U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 881 - 890 of 13311 results

Status:
Investigational
Source:
INN:levomequitazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levomequitazine is the L-enantiomer of mequitazine. The antihistaminergic activity mainly resides in the S-enantiomer, L-mequitazine, whereas the anticholinergic activity mainly resides in the D-enantiomer. It was shown, that L-enantiomer of mequitazine is less potent antagonist of human M3 muscarinic acetylcholine receptors than D-enantiomer. In vitro binding studies have shown that the affinity of L-mequitazine for H1 receptors is approximately ten times higher and to muscarinic receptors ten times lower, compared to d-mequitazine. Memory impairment was observed after administration of L-mequitazine 10 mg alone on delayed recall. This could be due to indirect effects of H1 receptor blockade. L-mequitazine 10 mg produced mild driving impairment, whereas L-mequitazine 2.5 and 5.0 mg show no effects on driving. Levomequitazine had been in phase III clinical trials by Pierre Fabre for the treatment of perennial allergic rhinitis and seasonal allergic rhinitis.
Status:
Investigational
Source:
INN:pimelautide
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Pimelautide is the immunomodulating lipopeptides lauroyl-L-Ala-gamma-D-Glu-LL-A2pmNH2-Gly. Pimelautide is an immunostimulant active on macrophages, polymorphonuclear leukocytes, T-lymphocytes, and NK cells, which in mice enhances delayed type hypersensitivity reactions, antibody production and resistance to bacterial infections. It was found to protect mice against the hepatotoxicity of paracetamol, which is due to cytochrome P-450 dependent formation of toxic metabolites and radicals. It decreased the amount of hepatic microsomal cytochrome P-450, and the level of CCl4-induced lipid peroxidation.
Status:
Investigational
Source:
NCT01723982: Phase 2 Interventional Completed Infertility
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Barusiban, a long-acting oxytocin antagonist, has been studied to stop preterm labor in pregnant women at late gestational age. The experiments failed to demonstrate the effectiveness and were discontinued. However, barusiban participates in phase II clinical trials for female infertility.
Status:
Investigational
Source:
INN:mercurobutol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Mercurobutol is an antiseptic and disinfectant. Mercurobutol exhibits fungistatic and fungicidal activities.
Status:
Investigational
Source:
NCT00040989: Phase 2 Interventional Withdrawn Stage IV Renal Cell Cancer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Afeletecan (Bay 38-3441) is a camptothecin glycoconjugate which stabilizes the active lactone form of camptothecin and allows selective uptake into tumor cells. Afeletecan is a topoisomerase inhibitor. Afeletecan was in phase I clinical trials with Bayer for the treatment of cancer; however, development appears to have been discontinued.
Status:
Investigational
Source:
NCT01064037: Phase 2 Interventional Terminated Heart Failure
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cinaciguat acts specifically on oxidized/haem-free soluble guanylyl cyclase by binding to the enzyme's haem pocket and mimicking the nitric-oxide-bound haem group. It is in clinical development for the treatment of acute decompensated heart failure. Cinaciguat had been in phase II clinical trials. However, trials were terminated early because of an excess of hypotension in the cinaciguat arms and subsequent slow enrolment.
Status:
Investigational
Source:
INN:coumazoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Coumazoline is a vasoconstrictor developed as a nasal decongestant by a French corporation Labez. Intravenous administration of the compound to dogs lead to a marked and prolonged drop in the temperature of the gingival mucosa. In rats, coumazoline caused slowing of the dye diffusion on the surface of the skin. The compound did not influence the ciliary motility, as was measured on an isolated guinea pig trachea.
Status:
Investigational
Source:
NCT00027781: Phase 2 Interventional Completed Prostate Cancer
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sabarubicin (previously known as MEN-10755), a disaccharide analog of doxorubicin that was developed by Menarini Pharmaceuticals for the treatment of solid tumors, including small cell lung cancer and prostate cancer. Sabarubicin exhibits a superior antitumor efficacy, presumably related to the activation of p53-independent apoptosis. The drug participated in phase II clinical trials to study its effectiveness in treating patients who have progressive prostate cancer that has not responded to hormone therapy and in chemotherapy-naive patients with extensive stage small cell lung cancer. On 21 December 2004, the European Commission granted the orphan designation to Menarini for sabarubicin for the treatment of small cell lung cancer.
Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.
Status:
Investigational
Source:
NCT00631488: Phase 2 Interventional Completed Diabetes Mellitus, Type 2
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



MK-0893, developed by Merck, is a reversible and competitive antagonist with high binding affinity (IC(50) of 6.6 nM) and functional cAMP activity (IC(50) of 15.7 nM). MK-0893 reached Phase 2; 12 weeks of once daily oral dosing led to significant and dose-dependent reductions in fasting and post-prandial plasma glucose and in HbA1c, with similar low incidences of hypoglycaemia as a metformin cohort. Combinations with metformin and sitagliptin were also trialled, and risk for hypoglycaemia was assessed in healthy males which showed the drug caused lengthening of recovery times. However, plasma levels of LDL cholesterol and liver transaminases were increased in some studies, as was body weight and blood pressure, all of which were not evident pre-clinically, and MK-0893 was discontinued.