{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
NCT00000650: Not Applicable Interventional Completed HIV Infections
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Ditiocarb, the sodium salt of diethyldithiocarbamate, is a drug with strong antioxidant capacity and chelating activities. It improves the depressed immune responses of newborn and aged mice and mice that are treated with chemotherapy or irradiation. Ditiocarb prevents cisplatin nephrotoxicity in animals without reducing the drug's antitumor activity. Ditiocarb has therapeutic activity in the LP-BM5 murine retrovirus-induced immunodeficiency disease. In that AIDS model, it reduces lymphadenopathy and hypergammaglobulinemia, restores immunocompetence, and prolongs survival. Ditiocarb was safe and reduced the incidence of opportunistic infections in patients with symptomatic HIV infection but ditiocarb had no positive effect on HIV patients. The administration of ditiocarb did not induce any major adverse clinical or biological reactions. Sixty-four patients with nonmetastatic high-risk breast cancer were randomized in a double-blind trial of adjuvant immunotherapy with sodium ditiocarb (DDC) versus placebo. At 6 years, overall survival was 81% in DDC group versus 55%.
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.
Class (Stereo):
CHEMICAL (ACHIRAL)
Brovanexine is a derivative of bromhexine used as an adjunct to antibacterials in preparations for the treatment of respiratory-tract infections. Oral administration of brovanexine hydrochloride (BR-222) caused a significant increase in the output volume of respiratory tract fluid. Brovanexine at 10 and 20 mg/kg showed a tendency to reduce the viscosity of respiratory tract fluid in anesthetized dogs. Brovanexine also showed a tendency to reduce the viscosity of sputum obtained from the SO2-exposed rabbits.
Status:
Investigational
Source:
NCT00048022: Phase 2 Interventional Completed Asthma
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Valategrast (R-411) is a dual-acting α4/β1 - α4/β7 integrin antagonist which underwent clinical development with Roche for the treatment of multiple sclerosis (MS) and asthma. Phase I and II studies have been
conducted. It had shown good efficacy in animal disease models. Following oral administration, R-411 was rapidly
and completely biotransformed into its active metabolite, RO-0270608, most of which was eliminated by biliary excretion. R-411 had shown acceptable pharmacokinetics and
good safety in healthy volunteers. R-411 inhibited eosinophil and T H 2 cell excitation and survival, and inhibited eosinophil migration from blood to pulmonary tissues. The idea of combining R-411 with montelukast (leukotriene antagonist) in the pharmaceutical dosage
forms, therefore, provided a therapeutic treatment that had the combined effect of reducing circulating eosinophil counts
and reducing eosinophil egress into pulmonary tissues, thereby providing an early onset of bronchodilation as well as sustained anti-inflammatory effects. Valategrast had been in phase II clinical trials by Roche for the treatment of asthma and in phase I clinical trials for the treatment of multiple sclerosis (MS). However, the study had been discontinued. Development of Valategrast was
discontinued for the treatment of asthma after clarification of the regulatory framework for that class of compounds.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Proterguride is a highly potent dopamine receptor agonist with a long duration of action patented by Schering A.-G. for the treatment of Parkinsonism, restless leg syndrome, or the prophylaxis of migraine. According to preclinical studies, Proterguride, unlike most dopamine receptor agonist, is suitable for transdermal administration. Especially in the case of dopamine agonists, the transdermal route of administration might become of great clinical importance due to the ability to achieve constant plasma levels and, thus, to imitate the physiological continuous release profile of dopamine. Pulsatile stimulation of dopaminergic receptors as it occurs with oral administration of dopaminergic drugs is considered the cause of treatment-associated motor complications.
Status:
Investigational
Source:
INN:limiglidole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Limiglidole belongs to the class of benzimidazole derivatives exhibiting various biological activities including inhibition of platelet aggregation and prolongation of clotting time in animal models. It inhibited platelet aggregation induced by ADP. Antithrombotic activity of hypoglycemic compound limiglidole that exhibits antiplatelet activity 2-fold exceeded activity of antiplatelet agent acetylsalicylic acid in the mouse model of systemic collagen-epinephrine thrombosis. Antithrombogenic properties of limiglidole are beneficial in the treatment of diabetes mellitus.
Status:
Investigational
Source:
NCT01568229: Phase 2 Interventional Terminated Schizophrenia
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Tilapertin (also known as AMG 747) is a piperazineacetic acid derivative patented by Amgen Inc as glycine transporter-1 inhibitor useful for the treatment of negative symptoms of schizophrenia. Oral administration of AMG 747 dose-dependently increases cerebrospinal fluid(CSF) glycine concentration in rats. In humans, Tilapertin has linear pharmacokinetics, prolonged half-life, and acceptable safety and tolerability at multiple doses up to 60 mg daily dosing. Unfortunately, in clinical trials, Tilapertin failed to demonstrate superior efficacy compare antipsychotic therapy in clinically stable people with schizophrenia.
Status:
Investigational
Source:
NCT01903824: Phase 1 Interventional Completed Cognitive Impairment
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
IRDABISANT is a histamine H3 receptor inverse agonist with potential therapeutic utility in cognition enhancement.
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.
Class (Stereo):
CHEMICAL (UNKNOWN)
Talisomycin (former trivial name: tallysomycin A), a third generation bleomycin analog that was studied as an antitumor antibiotic. The drug cleaved DNA preferentially at G-C and G-T sequences and produced specific cleavages at G-A sequences. Talisomycin participated in phase II clinical trial for the treatment of cancer; however, the further development of the drug was discontinued.
