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Restrict the search for
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Status:
Investigational
Source:
INN:thymotrinan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Thymotrinan (also known as RGH-0205) is a protected synthetic tripeptide patented by Hungarian multinational pharmaceutical and biotechnology company Gedeon Richter Plc. (Richter, Gedeon, Vegyeszeti Gyar Rt) as an immunomodulating agent. Thymotrinan is the shortest thymopoietin fragment, that induces differentiation of CD90 cytotoxic T cell in the thymus. In preclinical models Thymotrinan is shown to exert similar immunomodulatory activities to thymopoietin affecting both humoral and cellular responses. In chronic 28-days i.v. toxicity studies in dogs no adverse reaction has been found. The low toxicity of Thymotrinan is probably attributable to their short half-life.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tizabrin is the antithrombotic, fibrinolytic agent. Tizabrin (CP-2129) stimulates fibrinolysis after intravenous administration in human volunteers due to an increase in tissue plasminogen activator (t-PA) activity. Tizabrin has no intrinsic fibrinolytic activity in vitro.
Status:
Investigational
Source:
NCT01051921: Phase 2 Interventional Completed Hepatitis C
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CTS-1027 (Ro-1130830) is a hydroxamic acid matrix metalloprotease (MMP) inhibitor. CTS-1027 was originally designed as a strong inhibitor of MMP-2, -3, -8, -9, -12, -13 and -14, without inhibiting MMP-1 and MMP-7. CTS-1027 was proved to be safe in clinical trials for osteoarthritis conducted by Roche. CTS-1027 was then licensed from Roche to Conatus Pharmaceuticals and was investigated as a protector from liver fibrosis in hepatitis C virus patients. The development of the drug was discontinued due to laboratory abnormalities and adverse events in a subset of clinical trial participants.
Class (Stereo):
CHEMICAL (ACHIRAL)
Ticolubant (also known as SB-209247) is a pyridine derivative patented by SmithKline Beckman Corp. as an anti-inflammatory leukotriene B4 receptor antagonist. Ticolubant displays high affinity for the human neutrophil LTB4 receptor, blocks LTB4-induced Ca2+ mobilization, and demonstrates potent oral and topical antiinflammatory activity in a murine model of dermal inflammation. However, Ticolubant did not show significant oral activity in a murine model of inflammation. Development of Ticolubant was discontinued when administration to beagle dogs for 28 days was associated with non-dose-dependant inflammatory hepatopathy, with minimal hepatocellular necrosis being observed in the more severe cases
Class (Stereo):
CHEMICAL (EPIMERIC)
KETOTREXATE is an antifolate developed to overcome methotrexate (MTX) resistance. However, it demonstrated such potential only in MTX-resistant sensitive L1210/FR8 leukemia cells and its clinical development was discontinued. Unlike MTX, KETOTREXATE exhibited minimal inhibition of purified dihydrofolate reductase, which implies that it does not act as a classical antifolate.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Lotrafiban (SmithKline Beecham) is a member of the latest generation of orally-active platelet GPIIb/IIIa blockers undergoing Phase III clinical trials to test the relative effectiveness versus other oral platelet inhibitors for ischaemic conditions including unstable angina, restenosis after PCI and stroke. Lotrafiban is converted from an esterified prodrug by plasma and liver esterases to a peptidomimetic of the arginine-glycine-aspartic acid amino acid sequence. This sequence itself mimics the binding site of fibrinogen and von Willebrand Factor to the platelet GPIIb/IIIa receptor. Preliminary results of the clinical trial APLAUD (antiplatelet useful dose) show that lotrafiban is clinically safe and well-tolerated in patients with recent myocardial infarction, unstable angina, transient ischaemic attack (TIA), or stroke when added to aspirin therapy. The Blockade of the IIb/IIIa Receptor to Avoid Vascular Occlusion (BRAVO) trial of SmithKline Beecham's oral GpIIb/IIIa blocker, lotrafiban, has been stopped early because of concerns about both safety and efficacy. The drug was showing a higher mortality rate than placebo, and was also associated with an increased incidence of serious thrombocytopenia and major bleeding. As a result of these findings the company has discontinued development of lotrafiban.
Status:
Investigational
Source:
NCT01943162: Not Applicable Interventional Completed PTSD With a History of Mild to Moderate TBI
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Mureletecan is a water-soluble prodrug, consisting of camptothecin covalently linked to polymeric backbone methacryloylglycynamide, with potential antineoplastic activity. After entering tumor cells, the active moiety camptothecin is slowly released from mureletecan via hydrolysis of the ester linkage. Camptothecin, the active moiety, is an alkaloid isolatable from the Chinese tree Camptotheca acuminata. Camptothecin itself suffers from poor solubility, which is why it is often investigated with a solubilizing conjugate; such as in Mureletecan. Camptothecin binds to and stabilizes the topoisomerase I-DNA covalent complex producing potentially lethal double-stranded DNA breaks when encountered by DNA replication machinery. Camptothecin has also been shown to inhibit HIF1a. Camptothecin has been investigated with a number of solubilizing conjugates as a potential treatment in various forms of cancer.
Status:
Investigational
Source:
NCT00987753: Phase 1/Phase 2 Interventional Completed Hormone Refractory Prostate Cancer
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00090025: Phase 3 Interventional Terminated Biliary Tract Cancer
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Rebeccamycin analog (RA, Becatecarin/ BMS 181176, rebeccamycin derivative, NSC 655649) is an antitumor antibiotic with inhibitory activity against both topoisomerase I and II, and DNA-intercalating properties. The mechanism of action of becatecarin is not exactly known, but it is thought that by inhibiting (blocking) the function of topoisomerase enzymes, it will destroy cancer cells and slow down the growth of the tumour. On 25 July 2006, orphan designation (EU/3/06/388) was granted by the European Commission to Helsinn Birex Pharmaceuticals Ltd, Ireland, for becatecarin for the treatment of cancers of the biliary tree.
Class (Stereo):
CHEMICAL (ACHIRAL)
Dotarizine was developed as antimigraineur. Dotarizine inhibited the 5-HT2A response in a concentration-dependent manner. The mechanism of blockade by dotarizine of cerebral vessels contractility has three components: (i) presynaptic inhibition of noradrenaline release; (ii) blockade of postsynaptic vascular 5-HT receptors; (iii) blockade of Ca(2+)entry into the vascular smooth muscle cell cytosol. The compound does not affect the vascular receptors for noradrenaline, angiotensin II or prostaglandin F(2alpha). Dotarizine had a pronounced protective effect against electric seizures.
