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

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Showing 891 - 900 of 10251 results

Status:
Investigational
Source:
NCT01202370: Phase 1 Interventional Completed Solid Malignancies
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

AR-67 is a third-generation camptothecin analogue that was being developed by Arno Therapeutics for the treatment of cancer, but has been discontinued. AR-67 had been in phase II clinical trials for the treatment of glioblastoma multiforme and myelodysplastic syndrome. AR-67is a synthetic, highly lipophilic derivative of camptothecin, with potential antineoplastic and radiosensitizing activities. AR-67 binds to and stabilizes the topoisomerase I-DNA covalent complex, inhibiting the religation of topoisomerase I-mediated single-stranded DNA breaks and producing lethal double-stranded DNA breaks when encountered by the DNA replication machinery; inhibition of DNA replication and apoptosis follow. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form. Modifications on the E ring of camptothecin prevent binding of human serum albumin, which prefers the inactive carboxylate form, thereby enhancing the stability of the active lactone structure and resulting in prolonged agent activity.
Status:
Investigational
Source:
NCT02195232: Phase 2/Phase 3 Interventional Completed Thromboembolism of Vein VTE in Colorectal Cancer
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Isoquercetin is a flavonoid, derivative of quercetin. It was isolated from various plant species including Ammothamnus Lehmanii, Caragana alaica, Cicer baldshuanicum, C. macroconthum, C. pungens, Euphorbia cyparissias, E. helioscapia, E. lathyris, E. lucida, E. purporata and others. It demonstrated radical scavenging activity, inhibitory effects on Na+/K+-ATPase and positive inotropic activity. It is protein disulfide isomerase (PDI) inhibitor. As a PDI inhibitor, this agent blocks PDI-mediated platelet activation, and fibrin generation, which prevents thrombus formation after vascular injury. Isoquercetin inhibited the replication of both influenza A and B viruses at the lowest effective concentration. Isoquercetin activates the ERK1/2-Nrf2 pathway and protects against cerebral ischemia-reperfusion injury in vivo and in vitro. It is being investigated for prevention of thromboembolism in selected cancer patients and as an anti-fatigue agent in kidney cancer patients treated with sunitinib.
Status:
Investigational
Source:
NCT00945282: Phase 2 Interventional Completed Infection, Human Immunodeficiency Virus
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:noracymethadol
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Status:
Investigational
Source:
NCT00558662: Not Applicable Interventional Completed Venous Ulcer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02031432: Phase 3 Interventional Completed Pain
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Cebranopadol is a novel analgesic nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist. Cebranopadol, by its combination of agonism at NOP and opioid receptors, affords highly potent and efficacious analgesia in various pain models with a favorable side effect profile. Cebranopadol displays analgesic, antiallodynic and antihyperalgesic properties in several rat models of acute nociceptive, inflammatory, cancer and neuropathic pain. Unlike morphine, cebranopadol did not disrupt motor coordination and respiration at doses within and exceeding the analgesic dose range possessing a broader therapeutic window than classical opioids. It is currently in clinical development for the treatment of severe chronic nociceptive and neuropathic pain.
Status:
Investigational
Source:
NCT01677754: Phase 2 Interventional Completed Alzheimer's Disease
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sembragiline is a potent, selective, long-acting, and reversible monoamine oxidase B (MAO-B) inhibitor developed as a potential treatment for Alzheimer's disease (AD). Sembragiline was involved in phase II clinical trial to evaluate its the safety, tolerability, and efficacy in patients with moderate AD. In addition, the drug was studied for smoking cessation, however, it failed to demonstrate efficacy during a phase II proof-of-concept trial.
Status:
Investigational
Source:
NCT00525213: Phase 2 Interventional Completed Rheumatoid Arthritis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Rabeximod is an indolo[2,3-b]quinoxaline derivative patented by OxyPharma AB as anti-inflammatory agent useful for the treatment of autoimmune disease. Rabeximod impaired monocyte differentiation into monocyte-derived dendritic cells and pro-inflammatory allostimulated macrophages. Monocyte-derived dendritic cells that were treated with Rabeximod resulted in a significant decrease in their ability to pinocytose antigens, while no effect was exerted by the drug on the ability of allostimulated macrophages and anti-inflammatory macrophages to phagocytose. Rabeximod reduces the severity of arthritis in rodent models of rheumatoid arthritis and multiple sclerosis. Rabeximod efficiently prevented arthritis during the time window when TLR2 or TLR4 ligands activate inflammatory macrophages.
Status:
Investigational
Source:
NCT03830684: Phase 2 Interventional Unknown status Influenza
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Baicalein is a flavonoid is a component of the traditional herbal remedy known as Chinese skullcap (or Huang Qin), possesses various biological activities. Baicalein is a neuroprotective agent, which is studied in phase I for the treatment of Parkinson’s disease. By modulating of γ-aminobutyric acid (GABA) type A receptors, baicalein promotes nonamyloidogenic processing of amyloid precursor protein (APP), thereby reducing β-amyloid (Aβ) production and improving cognitive performance in models of Alzheimer's disease. By inhibiting the NF-κB signaling pathway, baicalein suppressed cancer cells proliferation and suppressed the viability of human endometrial stromal cells, thus it may provide a novel treatment option for endometriosis. Besides, this compound was evaluated for its ability to inhibit the influenza virus. Experiments on mice have shown that baicalein showed significant effects in preventing death, increasing the mean time to death and reducing the lung virus titer in a dose-dependent manner.
Status:
Investigational
Source:
INN:maridomycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Maridomycin is a macrolide antibiotic. Sreptomyces sp. No. B-5050 was found to produce maridomycin. Maridomycin was found to be composed of six components, maridomycins I, II, III, IV, V and VI. Their structures are different from each other in acyl moieties at C3 and C4" positions. Maridomycins I, II, III, IV, V and VI showed similar antibacterial spectra against Gram-positive bacteria including acid-fast bacteria. Maridomycin has bacteriostatic activity rather than bactericidal activity. Prominent therapeutic effect was observed against certain Gram-positive bacterial infection in mice.