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Restrict the search for
obeticholic acid
to a specific field?
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:
NCT00987753: Phase 1/Phase 2 Interventional Completed Hormone Refractory Prostate Cancer
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT01107522: Phase 1 Interventional Active, not recruiting Solid Tumors, Glioblastoma, Recurrent Malignant Gliomas
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Carboxyamidotriazole (L651582) is a carboxyamide-amino-imidazole compound originally developed as a coccidiostat, an antiprotozoal agent that acts upon Coccidia parasites. Carboxyamidotriazole (L651582) is an orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2 channels, blocking both Ca2 influx into cells and Ca2 release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion, and metastasis.
Status:
Investigational
Source:
NCT04551118: Not Applicable Interventional Completed Healthy
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Lintitript (SR 27897) is a selective cholecystokinin type A (CCK-A) receptor antagonist, which was initially developed by Sanofi for appetite disorders. It is known, that CCK modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. Lintitript presumably alters feeding habits, however, the exact mechanism of action is not known. Lintitript was investigated in animals with anorexia nervosa, in addition, drug was in clinical trial for the patients with advanced pancreatic cancer, but these studies were discontinued.
Status:
Investigational
Source:
NCT02944383: Phase 2 Interventional Completed Severe Hypertriglyceridemia
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Gemcabene calcium (PD 72953), the monocalcium salt of a dialkyl ether dicarboxylic acid, is a lipid-regulating compound that was first described in 1998. It down-regulates apolipoprotein C-III expression, enhancing the clearance of very low density lipoprotein (LDL), and reduces plasma triglycerides. It also raises high-density lipoprotein cholesterol (HDL). Unlike fibrates (blood trygliceride level lowering drugs), its mechanism of action is not linked to agonist or antagonist activity on PPAR-α receptors. There is limited information on the exact mechanism of action, but an anti-inflammatory profile was found, associated with a lowered expression of the high-sensitivity C-reactive protein gene regulating mechanisms. Gemcabene (administered as 6, 6’-oxybis [2, 2-dimethyl-4-hexanoic acid] monocalcium salt) has been investigated for treatment in a wide range of hyperlipidaemias, as well as atherosclerosis, and cardiovascular disorders. Gemcabene is generally well tolerated. One phase 2 study testing the preliminary efficacy and safety of gemcabene in children with established nonalcoholic fatty liver disease has been stopped early due to increasing weight and a rise in liver fat content in patients. Clinical trials are still ongoing.
