cancer cells before they enter mitosis or divide to create daughter cancer cells. The mechanism of action of CYC-116 affects cancer cells in several ways. CYC-116-treated cells display delayed entry into mitosis; defective polymerization of tubulins, or proteins that make up microtubules which are the target of the taxane drugs; changes in the function of the centrosome, or the cell's microtubule organizing center; and formation of the mitotic spindle, or the highway along which chromosomes and cellular materials are transported from the mother cell to the daughter cells. After cancer cells are treated with CYC-116, their spindle checkpoint is inactivated resulting in inhibition of cytokinesis or the process by which a mother cell divides. These defects result in the generation of polyploidy or cells with more than two chromosome sets, multinucleated cells or cells with multiple cores and apoptosis or cancer cell death. In a mouse model of leukemia CYC116-treatment induced decreases in tumor cell volume and infiltration of leukemic cells in the bone marrow and resulted in an increase in life span. No significant effects on body weight or normal bone marrow cells were observed at effective doses of CYC-116. Tumor neovascularization, or creation of new blood vessels around a tumor, was significantly reduced in a dose dependent manner. The data confirm that CYC-116 acts as a dual mitotic and angiogenesis inhibitor, a combination of anti-cancer mechanisms which could have therapeutic benefit in the clinic. CYC-116 is currently being studied in a Phase 1 trial in patients with solid tumors at Roswell Park Cancer Institute in Buffalo, New York, and South Texas Accelerated Research Therapeutics (START) in San Antonio. The study is designed to identify the maximum tolerated dose of CYC-116 and evaluate its pharmacokinetic, pharmacodynamic and anti-tumor effects.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Beciparcil, an antithrombotic drug, that was studied against thrombosis, however, further investigations were discontinued in 1997.
Class (Stereo):
CHEMICAL (ACHIRAL)
Clobenzepam (tarpane) is a drug exhibiting antihistaminic properties.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
There is no information about biological and medical application of dorastine . It’s known, that compound possesses antihistamine properties and can be obtained from 4-chloroaniline.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Pinoxepin belongs to the dibenzoxepine series of drugs which are characterized by a 6-7-6 tricyclic nuclear structure. Clinical studies indicated that pinoxepin was a potent antipsychotic-sedative equally effective to chlorpromazine and thioridazine. Pinoxepin in studies with chronic schizophrenic patients displayed useful effects on behavior without unduly prominent side effects. In doses above 300 mg seizures are reported and more frequent changes in liver-function tests were noted than with standard drug, but below 300 mg pinoxepin was found to have side effects similar to chlorpromazine and marked sedative effects.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Quazinone (also known as Ro 13-6438 ) is a cardiotonic and vasodilator drug which was developed and marketed in the 1980s for the treatment of heart disease. The positive inotropic response to Quazinone of the isolated guinea pig papillary muscle was accompanied by inhibition of myocardial phosphodiesterase (PDE) activity and elevation of intracellular cyclic AMP (cAMP) levels Quazinone had no effect on Na+, K+-stimulated or Ca2+-stimulated ATPase activity and did not influence the rate of calcium uptake in cardiac membrane vesicles. Quazinone caused a concentration-dependent increase in the upstroke velocity, overshoot, and duration of slow action potentials evoked in partially depolarized papillary muscles. Pretreatment of guinea pigs with reserpine did not prevent the effects of Quazinone on slow action potentials but slightly decreased its positive inotropic activity. In clinical trials, Quazinone induces dose-dependent hemodynamic changes, an increase in cardiac index combined with decreases in pulmonary capillary wedge pressure and systemic and pulmonary arterial pressures.
Status:
Investigational
Source:
NCT00083252: Phase 2 Interventional Completed Melanoma
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Talabostat is a prolineboronate ester derivative patented by Boehringer Ingelheim Pharmaceuticals, Inc. as an antineoplastic agent. Talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity. Talabostat has been shown to cause caspase-1 activation and IL-1β induction in macrophages, which in turn causes upregulation of the cytokines and chemokines that characterize the responses to talabostat, both in vitro and in tumor-bearing mice. Talabostat may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. In clinical trials, the combination of talabostat and cisplatin was well tolerated compared to historical data using cisplatin alone. The most frequent adverse events were nausea, vomiting, fatigue, anemia, edema, and constipation. Unfortunately was no evidence that Talabostat enhanced the clinical activity of other anticancer drugs and further development was discontinued.
